PMID
Article Title
Citation
Organization
Download
View Data
The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 458-64 (2008)
Pharmasset
Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6316-25 (2007)
University of Manchester
Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 423-6 (2008)
University of Bologna
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 256-61 (2008)
F. Hoffmann-La Roche
Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 909-21 (2008)
Kissei Pharmaceutical
2D QSAR and similarity studies on cruzain inhibitors aimed at improving selectivity over cathepsin L.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 838-53 (2008)
Universidade De S£O Paulo
Cytochrome P3A4 inhibitors and other constituents of Fibraurea tinctoria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1930-3 (2007)
National Cheng Kung University
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6367-82 (2007)
Nitromed
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6356-66 (2007)
Neurocrine Biosciences
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6383-91 (2007)
Research Triangle Institute
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 6303-6 (2007)
Merck Research Laboratories
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 16: 1242-53 (2008)
Universite Paris 7-Denis Diderot
Discovery of potent& selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6095-103 (2007)
Pfizer
Characterization of thyroid hormone receptor alpha (TRalpha)-specific analogs with varying inner- and outer-ring substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 762-70 (2008)
University of California San Francisco
Discovery of new MurF inhibitors via pharmacophore modeling and QSAR analysis followed by in-silico screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1218-35 (2008)
University of Jordan
Synthesis and evaluation of novel aromatic substrates and competitive inhibitors of GABA aminotransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 3122-5 (2008)
Northwestern University
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 215-9 (2008)
Schering-Plough Research Institute
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1304-8 (2008)
University of Maryland
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5886-9 (2007)
Pfizer
Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Comb Chem 10: 56-62 (2008)
Schering-Plough Research Institute
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1691-5 (2007)
Seoul National University
New potent indole derivatives as hyaluronidase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 70: 547-51 (2007)
TBA
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5912-25 (2007)
Astrazeneca Pharmaceuticals
Discovery of a novel warhead against beta-secretase through fragment-based lead generation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5903-11 (2007)
Astrazeneca R&D
Design and synthesis of indole-based peptoids as potent noncompetitive antagonists of transient receptor potential vanilloid 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6133-43 (2007)
University of Barcelona
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5976-83 (2007)
Georgetown University Medical Center
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1359-75 (2008)
Osi Pharmaceuticals
Synthesis and characterization of carnitine nitro-derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1444-51 (2008)
University of Perugia
Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 783-93 (2008)
Emory University
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 304-8 (2008)
F. Hoffmann-La Roche
Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 285-8 (2008)
Gakushuin University
Surveying polypeptide and protein domain conformation and association with FlAsH and ReAsH.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 779-84 (2007)
Yale University
Model structure of the Na+/H+ exchanger 1 (NHE1): functional and clinical implications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 37854-63 (2007)
Tel-Aviv University
Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 402-4 (2008)
The University of Sydney
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 18: 324-8 (2008)
Gsk
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1469-77 (2008)
Université
GRIND-based 3D-QSAR to predict inhibitory activity for similar enzymes, OSC and SHC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1462-8 (2008)
Casmedchem Laboratory
Synthesis and biological activity of imidazopyridine anticoccidial agents: Part II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1123-51 (2008)
Scynexis
Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1478-88 (2008)
Freie UniversitäT Berlin
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1299-308 (2008)
Dainippon Sumitomo Pharma
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1279-86 (2008)
Mclean Hospital
Design, synthesis, FGF-1 binding, and molecular modeling studies of conformationally flexible heparin mimetic disaccharides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 344-9 (2008)
Progen Pharmaceuticals
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 409-13 (2008)
Johnson & Johnson Pharmaceutical Research and Development
Combined 3D QSAR and molecular docking studies to reveal novel cannabinoid ligands with optimum binding activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6754-63 (2007)
The National Hellenic Research Foundation
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6841-6 (2007)
Eli Lilly
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 418-22 (2008)
Schering-Plough Research Institute
Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 18: 405-8 (2008)
Johnson & Johnson Pharmaceutical Research and Development
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5951-66 (2007)
Zydus Research Centre
Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1309-18 (2008)
Korea Food Research Institute
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1376-92 (2008)
University of Minnesota
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 650-7 (2008)
Kyoto University
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6729-33 (2007)
Methylgene
Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6697-700 (2007)
Universitat Jaume I
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6707-13 (2007)
Pfizer
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6691-6 (2007)
Pfizer
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1152-9 (2008)
Johannes Gutenberg University
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5967-75 (2007)
University of Southern California
Multiple N-methylation by a designed approach enhances receptor selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5878-81 (2007)
Technische UniversitäT MüNchen
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5890-3 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6265-73 (2007)
Abbott Laboratories
Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6059-66 (2007)
Cancercare Manitoba
Interactions of methylene blue with human disulfide reductases and their orthologues from Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 183-91 (2007)
Biochemie-Zentrum Der Universit£T Heidelberg
Madurahydroxylactone derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and RNase H.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 361-4 (2008)
National Cancer Institute
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 225-36 (2008)
Imquest Biosciences
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 157-63 (2008)
University of Pittsburgh School of Medicine
Synthesis and heparanase inhibitory activity of sulfated mannooligosaccharides related to the antiangiogenic agent PI-88.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 699-709 (2008)
Progen Pharmaceuticals
Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 771-82 (2008)
Universidade Federal Do Rio Grande Do Sul (Ufrgs)
Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6887-90 (2007)
Pfizer
Structure-activity relationships of adenosines with heterocyclic N6-substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6779-84 (2007)
Monash University (Parkville Campus)
5'-O-[(N-acyl)sulfamoyl]adenosines as antitubercular agents that inhibit MbtA: an adenylation enzyme required for siderophore biosynthesis of the mycobactins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6080-94 (2007)
University of Minnesota
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6144-53 (2007)
University M£Nster
Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 739-45 (2008)
University of South Carolina
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 981-94 (2008)
Nippon Shinyaku
Spermatinamine, the first natural product inhibitor of isoprenylcysteine carboxyl methyltransferase, a new cancer target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6860-3 (2007)
Griffith University
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6811-5 (2007)
F. Hoffmann-La Roche
Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6832-5 (2007)
Cardiff University
Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 209-21 (2008)
Lek Pharmaceuticals
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 902-8 (2008)
Sapienza University of Rome
Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 16: 746-54 (2008)
Research Triangle Institute
Discovery of small-molecule inhibitors of tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6871-5 (2007)
University of Texas Southwestern Medical Center
Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6806-10 (2007)
Ucb Pharma
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6825-31 (2007)
Neurocrine Biosciences
Structure activity relationships of quinoline-containing c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1321-9 (2008)
Pfizer
Activity of sulfonium bisphosphonates on tumor cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6067-79 (2007)
University of Illinois At Urbana-Champaign
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5882-5 (2007)
Astrazeneca R&D Charnwood
Discovery of 5-Substituted-6-chlorouracils as Efficient Inhibitors of Human Thymidine Phosphorylase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 6016-23 (2007)
Gilead Sciences
Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 36905-13 (2007)
University of Utah
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 869-73 (2008)
University of Maryland
Discovery of long-acting N-(cyanomethyl)-N-alkyl-L-prolinamide inhibitors of dipeptidyl peptidase IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 190-208 (2008)
Minase Research Institute
Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 1186-97 (2007)
University of Virginia At Charlottesville
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6154-64 (2007)
University of Wisconsin-Madison
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 6004-15 (2007)
Universidad De La RepúBlica
Cytotoxic metabolites from an Indonesian sponge Lendenfeldia sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1824-6 (2007)
University of Mississippi
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5568-70 (2007)
University of Antwerp
Discovery of small molecule CXCR4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5655-64 (2007)
Emory University
Probing Binding Requirements of Type I and Type II Isoforms of Inosine Monophosphate Dehydrogenase with Adenine-Modified Nicotinamide Adenine Dinucleotide Analogues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5743-5751 (2007)
University of Minnesota At Twin Citiies
The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5720-5726 (2007)
University of Southampton
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 17335-40 (2007)
Istituto Di Ricerche Di Biologia Molecolare
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5752-64 (2007)
University Hospital of The Westf£Lische Wilhelms-Universit£T M£Nster
Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5644-54 (2007)
Università
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5853-7 (2007)
Memorial Sloan-Kettering Cancer Center
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 17347-52 (2007)
Institut National De La Sant£
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 128-36 (2008)
Duke University Medical Center
In silico screening of HIV-1 non-nucleoside reverse transcriptase and protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1412-22 (2008)
Universidade Federal De Minas Gerais
Acetyl-lysine analog peptides as mechanistic probes of protein deacetylases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 37256-65 (2007)
University of Wisconsin-Madison
Synthesis and structure-activity relationships of N-{1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide derivatives as novel CCR3 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 144-56 (2008)
Astellas Pharma
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 6463-6 (2007)
The Scripps Research Institute
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6472-5 (2007)
University of Southern California
Structure of a novel thrombin inhibitor with an uncharged D-amino acid as P1 residue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1330-5 (2008)
Institut FüR Biochemie
Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6434-8 (2007)
Université
Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1188-98 (2008)
Medical University of Gdansk
Vanillic acid derivatives from the green algae Cladophora socialis as potent protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1790-2 (2007)
Griffith University
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 46: 13019-30 (2007)
Pfizer
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5735-42 (2007)
University of Kansas
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5863-5867 (2007)
University of California Davis
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5535-8 (2007)
Wyeth Research
Design of mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and new structural templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5589-99 (2007)
Institute of Sciences
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5712-9 (2007)
Pfizer
Mechanisms, biology and inhibitors of deubiquitinating enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 697-705 (2007)
Institute For Bio-Medical Research
First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5685-95 (2007)
University of Bonn
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6584-7 (2007)
Glaxosmithkline
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6623-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6505-10 (2007)
Universit£
Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6439-43 (2007)
Universidad De Navarra
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5543-6 (2007)
Methylgene
Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5547-9 (2007)
Wyeth Research
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5727-34 (2007)
St. Jude Research Hospital
New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5600-7 (2007)
University of Bonn
Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 52: 110-20 (2008)
Vertex Pharmaceuticals
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 276-83 (2008)
The University of The West Indies
Design, synthesis, and preliminary evaluation of 4-(6-(3-nitroguanidino)hexanamido)pyrrolidine derivatives as potential iNOS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 578-85 (2008)
Shandong University
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6448-54 (2007)
Astrazeneca
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6476-80 (2007)
Bristol-Myers Squibb Research and Development
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6539-45 (2007)
Amgen
2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6467-71 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1222-9 (2008)
Universit£
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 362-73 (2008)
Universit£
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 530-5 (2008)
Yonsei University
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6525-8 (2007)
Pfizer
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6593-601 (2007)
Abbott Laboratories
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6516-20 (2007)
Institute
A phosphorylated prodrug for the inhibition of Pin1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6615-8 (2007)
Virginia Tech
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6529-34 (2007)
Pfizer
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1611-5 (2007)
University of ZüRich
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 336-53 (2008)
Universit£
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6567-71 (2007)
The Institute of Cancer Research
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6489-92 (2007)
Johnson & Johnson Pharmaceutical Research & Development
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6493-8 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6481-8 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6546-52 (2007)
Neurocrine Biosciences
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 36829-36 (2007)
Bristol-Myers Squibb Research and Development
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6499-504 (2007)
Abbott Laboratories
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6572-5 (2007)
Emd-Serono Research Institute
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6511-5 (2007)
Merck Research Laboratories
2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6579-83 (2007)
Heriot-Watt University
3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6619-22 (2007)
Arena Pharmaceuticals
Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5425-38 (2007)
Nagoya City University
Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5561-3 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5493-508 (2007)
Neuroscience Research
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5564-7 (2007)
Merck Research Laboratories
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5550-3 (2007)
Schering-Plough Research Institute
Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5579-88 (2007)
Università
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5676-84 (2007)
Universit£
Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5790-5806 (2007)
Cnrs
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5528-32 (2007)
University of Arizona Tucson
A small-molecule therapeutic lead for Huntington's disease: preclinical pharmacology and efficacy of C2-8 in the R6/2 transgenic mouse.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 16685-9 (2007)
Harvard Medical School
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5824-32 (2007)
The Johns Hopkins University
De novo discovery of serotonin N-acetyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5330-8 (2007)
Johns Hopkins School of Medicine
Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4324-8 (2007)
Tulane University School of Medicine
ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Chem Biol 3: 722-6 (2007)
Glaxosmithkline
Profiling the enzymatic properties and inhibition of human complement factor B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 34809-16 (2007)
University of Queensland
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 6633-7 (2007)
Amgen
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 422-7 (2008)
Neurocrine Biosciences
Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 322-35 (2008)
Clemson University
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6056-61 (2007)
Amgen
Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6079-85 (2007)
Pfizer
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5439-48 (2007)
Abbott Laboratories
Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5249-52 (2007)
Neurocrine Biosciences
Inhibitors of the Interaction of a Thyroid Hormone Receptor and Coactivators: Preliminary Structure-Activity Relationships.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5269-5280 (2007)
St. Jude Research Hospital
Interactions of hepatitis B core antigen and peptide inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5620-6 (2007)
Universiti Putra Malaysia
Target specific virtual screening: optimization of an estrogen receptor screening platform.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5301-10 (2007)
Trinity College
Synthesis and structure-activity relationship for a novel class of potent and selective carbamate-based inhibitors of hormone selective lipase with acute in vivo antilipolytic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5449-56 (2007)
Novo Nordisk
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5403-11 (2007)
Sapienza University of Rome
CYP2C9 structure-metabolism relationships: substrates, inhibitors, and metabolites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5382-91 (2007)
Astrazeneca R&D MöLndal
Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5848-5852 (2007)
University of Pavia
Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: consequences in receptor affinity and functionality.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5471-84 (2007)
Université
Small molecule inhibitors of integrin alpha2beta1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5457-62 (2007)
University of Pennsylvania
Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5339-56 (2007)
Bristol-Myers Squibb
A surface on the androgen receptor that allosterically regulates coactivator binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 16074-9 (2007)
University of California
Potent oxindole based human beta3 adrenergic receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6270-3 (2007)
Eli Lilly
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6378-82 (2007)
Scripps Florida
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6066-9 (2007)
Glaxosmithkline
Substituted 2-pyrrolinone inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6155-9 (2007)
University of Southern California
Novel scaffold for cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6096-100 (2007)
Novartis Institutes For Biomedical Research
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6151-4 (2007)
Bayer Healthcare
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5412-24 (2007)
Universit£
Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5364-71 (2007)
University of Bari
Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5281-92 (2007)
University of Gent
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 390-9 (2008)
University of Iowa
Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6212-5 (2007)
Pedagogical University
Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7803-8 (2007)
Hoshi University
Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6070-4 (2007)
Johnson and Johnson Pharmaceutical Research and Development
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6234-8 (2007)
Korea Research Institute of Bioscience and Biotechnology
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6111-5 (2007)
Holden Laboratories
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6220-3 (2007)
Schering-Plough Research Institute
Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6123-8 (2007)
Johnson & Johnson Pharmaceutical Research and Development
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 457-73 (2008)
Tokyo Medical and Dental University
Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5245-8 (2007)
Wyeth Research
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5311-23 (2007)
Cnrs
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7576-80 (2007)
Purdue University
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7581-9 (2007)
Università
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 437-45 (2008)
Graduate School of Life Science and Systems Engineering
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6280-5 (2007)
Merck Research Laboratories
Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5135-46 (2007)
Université
Lateral compartmentalization of T cell receptor versus CD45 by galectin-N-glycan binding and microfilaments coordinate basal and activation signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 35361-72 (2007)
University of California
Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 36505-13 (2007)
The Scripps Research Institute
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6188-91 (2007)
Pfizer
Inhibition of human dimethylarginine dimethylaminohydrolase-1 by S-nitroso-L-homocysteine and hydrogen peroxide. Analysis, quantification, and implications for hyperhomocysteinemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 34684-92 (2007)
University of Texas
1,3-disubstituted ureas functionalized with ether groups are potent inhibitors of the soluble epoxide hydrolase with improved pharmacokinetic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5217-26 (2007)
Department of Entomology and University of California Davis Cancer Center
Phenylimidazole derivatives as specific inhibitors of bacterial enoyl-acyl carrier protein reductase FabK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7325-36 (2007)
Meiji Seika Kaisha
Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6160-3 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of 5-HT6 receptor ligands based on virtual HTS.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6224-9 (2007)
4Sc
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6261-5 (2007)
Université
New functional assay of P-glycoprotein activity using Hoechst 33342.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7470-9 (2007)
University of Bonn
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6290-4 (2007)
Schering-Plough Research Institute
Androstene-3,5-dienes as ER-beta selective SERMs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6295-8 (2007)
Merck Research Laboratories
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7626-37 (2007)
Universit£
Facile one-pot synthesis of thio and selenourea derivatives: a new class of potent urease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6387-91 (2007)
Institute of Science
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6172-7 (2007)
Merck Research Laboratories
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6178-82 (2007)
Epicept
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6373-7 (2007)
Development Center For Biotechnology
2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6266-9 (2007)
Johnson & Johnson
Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6245-9 (2007)
Peking University
Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7391-8 (2007)
University of Mysore
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6250-6 (2007)
Pfizer
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5176-82 (2007)
University of Bath
Macrolactins O-R, glycosylated 24-membered lactones from Bacillus sp. AH159-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1632-5 (2007)
Korea Research Institute of Bioscience and Biotechnology
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5253-6 (2007)
Pfizer
Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 5049-52 (2007)
Ligand Pharmaceuticals
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5202-16 (2007)
Bayer Pharmaceuticals
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5886-93 (2007)
Glaxosmithkline
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6299-304 (2007)
Taisho Pharmaceutical
Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6305-10 (2007)
Molecular Cancer Research Center
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6183-7 (2007)
Astrazeneca R&D Montreal
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6206-11 (2007)
Novartis Institutes For Biomedical Research
Rynaxypyr: a new insecticidal anthranilic diamide that acts as a potent and selective ryanodine receptor activator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6274-9 (2007)
Fmc Stine Research Center
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1570-7 (2007)
Chinese Academy of Sciences
Novel C2-purine position analogs of nitrobenzylmercaptopurine riboside as human equilibrative nucleoside transporter 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7726-37 (2007)
University of Tennessee Health Sciences Center
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7830-9 (2007)
Graduate School of Life Science and Systems Engineering
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5103-8 (2007)
Solvay Pharma
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5090-102 (2007)
University of Auckland
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5161-7 (2007)
Elan Pharmaceuticals
Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 15490-5 (2007)
Metabasis Therapeutics
Biochemical Characterization of SFC-1, a class A carbapenem-hydrolyzing beta-lactamase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4512-4 (2007)
University of Aveiro
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4356-60 (2007)
National Science and Technology Development Agency
In vitro efficacy of new antifolates against trimethoprim-resistant Bacillus anthracis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4447-52 (2007)
Oklahoma State University
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 33052-63 (2007)
University of California San Francisco
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7399-407 (2007)
Peking University
Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7344-54 (2007)
Uppsala University
Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7480-93 (2007)
Instituto De QuíMica MéDica
Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7865-77 (2007)
Università
Two new phenylpiperazines with atypical antipsychotic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5749-53 (2007)
Institute For Biological Research
Synthesis of novel anilinoquinolines as c-fms inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6257-60 (2007)
Glaxosmithkline
Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1248-60 (2008)
The University of Manchester
4-thiazolidinone--a biologically active scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 897-905 (2008)
Northern India Engineering College
The molecular pruning of a phosphoramidate peptidomimetic inhibitor of prostate-specific membrane antigen.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7434-43 (2007)
San Francisco State University
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7677-87 (2007)
University of Auckland
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7361-7 (2007)
Central Drug Research Institute
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6003-8 (2007)
Amgen
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6326-9 (2007)
Astrazeneca
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5853-7 (2007)
Merck Research Laboratories
Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5863-7 (2007)
Mitsubishi Pharma
Amino-caprolactam derivatives as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5790-5 (2007)
Bristol-Myers Squibb Research and Development
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1276-96 (2008)
University of Auckland
Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7380-90 (2007)
Università
Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7408-25 (2007)
Universidad De Santiago De Chile
Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5964-8 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of potent T-type calcium channel blocker.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5740-3 (2007)
Kyung Hee University
High dopamine transporter selectivity can be displayed by remarkably simple non-nitrogen containing inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6019-25 (2007)
University of Aarhus
Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5928-33 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5918-23 (2007)
F. Hoffmann-La Roche
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5076-89 (2007)
Glaxosmithkline
Synthesis and radioligand binding studies of bis-isoquinolinium derivatives as small conductance Ca(2+)-activated K(+) channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5070-5 (2007)
University of Li£Ge
Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 32549-60 (2007)
Lund University
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 34663-71 (2007)
Merck Research Laboratories
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5754-7 (2007)
Rti International
Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5876-80 (2007)
Purdue University
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5952-8 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5796-800 (2007)
Wyeth Research
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5147-60 (2007)
Schering-Plough Research Institute
Brunneins A-C, beta-carboline alkaloids from Cortinarius brunneus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1529-31 (2007)
Institute of Plant Biochemistry
Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7809-29 (2007)
Institute of Pharmaceutical Industry
Myricetin inhibits Escherichia coli DnaB helicase but not primase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7203-8 (2007)
University of Nebraska-Lincoln
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6876-81 (2007)
University of Ferrara
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5806-11 (2007)
Merck Research Laboratories
Inactivation of soybean sterol 24-C-methyltransferase by elongated sterol side chains at C26.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5902-6 (2007)
Texas Tech University
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5825-30 (2007)
Amgen
The selectivity of protein kinase inhibitors: a further update.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem J 408: 297-315 (2007)
University of Dundee
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4882-97 (2007)
University of Bologna
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4789-92 (2007)
James Black Foundation
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5043-7 (2007)
Università
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4928-38 (2007)
Montana State University
Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4993-5002 (2007)
University of Florence
Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4808-17 (2007)
Instituto Universitario De Bio-Organica Antonio Gonzalez
Discovery of a new series of potent and selective linear tachykinin NK2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4793-807 (2007)
Menarini Ricerche
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4976-85 (2007)
Institute Genomics Functional (Igf)
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 33295-304 (2007)
Wyeth Research
Accumulation of glucosylceramide in murine testis, caused by inhibition of beta-glucosidase 2: implications for spermatogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 32655-64 (2007)
University of Oxford
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4133-40 (2007)
Veterans Affairs Medical Center
Molecular and biochemical characterization of the chromosome-encoded class A beta-lactamase BCL-1 from Bacillus clausii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4009-14 (2007)
H�Pital De Bic�Tre
Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Antimicrob Agents Chemother 51: 3915-23 (2007)
University of California San Francisco
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7184-202 (2007)
LinköPing University
Is adamantane a suitable substituent to pre-organize the acid orientation in E-selectin antagonists?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 16: 1046-56 (2008)
University of Basel
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5924-7 (2007)
University of Southern Denmark
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5003-11 (2007)
Universit£
Pyrido[1,2-a]pyrimidin-4-one derivatives as a novel class of selective aldose reductase inhibitors exhibiting antioxidant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4917-27 (2007)
Università
Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4845-53 (2007)
University of Queensland
Benzochromenones from the marine crinoid Comantheria rotula inhibit hypoxia-inducible factor-1 (HIF-1) in cell-based reporter assays and differentially suppress the growth of certain tumor cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1462-6 (2007)
University of Mississippi
Novel, potent THC/anandamide (hybrid) analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7850-64 (2007)
Organix
Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6956-74 (2007)
Jagiellonian University Medical College
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7248-57 (2007)
Friedrich-Alexander University
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5465-71 (2007)
Universit£
Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5472-8 (2007)
Pfizer
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5944-51 (2007)
Abbott Laboratories
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5812-8 (2007)
Targegen
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5831-5 (2007)
Merck Research Laboratories
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5978-82 (2007)
Tanabe Research Laboratories Usa
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 6013-8 (2007)
Astrazeneca
N(4)-Phenyl modifications of N(2)-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5783-9 (2007)
Nih
Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5995-9 (2007)
Entremed
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5934-9 (2007)
Merck Research Laboratories
Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5872-5 (2007)
University of Toyama
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5983-8 (2007)
Pfizer
Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5940-3 (2007)
University of Texas Medical Branch
Conformationally constrained analogues of 2-arachidonoylglycerol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5959-63 (2007)
Northeastern University
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5768-71 (2007)
Kobe Gakuin University
5'-halogenated analogs of oxymorphindole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5916-7 (2007)
University of Maryland
Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7229-36 (2007)
Kochi Medical School
Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6900-8 (2007)
University of California
Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7138-43 (2007)
Yeungnam University
Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7258-73 (2007)
Johann Wolfgang Goethe University
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5514-7 (2007)
Glaxosmithkline
On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5590-4 (2007)
Université
Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 7166-83 (2007)
Uppsala University
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 7116-25 (2007)
Polish Academy of Sciences
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4953-75 (2007)
Irbm-Mrl
Structural Modification of the P2' Position of 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The Discovery of Aliskiren, a Potent Nonpeptide Human Renin Inhibitor Active after Once Daily Dosing in Marmosets.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4832-44 (2007)
Novartis Pharmaceuticals
Novel 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamide Transition State Peptidomimetics Are Potent and Orally Active Inhibitors of Human Renin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4818-31 (2007)
Novartis Pharmaceuticals
Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4909-16 (2007)
University of Bari
Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6975-84 (2007)
Assiut University
Pyrazole-based cathepsin S inhibitors with improved cellular potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5525-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5614-9 (2007)
University of Minnesota
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5595-9 (2007)
Merck Research Laboratories
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5704-8 (2007)
Corcept Therapeutics
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5610-3 (2007)
Neurocrine Biosciences
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5634-7 (2007)
Shaheed Beheshti University of Medical Sciences
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5638-42 (2007)
Pfizer
3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1025-34 (2008)
Biocampus
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1458-61 (2007)
Chinese Academy of Sciences
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5630-3 (2007)
Wyeth Research
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5671-6 (2007)
Merck Research Laboratories
Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5543-7 (2007)
Schering-Plough Research Institute
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5573-6 (2007)
Chugai Pharmaceutical
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5600-4 (2007)
Eli Lilly
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5989-94 (2007)
Merck Research Laboratories
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5563-6 (2007)
Eli Lilly
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5577-81 (2007)
Astellas Pharma
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5620-3 (2007)
Arena Pharmaceuticals
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5024-33 (2007)
Pierre Fabre Research Center
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4854-67 (2007)
Purdue University
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5665-70 (2007)
Abbott Laboratories
Discovery of novel and orally active NR2B-selective N-methyl-D-aspartate (NMDA) antagonists, pyridinol derivatives with reduced HERG binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5533-6 (2007)
Pfizer
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5720-3 (2007)
Merck
Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5656-60 (2007)
Vanderbilt University
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5647-51 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5693-7 (2007)
Pfizer
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5677-82 (2007)
Merck Research Laboratories
Synthesis and biological evaluation of a C5-biphenyl thiolactomycin library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5643-6 (2007)
University of Birmingham
Novel anti-infection agents: small-molecule inhibitors of bacterial transcription factors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5652-5 (2007)
Paratek Pharmaceuticals
Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5537-42 (2007)
Pfizer
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5558-62 (2007)
Pfizer
Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6834-45 (2007)
University of London
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6819-29 (2007)
Johannes Gutenberg University
Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5325-9 (2007)
Johnson & Johnson Pharmaceutical Research and Development
A refined agonist pharmacophore for protease activated receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5552-7 (2007)
University of Queensland
Nucleation of an allosteric response via ligand-induced loop folding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 373: 96-111 (2007)
University of Maryland College Park
Novel (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic ester prodrugs possessing a diazen-1-ium-1,2-diolate moiety: design, synthesis, cyclooxygenase inhibition, and nitric oxide release studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6796-801 (2007)
University of Alberta
Thiazole-diamides as potent gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5518-22 (2007)
Pfizer
Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5567-72 (2007)
Pfizer
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5529-32 (2007)
Pfizer
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5686-9 (2007)
Crystalgenomics
Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5012-23 (2007)
Universidad Complutense
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6810-8 (2007)
Waseda University
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5390-5 (2007)
Merck Research Laboratories
Thiophene substituted acylguanidines as BACE1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5353-6 (2007)
Wyeth Research
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5330-5 (2007)
Schering-Plough Research Institute
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5300-9 (2007)
Merck Research Laboratories
Influence of conformation on GRIND-based three-dimensional quantitative structure-activity relationship (3D-QSAR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 5039-42 (2007)
Universit£
2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5357-60 (2007)
Inha University
Novel ATP-competitive kinesin spindle protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4939-52 (2007)
Glaxosmithkline
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4630-41 (2007)
Universit£
A Ser678Pro substitution in Fks1p confers resistance to echinocandin drugs in Aspergillus fumigatus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4174-6 (2007)
Umdnj-New Jersey Medical School
Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 30699-706 (2007)
University of Utah
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6649-58 (2007)
Incyte
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5310-5 (2007)
Merck Research Laboratories
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5428-31 (2007)
Darmstadt University of Technology
Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5396-9 (2007)
Pfizer
Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4669-80 (2007)
Université
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4616-29 (2007)
University of Copenhagen
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4868-81 (2007)
Astrazeneca Discovery
L-(+)-2-Amino-4-thiophosphonobutyric acid (L-thioAP4), a new potent agonist of group III metabotropic glutamate receptors: increased distal acidity affords enhanced potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4656-64 (2007)
Université
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4585-605 (2007)
University of Washington
Synthesis and structure-affinity relationships of new 4-(6-iodo-H-imidazo[1,2-a]pyridin-2-yl)-N-dimethylbenzeneamine derivatives as ligands for human beta-amyloid plaques.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4746-58 (2007)
National Institute of Mental Health
Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5340-4 (2007)
Gedeon Richter
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5349-52 (2007)
Eli Lilly
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5455-61 (2007)
Bristol-Myers Squibb
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1008-14 (2008)
Università
Virtual screening application of a model of full-length HIV-1 integrase complexed with viral DNA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5361-5 (2007)
National Cancer Institute
Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 70: 268-72 (2007)
Pfizer
Crystal structure of the T315I mutant of AbI kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 70: 171-81 (2007)
Ariad Pharmaceuticals
Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5336-9 (2007)
University of Tartu
Toward novel HIV-1 integrase binding inhibitors: molecular modeling, synthesis, and biological studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5370-3 (2007)
Universit£
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5366-9 (2007)
Seoul National University
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4728-45 (2007)
Wyeth Research
Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 30062-9 (2007)
Université
Exploration of physicochemical properties and molecular modelling studies of 2-sulfonyl-phenyl-3-phenyl-indole analogs as cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1297-303 (2008)
Institute of Technology and Science
Phenylimidazole derivatives of 4-pyridone as dual inhibitors of bacterial enoyl-acyl carrier protein reductases FabI and FabK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4710-20 (2007)
Meiji Seika Kaisha
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4648-55 (2007)
Universit£
Novel small-molecule inhibitors of transmissible gastroenteritis virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3924-31 (2007)
National Health Research Institute
TEM-158 (CMT-9), a new member of the CMT-type extended-spectrum beta-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4181-3 (2007)
Chu Clermont-Ferrand
Quinuclidine derivatives as potential antiparasitics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4049-61 (2007)
Cardiff University
Correlation of carboxylic acid pKa to protein binding and antibacterial activity of a novel class of bacterial translation inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5479-82 (2007)
Pharmacia
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5384-9 (2007)
Amgen
Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1397-405 (2007)
University of Mississippi
Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 949-57 (2008)
National Institute of Pharmaceutical Education and Research
QSAR studies on benzoylaminobenzoic acid derivatives as inhibitors of beta-ketoacyl-acyl carrier protein synthase III.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 1071-80 (2008)
Shri G.S. Institute of Technology and Science
Pyrimidine benzamide-based thrombopoietin receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5447-54 (2007)
Pfizer
Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 830-8 (2008)
University College of Pharmaceutical Sciences
Schiff base transition metal complexes as novel inhibitors of xanthine oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 862-71 (2008)
Nanjing University
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4699-709 (2007)
Ligand Pharmaceuticals
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4681-98 (2007)
Wyeth Research
Synthesis and in vivo evaluation of fluorine-18 and iodine-123 labeled 2beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane as a candidate serotonin transporter imaging agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4553-60 (2007)
Emory University
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5442-6 (2007)
Ligand Pharmaceuticals
Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 29803-11 (2007)
University of Washington
Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 29441-7 (2007)
Yale University
Targeting of the Brucella suis virulence factor histidinol dehydrogenase by histidinol analogues results in inhibition of intramacrophagic multiplication of the pathogen.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3752-5 (2007)
University of Montpellier
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 621-32 (2008)
Sapienza University of Rome
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6574-95 (2007)
Amgen
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4509-15 (2007)
Georgia State University
Design and Synthesis of HIV-1 Protease Inhibitors Incorporating Oxazolidinones as P2/P2' Ligands in Pseudosymmetric Dipeptide Isosteres.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4316-28 (2007)
University of Massachusetts Medical School
Conformation-activity relationship of neuropeptide S and some structural mutants: helicity affects their interaction with the receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4501-8 (2007)
Istituto Di Chimica Biomolecolare
3,17-disubstituted 2-alkylestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4431-43 (2007)
University of Bath
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4351-4373 (2007)
Amgen
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4471-81 (2007)
University of Southern California
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4374-81 (2007)
University of Tennessee At Knoxville
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 13827-32 (2007)
University of Utah
Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5462-4 (2007)
Amorepacific
New amido derivatives as potential BKCa potassium channel activators. XI.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 792-9 (2008)
Universit£
Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6535-48 (2007)
Inha University
Identification of dissociated non-steroidal glucocorticoid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5025-31 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5432-6 (2007)
Merck Research Laboratories
Aldehyde dehydrogenase inhibitors: alpha,beta-acetylenic N-substituted aminothiolesters are reversible growth inhibitors of normal epithelial but irreversible apoptogens for cancer epithelial cells from human prostate in culture.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 906-16 (2008)
Claude Bernard University Lyon 1
Synthesis of N-aryl-5-amino-4-cyanopyrazole derivatives as potent xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 771-80 (2008)
Universidade Do Minho
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 966-72 (2008)
University of Montpellier
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4405-18 (2007)
University of Regensburg
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4516-27 (2007)
University of Dublin
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 317: 1390-3 (2007)
New York University School of Medicine
Towards predictive inhibitor design for the EGFR autophosphorylation activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 781-91 (2008)
Korea Institute of Science and Technology
Dual acting antioxidant A1 adenosine receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5437-41 (2007)
Monash University (Parkville Campus)
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5406-9 (2007)
Abbott Laboratories
Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 28501-13 (2007)
University WüRzburg
3,3-diphenylpentane skeleton as a steroid skeleton substitute: novel inhibitors of human 5alpha-reductase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5414-8 (2007)
The University of Tokyo
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1278-82 (2007)
The University of Iowa
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4265-8 (2007)
University Di Perugia
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4279-94 (2007)
Targegen
2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4261-4 (2007)
Johnson & Johnson Pharmaceutical
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 13283-8 (2007)
Center For Molecular Medicine of The Austrian Academy of Sciences
4-Hydroxynonenal, an endogenous aldehyde, causes pain and neurogenic inflammation through activation of the irritant receptor TRPA1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 13519-24 (2007)
Florence University
Structure of compstatin in complex with complement component C3c reveals a new mechanism of complement inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 29241-7 (2007)
Utrecht University
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5150-4 (2007)
Schering-Plough Research Institute
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6556-64 (2007)
Wyeth Research
Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6596-607 (2007)
Woosuk University
Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6367-78 (2007)
Dalhousie University
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5032-5 (2007)
Griffith University
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5091-5 (2007)
Boehringer Ingelheim Pharmaceuticals
Dopamine/serotonin receptor ligands. 16.(1) Expanding dibenz[d,g]azecines to 11- and 12-membered homologues. Interaction with dopamine D(1)-D(5) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4528-33 (2007)
Friedrich-Schiller-UniversitäT Jena
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4453-70 (2007)
Gsk
Targeting plague virulence factors: a combined machine learning method and multiple conformational virtual screening for the discovery of Yersinia protein kinase A inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3980-3 (2007)
The Rockefeller University
Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4482-92 (2007)
Paris-Sud University
Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4543-7 (2007)
Institute of Science and Technology
Structural and mechanistic basis of penicillin-binding protein inhibition by lactivicins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 565-9 (2007)
Universit£
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 28408-18 (2007)
University of Minnesota
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4177-85 (2007)
University of Copenhagen
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4135-46 (2007)
National Institute On Drug Abuse-Intramural Research Program
C1'-cycloalkyl side chain pharmacophore in tetrahydrocannabinols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4048-60 (2007)
National Hellenic Research Foundation
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 104: 13192-7 (2007)
Nih
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3883-90 (2007)
Lundbeck Research Usa
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3870-82 (2007)
Lundbeck Research Usa
Design, synthesis, and in vitro evaluation of carbamate derivatives of 2-benzoxazolyl- and 2-benzothiazolyl-(3-hydroxyphenyl)-methanones as novel fatty acid amide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4236-42 (2007)
Helsinki University of Technology
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4255-9 (2007)
Gnf
4-Substituted trinems as broad spectrum beta-lactamase inhibitors: structure-based design, synthesis, and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4113-21 (2007)
Lek Pharmaceuticals
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4061-74 (2007)
Università
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4027-37 (2007)
University of Athens
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3498-504 (2007)
Gilead Sciences
Plasmid-encoded ACC-4, an extended-spectrum cephalosporinase variant from Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3763-7 (2007)
Institute
The phenolic diterpene totarol inhibits multidrug efflux pump activity in Staphylococcus aureus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4480-3 (2007)
University of London
Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6425-42 (2007)
Wyeth Research
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5019-24 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
In vitro PAI-1 inhibitory activity of oxalamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 880-4 (2008)
Zydus Research Centre
Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4003-4015 (2007)
Nci-Fcrdc
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4753-5 (2007)
Wonkwang University
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5082-5 (2007)
Eli Lilly
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 323: 285-93 (2007)
Abbott Laboratories
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5175-6 (2007)
University of Maryland
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4162-76 (2007)
Abbott Laboratories
Discovery and optimization of p38 inhibitors via computer-assisted drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4016-26 (2007)
Boehringer Ingelheim Pharmaceuticals
New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4991-5 (2007)
University of Tours
Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 28096-105 (2007)
Michigan State University
Rational design, synthesis, and biological evaluation of progesterone-modified MRI contrast agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 824-34 (2007)
Northwestern University
Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 764-74 (2007)
The Johns Hopkins University
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4761-6 (2007)
University of Pennsylvania
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 5115-20 (2007)
Bristol-Myers Squibb
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 46: 9551-63 (2007)
Abbott Laboratories
Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 2: 536-44 (2007)
University of New Mexico Health Sciences Center
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4147-61 (2007)
University of Copenhagen
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 4250-4 (2007)
University of Bologna
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 13432-7 (2007)
University of California
Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4808-11 (2007)
Tsukuba Research Institute
Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4804-7 (2007)
Tsukuba Research Institute
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 4214-21 (2007)
Universita Degli Studi Di Bari
Biochemical and biophysical characterization of inhibitor binding to caspase-3 reveals induced asymmetry.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 46: 9462-71 (2007)
Wyeth Research
Design of protein membrane interaction inhibitors by virtual ligand screening, proof of concept with the C2 domain of factor V.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 12697-702 (2007)
Maastricht University
(R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 31542-8 (2007)
Institut De Biologie Et Chimie Des ProtéInes
A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6397-406 (2007)
Dr. Reddy'S Laboratories
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5041-8 (2007)
Bristol-Myers Squibb
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5133-5 (2007)
Taisho Pharmaceutical
Splicing factor SF3b as a target of the antitumor natural product pladienolide.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Chem Biol 3: 570-5 (2007)
Eisai
Cyclic nucleotide phosphodiesterase type 4 inhibitors: evaluation of pyrazolo[1,5-a]-1,3,5-triazine ring system as an adenine bioisostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 816-29 (2008)
Université
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cancer Res 67: 6916-24 (2007)
University Hospital Basel
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 4036-43 (2007)
Ambrilia Biopharma
Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6463-73 (2007)
Loma Linda University School of Medicine
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5191-8 (2007)
Merck
Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1370-81 (2007)
Central University of Las Villas
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3841-50 (2007)
University of Mississippi
Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3906-20 (2007)
University of Tennessee Health Science Center
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3777-85 (2007)
Gsk
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 129: 9613-5 (2007)
University of California Berkeley
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 28709-20 (2007)
Kumamoto University Graduate School of Medical and Pharmaceutical Sciences
Identification and mechanistic characterization of low-molecular-weight inhibitors for HuR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 508-15 (2007)
Novartis Institutes For Biomedical Research
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5245-50 (2007)
Pfizer
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 70: 1-12 (2007)
Abbott Laboratories
Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPalpha and TPbeta isoforms of the human thromboxane A2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3928-36 (2007)
University of LièGe
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3851-6 (2007)
Novartis Institutes For Biomedical Research
Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3964-8 (2007)
Università
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 12282-7 (2007)
University of North Carolina
Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5165-70 (2007)
Neurocrine Biosciences
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5218-21 (2007)
Glaxosmithkline
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5256-60 (2007)
Ranbaxy Research Laboratories
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5214-7 (2007)
Glaxosmithkline
Discovery and SAR studies of novel GlyT1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5233-8 (2007)
Eli Lilly
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6043-53 (2007)
Seoul National University
Inhibition of the bacterial heme oxygenases from Pseudomonas aeruginosa and Neisseria meningitidis: novel antimicrobial targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3804-13 (2007)
University of Maryland
Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 26316-25 (2007)
University of Bern
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3765-76 (2007)
National Institute On Drug Abuse
Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6208-26 (2007)
Wyeth Research
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 5239-44 (2007)
Korea Research Institute of Chemical Technology
Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4729-32 (2007)
Chiba University
Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 657-61 (2008)
Università
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 27781-91 (2007)
Pfizer
Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 26284-93 (2007)
Niddk
Synthesis and antiviral evaluation of 6-(alkyl-heteroaryl)furo[2,3-d]pyrimidin-2(3H)-one nucleosides and analogues with ethynyl, ethenyl, and ethyl spacers at C6 of the furopyrimidine core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3897-905 (2007)
Brigham Young University
Novel antagonists of the thioesterase domain of human fatty acid synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Cancer Ther 6: 2120-6 (2007)
Burnham Institute For Medical Research
In vitro suppression of K65R reverse transcriptase-mediated tenofovir- and adefovir-5'-diphosphate resistance conferred by the boranophosphonate derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3162-7 (2007)
Afmb-Cnrs-Esil
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3147-54 (2007)
Glaxosmithkline
Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5787-810 (2007)
Uppsala University
Synthesis, biological evaluation, and molecular modeling of 3,5-substituted-N1-phenyl-N4,N4-di-n-butylsulfanilamides as antikinetoplastid antimicrotubule agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6071-9 (2007)
The Ohio State University
Mycophenolic acid as a latent agonist of PPARgamma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4767-70 (2007)
Hokkaido University
Pyridinylimidazole inhibitors of Tie2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4756-60 (2007)
Glaxosmithkline
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4812-8 (2007)
Mahidol University
Bioactive peroxides as potential therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 223-51 (2008)
The Hebrew University of Jerusalem
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 72: 876-84 (2007)
Nih
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 27126-32 (2007)
University of WÜRzburg
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4799-803 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4737-45 (2007)
Glaxosmithkline
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4795-8 (2007)
Merck Research Laboratories
Orally bioavailable potent soluble epoxide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3825-40 (2007)
University of California Davis
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3786-94 (2007)
Jerini
Hydroxyethylene isosteres of selective neuronal nitric oxide synthase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6096-108 (2007)
Northwestern University
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4824-8 (2007)
Eli Lilly
A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5775-86 (2007)
Hacettepe University
4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4861-5 (2007)
Johnson and Johnson Pharmaceutical Research and Development
Prenylated xanthones from the root bark of Cudrania tricuspidata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1207-9 (2007)
Chungbuk National University
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3416-9 (2007)
TBA
Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3954-63 (2007)
Johnson & Johnson Pharmaceutical
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3427-30 (2007)
TBA
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 11927-32 (2007)
The Scripps Research Institute
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 6170-81 (2007)
Wyeth Research
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4947-54 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4432-6 (2007)
Bristol-Myers Squibb Research and Development
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4746-52 (2007)
Altana Pharma
2D Quantitative structure-activity relationship studies on a series of cholesteryl ester transfer protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6242-52 (2007)
Universidade Federal Da Bahia
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6109-18 (2007)
University of Vienna
alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4841-4 (2007)
Menarini Ricerche
Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5819-27 (2007)
Aristotle University of Thessaloniki
Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4878-81 (2007)
Università
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4845-50 (2007)
Schering-Plough Research Institute
Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4855-60 (2007)
Virginia Commonwealth University
QSAR study of heparanase inhibitors activity using artificial neural networks and Levenberg-Marquardt algorithm.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 548-56 (2008)
Sharif University of Technology
3D-QSAR and docking studies of aminopyridine carboxamide inhibitors of c-Jun N-terminal kinase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 604-13 (2008)
Chinese Academy of Sciences
Synthesis and adenosine receptor binding studies of some novel triazolothienopyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 614-20 (2008)
University College of Pharmaceutical Sciences
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3686-95 (2007)
Research Triangle Institute
Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3585-95 (2007)
University Paris Descartes
Rational optimization of the binding affinity of CD4 targeting peptidomimetics with potential anti HIV activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3482-8 (2007)
University of Hamburg
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3561-72 (2007)
Radiopharmaceuticals Research Institute
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 5837-44 (2007)
Astellas Pharma
Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4829-31 (2007)
University of Maryland
Indanylacetic acids as PPAR-delta activator insulin sensitizers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4369-73 (2007)
Bayer Research Center
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4837-40 (2007)
Biovitrum
Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4982-6 (2007)
Meiji Seika Kaisha
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4363-8 (2007)
Gsk
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 27354-65 (2007)
University of Copenhagen
Design, synthesis, and discovery of stilbene derivatives based on lithospermic acid B as potent protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4481-6 (2007)
Yonsei University
Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin mimic demethylasterriquinone B1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3423-6 (2007)
TBA
Interactions of ceftobiprole with beta-lactamases from molecular classes A to D.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 3089-95 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3465-81 (2007)
National Cancer Institute-Frederick
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3442-56 (2007)
Pfizer
Modification of eukaryotic initiation factor 5A from Plasmodium vivax by a truncated deoxyhypusine synthase from Plasmodium falciparum: An enzyme with dual enzymatic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6200-7 (2007)
Institute For Medical Parasitology
Structure-based design of alpha-amido aldehyde containing gluten peptide analogues as modulators of HLA-DQ2 and transglutaminase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6253-61 (2007)
Stanford University
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4415-8 (2007)
Pfizer
The identification of potent, selective, and bioavailable cathepsin S inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4929-33 (2007)
Merck Frosst Centre For Therapeutic Research
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 316: 1759-1761 (2007)
Anacor Pharmaceuticals
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 317: 516-9 (2007)
Harvard Medical School
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4873-7 (2007)
Universidad De Santiago De Compostela
Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4961-6 (2007)
Institute of Research
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4630-4 (2007)
Merck Research Laboratories
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4419-27 (2007)
Bristol-Myers Squibb
Agonist lead identification for the high affinity niacin receptor GPR109a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4914-9 (2007)
Arena Pharmaceuticals
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4895-900 (2007)
The University of Tokyo
New chemical tools for investigating human mitotic kinesin Eg5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 6474-88 (2007)
Cnrs-Université
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4901-5 (2007)
Argenta Discovery
Gypsophin: a novel alpha-glucosidase inhibitory cyclic peptide from the roots of Gypsophila oldhamiana.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4460-3 (2007)
China Pharmaceutical University
Interaction of O-(undec-10-en)-yl-D-glucose derivatives with the Plasmodium falciparum hexose transporter (PfHT).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4934-7 (2007)
Université
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4442-6 (2007)
Tanabe Research Laboratories Usa
Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4382-6 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3751-5 (2007)
Washington University
From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3706-15 (2007)
Università
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3730-42 (2007)
Bristol-Myers Squibb
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3420-2 (2007)
TBA
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3528-39 (2007)
Amgen
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3515-27 (2007)
Amgen
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3497-514 (2007)
Amgen
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3627-44 (2007)
Abbott Laboratories
Synthesis of unnatural flavonoids and stilbenes by exploiting the plant biosynthetic pathway in Escherichia coli.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 613-21 (2007)
University of Tokyo
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1118-21 (2007)
Griffith University
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1093-7 (2007)
Korean Research Institute of Biosciences and Biotechnology
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4374-7 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4437-41 (2007)
Boehringer Ingelheim (Canada)
Aminopyrrolidineamide inhibitors of site-1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4411-4 (2007)
Pfizer
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3651-60 (2007)
Abbott Laboratories
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3431-3 (2007)
TBA
Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3434-41 (2007)
Università
Synthesis and biological activities of isogranulatimide analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5965-80 (2007)
Université
Design, synthesis, and molecular modeling studies of 5'-deoxy-5'-ureidoadenosine: 5'-ureido group as multiple hydrogen bonding donor in the active site of S-adenosylhomocysteine hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4456-9 (2007)
Ewha Womans University
Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 315-26 (2008)
University of Antwerp
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 513-39 (2008)
Monash University (Parkville Campus)
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 69: 444-50 (2007)
Pfizer
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3596-603 (2007)
The University of Iowa
Dual aromatase-steroid sulfatase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3540-60 (2007)
University of Bath
Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3661-6 (2007)
Institute For Natural Products Research and Infection Biology
Multistructure 3D-QSAR studies on a series of conformationally constrained butyrophenones docked into a new homology model of the 5-HT2A receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3242-55 (2007)
Universitat Pompeu Fabra
Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3314-21 (2007)
Purdue University
SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3222-8 (2007)
Kyoto University
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3194-204 (2007)
Washington University
Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5811-8 (2007)
Cairo University
Benzo[b]thiophene-based histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4562-7 (2007)
Merck Research Laboratories
The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4664-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4678-82 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and matrix metalloproteinase (MMP)-12 inhibitory activity of ageladine A and its analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4495-9 (2007)
Kyorin Pharmaceutical
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4509-13 (2007)
Schering-Plough Research Institute
Inhibitors of anthrax lethal factor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4575-8 (2007)
Purdue University
Aza analogues of equol: novel ligands for estrogen receptor beta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5828-36 (2007)
Chinese Academy of Sciences
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 5912-49 (2007)
Pfizer
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4464-70 (2007)
Institut Henri Beaufour
SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4378-81 (2007)
Bayer Research Center
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4557-61 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4613-8 (2007)
National Institute of Pharmaceutical Education and Research
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4487-90 (2007)
Bristol-Myers Squibb Research and Development
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4538-44 (2007)
Pfizer
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4531-7 (2007)
Pfizer
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4450-5 (2007)
Glaxosmithkline
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 166-73 (2008)
Sun Yat-Sen University
Enzymatic therapeutic index of acyclovir. Viral versus human polymerase gamma specificity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 25159-67 (2007)
The University of Texas
Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 24504-13 (2007)
Emmy Noether Research Group
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5369-85 (2007)
Schering-Plough Research Institute
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4248-53 (2007)
Mcgill University/Royal Victoria Hospital
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3256-66 (2007)
National Institute of Mental Health
Enaminone amides as novel orally active GABAA receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3369-79 (2007)
University of California Irvine
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4657-63 (2007)
Pfizer
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3880-5 (2007)
Vernalis (R&D)
A novel arginine methyltransferase inhibitor with cellular activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4150-3 (2007)
Albert-Ludwigs-University of Freiburg
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3283-9 (2007)
Southern Research Institute
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3388-91 (2007)
Research Triangle Institute
RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nature 447: 864-868 (2007)
Columbia University
Exploitation of structural and regulatory diversity in glutamate racemases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nature 447: 817-822 (2007)
Astrazeneca Global Structural Chemistry
X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 25436-44 (2007)
Jacobus Pharmaceutical
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3267-73 (2007)
Nci-Fcrdc
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4568-74 (2007)
Pfizer
Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4527-30 (2007)
Southern Research Institute
Reversine increases the plasticity of lineage-committed mammalian cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 10482-7 (2007)
The Scripps Research Institute
P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3229-41 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
2-tert-butyl-8-quinolinamines exhibit potent blood schizontocidal antimalarial activity via inhibition of heme crystallization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2842-7 (2007)
Kyoto Institute of Technology
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 24463-70 (2007)
Stony Brook University
Synthesis and biological evaluation of cyclic and branched peptide analogues as ligands for cholecystokinin type 1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5845-53 (2007)
Istituto Di Biostrutture E Bioimmagini-Cnr
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5519-28 (2007)
Gilead Sciences
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4579-83 (2007)
Merck Research Laboratories
N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4599-603 (2007)
Pfizer
A chemometric study of the 5-HT(1A) receptor affinities presented by arylpiperazine compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 364-72 (2008)
Universidade De S£O Paulo
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5406-16 (2007)
Universit£
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5590-603 (2007)
Neurocrine Biosciences
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 5576-89 (2007)
Pfizer
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4670-7 (2007)
Glaxosmithkline
Design of a partial PPARdelta agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4625-9 (2007)
Novo Nordisk
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5440-7 (2007)
Santaris Pharma
Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca)).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5457-79 (2007)
University College London
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4242-7 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis of 4-phenoxybenzamide adenine dinucleotide as NAD analogue with inhibitory activity against enoyl-ACP reductase (InhA) of Mycobacterium tuberculosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4588-91 (2007)
University of Minnesota
Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4118-22 (2007)
University of Illinois
Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4646-9 (2007)
Pharmacia
New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3397-401 (2007)
Vrije Universiteit Brussel
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3359-68 (2007)
The Scripps Research Institute
NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proteins 69: 97-111 (2007)
India Central Drug Research Institute
Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 22619-28 (2007)
Vertex Pharmaceuticals
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 23231-9 (2007)
Novartis
Design of novel histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4619-24 (2007)
Merck Research Laboratories
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4683-8 (2007)
Daiichi Pharmaceutical
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3159-62 (2007)
Ewha Womans University
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3274-82 (2007)
Purdue University
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3392-6 (2007)
University of Minnesota
Structural variation governs substrate specificity for organic anion transporter (OAT) homologs. Potential remote sensing by OAT family members.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 23841-53 (2007)
University of California
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4271-4 (2007)
Sungkyunkwan University
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4144-9 (2007)
Re&D Vufb
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4158-62 (2007)
Ligand Pharmaceuticals
Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4689-93 (2007)
Kowa
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3163-6 (2007)
University of Michigan
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3015-3025 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3046-3053 (2007)
Duquesne University
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3143-7 (2007)
Ewha Womans University
Bidirectional, iterative approach to the structural delineation of the functional"chemoprint" in GPR40 for agonist recognition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2981-9 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5563-75 (2007)
Dipartimento Di Scienze Farmaceutiche
Extension of Drosophila melanogaster life span with a GPCR peptide inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 415-9 (2007)
California Institute of Technology
Activation of inhibitors by sortase triggers irreversible modification of the active site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 23129-39 (2007)
University of Chicago
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4167-72 (2007)
Lg Life Sciences
Synthesis and biological evaluation of 9-deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid as multi-substrate analogue inhibitors of PNP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4173-7 (2007)
Tokyo University of Pharmacy and Life Sciences
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5166-76 (2007)
Neurocrine Biosciences
Synthesis, 3D-QSAR, and docking studies of 1-phenyl-1H-1,2,3-triazoles as selective antagonists for beta3 over alpha1beta2gamma2 GABA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5090-104 (2007)
Shimane University
Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5047-60 (2007)
University of Maryland
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3819-25 (2007)
Berlex Biosciences
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4308-15 (2007)
Abbott Laboratories
Primary amides as selective inhibitors of cathepsin K.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4328-32 (2007)
Merck Frosst Centre For Therapeutic Research
5-Arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5137-49 (2007)
Universit£
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4131-4 (2007)
Karo Bio
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4128-30 (2007)
Harvard Medical School
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 4284-9 (2007)
Bristol-Myers Squibb
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4191-5 (2007)
Polaris Pharmaceuticals
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 69: 331-7 (2007)
Chemdiv
Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 69: 298-313 (2007)
University of Maryland
Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3054-61 (2007)
University of Illinois At Chicago
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 3138-3142 (2007)
Universita Degli Studi
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3062-9 (2007)
Institut D'Investigacions BiomèDiques August Pi I
Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 10619-24 (2007)
Pfizer
Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 20847-53 (2007)
Institute For Medical Research
Isolation of glycosidase-inhibiting hyacinthacines and related alkaloids from Scilla socialis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 993-7 (2007)
University of Toyama
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3101-12 (2007)
James Black Foundation
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2967-80 (2007)
Berlex Biosciences
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2931-41 (2007)
Pfizer
Small-molecule activators of RNase L with broad-spectrum antiviral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 9585-90 (2007)
Lerner Research Institute
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 10022-7 (2007)
Institute of Biological Chemistry
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 20836-46 (2007)
Merck Research Laboratories
Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4187-90 (2007)
Tranzyme Pharma
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4290-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3916-20 (2007)
Glaxosmithkline
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5177-90 (2007)
University of Tokyo
Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4228-31 (2007)
Ucb Pharma
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4297-302 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4208-12 (2007)
Nagoya City University
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 456-63 (2008)
University of Alexandria
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4303-7 (2007)
Abbott Laboratories
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4232-41 (2007)
Astrazeneca R&D MöLndal
C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3835-9 (2007)
Roche Research Center
Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 189-203 (2008)
Università
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4323-7 (2007)
Emd-Serono Research Institute
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3814-8 (2007)
Berlex Biosciences
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4333-7 (2007)
Wyeth Research
Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4338-42 (2007)
Yale University
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4347-50 (2007)
Novartis Institutes of Biomedical Research
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3925-9 (2007)
Shionogi
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 3086-100 (2007)
Abbott Laboratories
Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2726-32 (2007)
University of Copenhagen
Alternative chemical modifications reverse the binding orientation of a pharmacophore scaffold in the active site of macrophage migration inhibitory factor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 23089-95 (2007)
Yale University
Alkyl-CoA disulfides as inhibitors and mechanistic probes for FabH enzymes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 513-24 (2007)
Portland State University
Structure-activity relationships of semisynthetic mumbaistatin analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5207-18 (2007)
Stanford University
QSAR study of selective ligands for the thyroid hormone receptor beta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5251-61 (2007)
University of Insubria
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4351-7 (2007)
Nagoya City University
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3864-7 (2007)
Glaxosmithkline
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3921-4 (2007)
University of Shizuoka
Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3855-9 (2007)
Johnson and Johnson Pharmaceutical Research and Development
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2990-3003 (2007)
Abbott Laboratories
The biology and chemistry of hyperlipidemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4674-99 (2007)
Sinhgad College of Pharmacy
Human and rat monoamine oxidase-A are differentially inhibited by (S)-4-alkylthioamphetamine derivatives: insights from molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5198-206 (2007)
University of Santiago De Chile
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3845-50 (2007)
Neurocrine Biosciences
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4030-4 (2007)
Shionogi
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2875-85 (2007)
The National Hellenic Research Foundation
The inhibitory effect of some new synthesized xanthates on mushroom tyrosinase activities.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzyme Inhib Med Chem 22: 239-46 (2007)
University of Tehran
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2911-9 (2007)
Mcgill University
7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5239-50 (2007)
Jagiellonian University Medical College
Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4876-90 (2007)
Universitat De Barcelona
QSAR studies and pharmacophore identification for arylsubstituted cycloalkenecarboxylic acid methyl esters with affinity for the human dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5262-74 (2007)
University of Aarhus
Synthesis and evaluation of homo-bivalent GnRHR ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4841-56 (2007)
Leiden University
Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5316-21 (2007)
Università
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3930-4 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3769-73 (2007)
Zhengzhou University
Inhibitory effect of 2-arylbenzofurans from Erythrina addisoniae on protein tyrosine phosphatase-1B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3868-71 (2007)
Korea Research Institute of Bioscience and Biotechnology
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2779-86 (2007)
University of Arizona Tucson
Crystal structures of Saccharomyces cerevisiae N-myristoyltransferase with bound myristoyl-CoA and inhibitors reveal the functional roles of the N-terminal region.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 22185-94 (2007)
Chinese Academy of Sciences
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3939-42 (2007)
University of Michigan
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3978-82 (2007)
Pharmaceutical Research Institute
Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3793-7 (2007)
University of Minnesota
Quantitative structure activity relationship studies on thiourea analogues as influenza virus neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 293-9 (2008)
National Institute of Pharmaceutical Education and Research (NIPER)
Structure-based discovery of a new class of Bcl-xL antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 35: 344-53 (2007)
Burnham Institute For Medical Research
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4753-66 (2007)
Université
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3860-3 (2007)
Johnson & Johnson Pharmaceutical Research & Development
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3988-91 (2007)
Novartis Institutes For Biomedical Research
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3630-5 (2007)
Pfizer
Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3886-93 (2007)
Universit£
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2799-806 (2007)
Purdue University
O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4767-74 (2007)
National Cancer Institute At Frederick
New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3943-6 (2007)
Université
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3595-8 (2007)
Seoul National University
Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3652-6 (2007)
Adolor
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3983-7 (2007)
Novartis Institutes For Biomedical Research
Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3969-71 (2007)
Merck Research Laboratories
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3894-9 (2007)
Abbott Laboratories
Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2903-15 (2007)
Medical University of Lublin
Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2818-41 (2007)
Cardiome Pharma
Fawcettimine-related alkaloids from Lycopodium serratum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1024-8 (2007)
Chiba University
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2445-53 (2007)
Achillion Pharmaceuticals
Pyrophosphorolytic excision of nonobligate chain terminators by hepatitis C virus NS5B polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2920-8 (2007)
Mcgill University
Discovery of structurally diverse HIV-1 integrase inhibitors based on a chalcone pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4985-5002 (2007)
University of Southern California
Inhibition of IGF-1R and lipoxygenase by nordihydroguaiaretic acid (NDGA) analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4026-9 (2007)
San Francisco State University
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3972-7 (2007)
Gsk
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3910-5 (2007)
Bristol-Myers Squibb
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3877-9 (2007)
Merck Research Laboratories
Radioiodinated aza-diphenylacetylenes as potential SPECT imaging agents for beta-amyloid plaque detection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3581-4 (2007)
University of Pennsylvania
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4006-11 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3511-5 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of pyrrolo[3,4-a]carbazole-1,3-diones, pyrrolo[3,4-c]carbazole-1,3-diones, and 2-aminopyridazino[3,4-a]pyrrolo[3,4-c]carbazole-1,3,4,7-tetraone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 282-92 (2008)
Université
Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2807-17 (2007)
Johnson & Johnson Pharmaceutical
Synthesis and in vitro antiplatelet activity of new 4-(1-piperazinyl)coumarin derivatives. Human platelet phosphodiesterase 3 inhibitory properties of the two most effective compounds described and molecular modeling study on their interactions with phosphodiesterase 3A catalytic site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2886-95 (2007)
Universit£
Novel heterocyclic thyromimetics. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3992-6 (2007)
Bayer Healthcare
N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 5003-17 (2007)
Jagiellonian University
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4035-9 (2007)
Forschungszentrum Dresden-Rossendorf
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3660-5 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3962-8 (2007)
Università
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3562-9 (2007)
Kalypsys
A new class of histamine H3 receptor antagonists derived from ligand based design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3670-5 (2007)
F. Hoffmann-La Roche
The discovery of long acting beta2-adrenoreceptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4012-5 (2007)
Pfizer
Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3624-9 (2007)
Pfizer
Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3957-61 (2007)
University of Tokyo
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3997-4000 (2007)
Merck Research Laboratories
Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2787-98 (2007)
University of California San Francisco
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2753-66 (2007)
Kobe Gakuin University
Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1010-5 (2007)
Department of Chemistry and Applied Biosciences
Diarylquinolines target subunit c of mycobacterial ATP synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 323-4 (2007)
Tibotec
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 19716-27 (2007)
University of California
Structures of Mycobacterium tuberculosis 1-deoxy-D-xylulose-5-phosphate reductoisomerase provide new insights into catalysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 19905-16 (2007)
Uppsala University
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4434-43 (2007)
University of Ferrara
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4396-405 (2007)
Wyeth Research
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3618-23 (2007)
Abbott Laboratories
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3647-51 (2007)
Schering-Plough Research Institute
Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5alpha-reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3603-7 (2007)
University of Canterbury
Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3491-6 (2007)
Johnson and Johnson Pharmaceutical Research and Development
Isoprenylated flavonoids from the stem bark of Erythrina abyssinica.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 1039-42 (2007)
Korea Research Institute of Bioscience and Biotechnology
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2682-92 (2007)
University of Illinois At Chicago
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2718-31 (2007)
Georgia Institute of Technology
An adamantyl-substituted retinoid-derived molecule that inhibits cancer cell growth and angiogenesis by inducing apoptosis and binds to small heterodimer partner nuclear receptor: effects of modifying its carboxylate group on apoptosis, proliferation, and protein-tyrosine phosphatase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2622-39 (2007)
Burnham Institute For Medical Research
Kv7 (KCNQ) channel modulators and neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2576-82 (2007)
Neurosearch
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2563-8 (2007)
Eli Lilly
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2589-96 (2007)
Glaxosmithkline
Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 8316-21 (2007)
Hebrew University of Jerusalem
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2747-51 (2007)
Chinese Academy of Sciences
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2767-78 (2007)
Biogen Idec
Mass spectrometry-based systems approach for identification of inhibitors of Plasmodium falciparum fatty acid synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2552-8 (2007)
Institute of Science
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2403-11 (2007)
University of California
RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3497-503 (2007)
Johnson and Johnson Pharmaceutical Research and Development
3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3504-7 (2007)
Roche Pharmaceuticals
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3570-4 (2007)
Eli Lilly
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 8520-5 (2007)
Abbott Laboratories
3D-QSAR studies on malonyl coenzyme A decarboxylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4470-81 (2007)
St. John'S University
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4044-8 (2007)
Abbott Laboratories
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4057-61 (2007)
Merck Research Laboratories
ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 4053-6 (2007)
Wyeth Research
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 73-80 (2008)
Central Drug Research Institute
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3575-80 (2007)
Pfizer
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3544-9 (2007)
Eli Lilly
3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3636-41 (2007)
Merck Research Laboratories
Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3608-12 (2007)
Merck
Brucella suis histidinol dehydrogenase: synthesis and inhibition studies of a series of substituted benzylic ketones derived from histidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4427-33 (2007)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Synthesis and biological activity of new melatonin dimeric derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4643-50 (2007)
Università
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3266-70 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3550-7 (2007)
Chemical Diversity
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 795-801 (2007)
Chiang Mai University
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2647-54 (2007)
Pfizer
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2700-7 (2007)
University of Liverpool
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2737-41 (2007)
Kribb
Discovery of a rhodanine class of compounds as inhibitors of Plasmodium falciparum enoyl-acyl carrier protein reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2665-75 (2007)
Institute of Science
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2597-600 (2007)
Glaxosmithkline
Carbonic anhydrases as targets for medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4336-50 (2007)
Universit£
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3558-61 (2007)
Merck Research Laboratories
2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3696-701 (2007)
Universit£
Plant P5C reductase as a new target for aminomethylenebisphosphonates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Agric Food Chem 55: 4340-7 (2007)
University of Ferrara
Isoform-selective inhibition of the human UDP-glucuronosyltransferase 2B7 by isolongifolol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2655-64 (2007)
University of Helsinki
Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2605-8 (2007)
Mcgill University Health Center/Royal Victoria Hospital
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 8059-64 (2007)
University of California
Binding of ceftobiprole and comparators to the penicillin-binding proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2621-4 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2600-4 (2007)
Kagoshima University
Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4618-28 (2007)
Imperial College
Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2693-9 (2007)
University of California Berkeley
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2732-6 (2007)
Almirall
2D QSAR studies on thyroid hormone receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4609-17 (2007)
Universidade De S£O Paulo
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3354-61 (2007)
Merck Research Laboratories
Discovery of new C3aR ligands. Part 1: arginine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3258-61 (2007)
Ucb Pharma
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3736-40 (2007)
Ajinomoto
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3760-4 (2007)
Schering-Plough Research Institute
Crystal structures of multidrug binding protein TtgR in complex with antibiotics and plant antimicrobials.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 369: 829-40 (2007)
Imperial College
A fragment-based approach for the discovery of isoform-specific p38alpha inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 2: 329-36 (2007)
Burnham Institute For Medical Research
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 104: 7391-6 (2007)
University of Central Florida College of Medicine
Docking-based 3D-QSAR study for selectivity of DPP4, DPP8, and DPP9 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3716-21 (2007)
Korea Research Institute of Chemical Technology
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3322-9 (2007)
Curacyte Discovery
Benzopyran sulfonamides as KV1.5 potassium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3271-5 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2609-11 (2007)
Merck Research Laboratories
Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2640-6 (2007)
Johann Wolfgang Goethe-UniversitäT
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 7444-8 (2007)
The Scripps Research Institute
7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4543-51 (2007)
University College London
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3778-83 (2007)
Schering-Plough Research Institute
Novel inhibitors of fatty acid amide hydrolase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3287-91 (2007)
Bristol-Myers Squibb
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3463-7 (2007)
Ucb Pharma
Discovery of new C3aR ligands. Part 2: amino-piperidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3262-5 (2007)
Ucb Pharma
Classification of estrogen receptor-beta ligands on the basis of their binding affinities using support vector machine and linear discriminant analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 43-52 (2008)
Yantai University
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2391-8 (2007)
Tufts University School of Medicine
De Novo Parallel Design, Synthesis and Evaluation of Inhibitors against the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 and Drug-Resi![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2370-84 (2007)
Bar-Ilan University
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2408-14 (2007)
University of Copenhagen
Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2520-6 (2007)
Merck Research Laboratories
Nicotinic acid receptor agonists differentially activate downstream effectors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 18028-36 (2007)
Arena Pharmaceuticals
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3292-7 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Exploring molecular shape analysis of styrylquinoline derivatives as HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 81-92 (2008)
Jadavpur University
Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 62-72 (2008)
Sapienza University of Rome
Assessing potency of c-Jun N-terminal kinase 3 (JNK3) inhibitors using 2D molecular descriptors and binary QSAR methodology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4256-64 (2007)
Aureus Pharma
Synthesis and glycogen phosphorylase inhibitor activity of 2,3-dihydrobenzo[1,4]dioxin derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4048-56 (2007)
University of Debrecen
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3765-8 (2007)
Sun Yat-Sen University
Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 872-5 (2007)
Griffith University
Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2289-92 (2007)
Astex
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2293-2296 (2007)
Astex
Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3729-32 (2007)
Harvard Medical School
Squalene-derived flexible linkers for bioactive peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3310-3 (2007)
University of Arizona
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3754-9 (2007)
Cerep
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3339-43 (2007)
Amgen
Bridged androstenediol analogs as ER-beta selective SERMs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2944-8 (2007)
Merck Research Laboratories
Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1084-94 (2007)
Zentiva Vufb
1-Aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones: a new class of antiproliferative agents with selectivity for human leukemia and breast cancer cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1317-24 (2007)
Technische UniversitÄT Braunschweig
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2415-23 (2007)
University of Pennsylvania
Small molecule designed to target metal binding site in the alpha2I domain inhibits integrin function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2742-6 (2007)
University of Turku
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2497-505 (2007)
Universidade De Vigo
Enhanced substituted resorcinol hydrophobicity augments tyrosinase inhibition potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2676-81 (2007)
Migal - Galilee Technology Center
A high-throughput screen for aggregation-based inhibition in a large compound library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2385-90 (2007)
University of California San Francisco
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2341-51 (2007)
Pfizer
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4159-74 (2007)
University of Aarhus
Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3458-62 (2007)
Katholieke Universiteit Leuven
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3367-72 (2007)
Tanabe Research Laboratories
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2987-91 (2007)
National Institute On Drug Abuse
Synthesis and biological evaluation of 2beta,3alpha-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3044-7 (2007)
Emory University
Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2285-8 (2007)
TBA
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2310-8 (2007)
Schering-Plough Research Institute
Benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides as inhibitors of carbonic anhydrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3335-8 (2007)
Institute of Biotechnology
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3421-5 (2007)
Biovitrum
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 69: 204-11 (2007)
Shanghai Jiao Tong University
Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 69: 170-9 (2007)
Queen'S University of Belfast
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2297-300 (2007)
Takeda Pharmaceutical
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2486-96 (2007)
Ligand Pharmaceuticals
Sensitivity of monkey B virus (Cercopithecine herpesvirus 1) to antiviral drugs: role of thymidine kinase in antiviral activities of substrate analogs and acyclonucleosides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2028-34 (2007)
Glsynthesis
Biochemical characterization of PER-2 and genetic environment of blaPER-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2359-65 (2007)
Universidad De Buenos Aires
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 16379-90 (2007)
Vanderbilt Institute For Chemical Biology
Synthesis and evaluation of amino-threoses in D- and L-series: are five membered ring amino-sugars more potent glycosidase inhibitors than the six membered ones?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4125-35 (2007)
Universit£
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3435-9 (2007)
Daiichi Asubio Pharma
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3378-83 (2007)
Pfizer
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3388-91 (2007)
Abbott Laboratories
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3373-7 (2007)
Merck Research Laboratories
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3344-8 (2007)
Eli Lilly
Caffeoylglycolic and caffeoylamino acid derivatives, halfmers of L-chicoric acid, as new HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1309-15 (2007)
Korea Institute of Science & Technology
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3349-53 (2007)
Pfizer
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4136-43 (2007)
Technische UniversitäT MüNchen
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 4077-84 (2007)
Astrazeneca
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4106-12 (2007)
Harvard Medical School
Novel 3-galloylamido-N'-substituted-2,6-piperidinedione-N-acetamide peptidomimetics as metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2935-8 (2007)
Shandong University
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3384-7 (2007)
Merck Research Laboratories
Synthesis and biological activity of imidazopyridine anticoccidial agents: part I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1334-57 (2007)
Scynexis
Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2399-407 (2007)
Purdue University
Target-based approach to inhibitors of histone arginine methyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2319-25 (2007)
Albert-Ludwigs-University of Freiburg
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 6846-51 (2007)
Pharmaceutical Research Institute
chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 17837-44 (2007)
The University of Queensland
Inhibitory effect of obovatal on the migration and invasion of HT1080 cells via the inhibition of MMP-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4085-90 (2007)
Korea Research Institute of Bioscience and Biotechnology
Synthesis of andrographolide derivatives: a new family of alpha-glucosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4247-55 (2007)
Zhengzhou University
Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3480-5 (2007)
Université
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3023-7 (2007)
Schering-Plough Research Institute
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3006-9 (2007)
Merck
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2225-39 (2007)
P. Angeletti S.P.A. (Merck Research Laboratories)
Glyoxylate and pyruvate are antagonistic effectors of the Escherichia coli IclR transcriptional regulator.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 16476-91 (2007)
University of Toronto
Novel selective neuropeptide Y2 receptor PEGylated peptide agonists reduce food intake and body weight in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2264-8 (2007)
Bayer Pharmaceuticals
Virtual screening for novel openers of pancreatic K(ATP) channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2117-26 (2007)
University of Perugia
Structure-based design and synthesis of N(omega)-nitro-L-arginine-containing peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. Displacement of the heme structural water.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2089-99 (2007)
Northwestern University
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2011-29 (2007)
Abbott Laboratories
Serum differentially alters the antifungal properties of echinocandin drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2253-6 (2007)
Public Health Research Institute
Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4152-8 (2007)
Istituto Di Biostrutture E Bioimmagini-Cnr
Calculation of binding energy using BLYP/MM for the HIV-1 integrase complexed with the S-1360 and two analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3818-24 (2007)
Universidade Federal Do Par£
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3028-33 (2007)
Schering-Plough Research Institute
Selective and dual action orally active inhibitors of thrombin and factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2927-30 (2007)
Glaxosmithkline
Synthesis of bridged piperazines with sigma receptor affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1247-62 (2007)
Institut F£R Pharmazeutische Und Medizinische Chemie
Design and synthesis of a potent histone deacetylase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2003-6 (2007)
Virginia Tech
Novel aminoethylbiphenyls as 5-HT7 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3018-22 (2007)
Université
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3431-4 (2007)
Daiichi Asubio Pharma
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2998-3002 (2007)
Alcon Research
QSAR study on a novel series of 8-azaadenine analogues proposed as A1 adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 43: 114-21 (2008)
University of Pisa
Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3010-3 (2007)
Pharmacopeia Drug Discovery
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2992-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Ligand based virtual screening and biological evaluation of inhibitors of chorismate mutase (Rv1885c) from Mycobacterium tuberculosis H37Rv.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3053-8 (2007)
Central Drug Research Institute
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2966-70 (2007)
F. Hoffmann-La Roche
Evidence for a novel binding site conformer of aldose reductase in ligand-bound state.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 369: 186-97 (2007)
University of Marburg
A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2127-36 (2007)
National Cancer Institute At Frederick
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 4175-92 (2007)
Astellas Pharma
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3635-48 (2007)
Wyeth Research
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3473-9 (2007)
Tanabe Research Laboratories Usa
Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2921-6 (2007)
China Pharmaceutical University
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3130-5 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2157-65 (2007)
University of Pennsylvania
Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2060-6 (2007)
Eberhard-Karls-University T£Bingen
Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 3146-51 (2007)
Merck Frosst Centre For Therapeutic Research
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2200-12 (2007)
Amgen
Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3896-911 (2007)
University of Navarra
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3649-60 (2007)
Janssen-Cilag
PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2728-30 (2007)
Inha University
Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3117-21 (2007)
Wyeth Research
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2254-8 (2007)
Harvard Medical School
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2030-9 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
Mechanisms for picrotoxinin and picrotin blocks of alpha2 homomeric glycine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 16016-35 (2007)
Université
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2078-84 (2007)
Emory University
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 17314-24 (2007)
Consiglio Nazionale Delle Ricerche
Interaction between HIV-1 Rev and integrase proteins: a basis for the development of anti-HIV peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 15743-53 (2007)
The Hebrew University of Jerusalem
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2144-56 (2007)
University of Missouri-Columbia
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2067-77 (2007)
Salk Institute
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2269-72 (2007)
Bristol-Myers Squibb
Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3684-91 (2007)
Texas A&M University
Polyphenols based on isoflavones as inhibitors of Helicobacter pylori urease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3703-10 (2007)
Nanjing University
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3048-52 (2007)
Kyoto Pharmaceutical University
PDE-10A inhibitors as insulin secretagogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2869-73 (2007)
Bayer Pharmaceuticals
Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3113-6 (2007)
Pharmacia
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3854-68 (2007)
Université
Structure based de novo design of novel glycogen synthase kinase 3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3728-36 (2007)
Addis Ababa University
3-{2-[Bis-(4-fluorophenyl)methoxy]ethyl}-6-substituted-3,6-diazabicyclo[3.1.1]heptanes as novel potent dopamine uptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3748-55 (2007)
Universit£
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3783-800 (2007)
Pfizer
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3801-17 (2007)
St. Jude Children'S Research Hospital
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3072-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3081-6 (2007)
Pfizer
Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3077-80 (2007)
Ucb Pharma
Cellular characterization of a novel focal adhesion kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 14845-52 (2007)
University of Virginia
Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 15208-16 (2007)
University of Wisconsin
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3883-8 (2007)
Kyushu University
Small molecule antagonists of the CC chemokine receptor 4 (CCR4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3141-5 (2007)
Millennium Pharmaceuticals
4-substituted indazoles as new inhibitors of neuronal nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3177-80 (2007)
Upres-Ea 3915
Methylenebis(sulfonamide) linked nicotinamide adenine dinucleotide analogue as an inosine monophosphate dehydrogenase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3152-5 (2007)
University of Minnesota
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2697-702 (2007)
Merck Research Laboratories
Development of molecular probes for second-site screening and design of protein tyrosine phosphatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 2137-43 (2007)
Institute For Medical Research
Identification of novel fragment compounds targeted against the pY pocket of v-Src SH2 by computational and NMR screening and thermodynamic evaluation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proteins 67: 981-90 (2007)
University College London
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3368-72 (2007)
University of Chile
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 3321-33 (2007)
Wyeth Research
Discovery of a novel small molecule binding site of human survivin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3122-9 (2007)
Abbott Laboratories
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3099-104 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3136-40 (2007)
Abbott Laboratories
Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 6061-5 (2007)
University of Minnesota
Habbemines A and B, pyrrolidine alkaloids with human delta-opioid receptor binding affinity from the leaves of Elaeocarpus habbemensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 866-8 (2007)
Griffith University
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3390-412 (2007)
Pfizer
Phenolic hydrazones are potent inhibitors of macrophage migration inhibitory factor proinflammatory activity and survival improving agents in sepsis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1993-7 (2007)
The New York School of Medicine
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3208-11 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3109-12 (2007)
Pfizer
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2706-11 (2007)
Bayer Healthcare
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2899-903 (2007)
Gnf
Neuroprotective principles from Gastrodia elata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 571-4 (2007)
National Research Institute of Chinese Medicine
Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1850-64 (2007)
University of Alberta
Synthesis and SAR studies of a novel class of S1P1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3548-64 (2007)
Sankyo
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3450-6 (2007)
Institute of Biological Chemistry and The Genomics Research Center
Design of potent PPARalpha agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3198-202 (2007)
Novo Nordisk
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2465-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 3212-6 (2007)
Université
Fluorinated NSC as a Cdc25 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2351-4 (2007)
Sejong University
Covalent reactions of wortmannin under physiological conditions.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 321-8 (2007)
Massachusetts General Hospital
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 859-62 (2007)
Tahitian Noni International
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1876-85 (2007)
St. Jude Research Hospital
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1723-6 (2007)
University of Michigan
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1810-27 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3499-504 (2007)
Inha University
Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3524-38 (2007)
The Danish University of Pharmaceutical Sciences
Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2685-91 (2007)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2712-7 (2007)
Nippon Shinyaku
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2372-5 (2007)
Birla Institute of Technology and Science
ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Pharmacol 562: 1-11 (2007)
The Hebrew University of Jerusalem
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1988-92 (2007)
University of Copenhagen
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1939-57 (2007)
University of Montpellier
NMR screening applied to the fragment-based generation of inhibitors of creatine kinase exploiting a new interaction proximate to the ATP binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1865-75 (2007)
Universit£
Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3445-9 (2007)
Nippon Suisan Kaisha
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2213-24 (2007)
Astrazeneca
Inhibitory effect on soybean lipoxygenase and docking studies of some secondary metabolites, isolated from Origanum vulgare L. ssp. hirtum.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzyme Inhib Med Chem 22: 99-104 (2007)
University of Athens
The nucleoside analog sangivamycin induces apoptotic cell death in breast carcinoma MCF7/adriamycin-resistant cells via protein kinase Cdelta and JNK activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 15271-83 (2007)
Georgetown University Medical Center
Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 15799-811 (2007)
University of Copenhagen
Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2123-9 (2007)
Instituto De Parasitolog£A Y Biomedicina&Quot;L£Pez-Neyra
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Drug Metab Dispos 35: 929-36 (2007)
Targegen
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1978-82 (2007)
National Cancer Institute-Frederick
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1958-72 (2007)
Newcastle University
1-(1,3-Benzodioxol-5-ylmethyl)-3-[4-(1H-imidazol-1-yl)phenoxy]-piperidine analogs as potent and selective inhibitors of nitric oxide formation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2499-504 (2007)
Berlex Biosciences
Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2749-55 (2007)
Lucknow University
Structural and thermodynamic study on aldose reductase: nitro-substituted inhibitors with strong enthalpic binding contribution.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 368: 618-38 (2007)
University of Marburg
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2828-33 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2760-4 (2007)
Inha University
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2769-74 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2355-60 (2007)
The Scripps Research Institute
Development of integrase inhibitors for treatment of AIDS: an overview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1159-68 (2007)
K.L.E.S. College of Pharmacy
Structure-based discovery of new small molecule inhibitors of low molecular weight protein tyrosine phosphatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1102-8 (2007)
Institute For Research In Biomedicine (Irb)
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1983-7 (2007)
Abbott Laboratories
Nodulisporol and Nodulisporone, novel specific inhibitors of human DNA polymerase lambda from a fungus, Nodulisporium sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3109-14 (2007)
Science University of Tokyo
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1727-30 (2007)
Johnson & Johnson Pharmaceutical Research and Development
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 3520-5 (2007)
Harvard Medical School
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 3456-9 (2007)
The Johns Hopkins University School of Medicine
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 4106-11 (2007)
Millennium Pharmaceuticals
Synthesis and evaluation of transthyretin amyloidosis inhibitors containing carborane pharmacophores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 4808-13 (2007)
University of California
Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1445-8 (2007)
Arena Pharmaceuticals
Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1711-5 (2007)
Uppsala University
SCO-1, a novel plasmid-mediated class A beta-lactamase with carbenicillinase characteristics from Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2185-8 (2007)
Institut Pasteur Hellenique
Probing the pharmacophore of ginkgolides as glycine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1610-7 (2007)
University of Copenhagen
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1514-27 (2007)
Abbott Laboratories
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1693-7 (2007)
Via Zambeletti 25
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1571-83 (2007)
Via Zambeletti 25
Self-organizing maps for identification of new inhibitors of P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1698-702 (2007)
University of Vienna
Fluorogenic probes for monitoring peptide binding to class II MHC proteins in living cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 222-8 (2007)
University of Massachusetts Medical School
The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 13395-401 (2007)
Stanford University
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2879-85 (2007)
Merck Research Laboratories
Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2849-53 (2007)
Icagen
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2171-8 (2007)
Neurocrine Biosciences
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2886-9 (2007)
Amgen
Synthesis of fluorescent-labeled aeruginosin derivatives for high-throughput fluorescence correlation spectroscopy assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2904-7 (2007)
Graduate School of Science and Engineering
Further studies of tyrosine surrogates in opioid receptor peptide ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2656-60 (2007)
Adolor
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 3235-40 (2007)
Hokkaido University
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3161-70 (2007)
Universit£
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2863-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2838-43 (2007)
University of Edinburgh
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2817-22 (2007)
Abbott Laboratories
Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2834-7 (2007)
University of Oslo
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2365-71 (2007)
Abbott Laboratories
3D-QSAR and molecular docking studies on benzothiazole derivatives as Candida albicans N-myristoyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 477-86 (2007)
Second Military Medical University
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cancer Cell 11: 217-27 (2007)
Harvard Medical School
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1558-70 (2007)
University Walk
Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1973-7 (2007)
Sapienza University of Rome
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2558-60 (2007)
Institute For Natural Product Research and Infection Biology
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2430-3 (2007)
China Pharmaceutical University
Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2874-8 (2007)
Ithaca College
Design, synthesis and melatoninergic activity of new unsubstituted and beta,beta'-difunctionalised 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-alkanamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1004-13 (2007)
University of Athens
Synthesis of valiolamine and some precursors for bioactive carbaglycosylamines from (-)-vibo-quercitol produced by biogenesis of myo-inositol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 493-7 (2007)
Keio University
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1651-7 (2007)
Griffith University
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1584-97 (2007)
Abbott Laboratories
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1495-503 (2007)
Novo Nordisk
Nonprenylated rotenoids, a new class of potent breast cancer resistance protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1933-8 (2007)
Umr 5086 Cnrs/Universit£
Structural and functional basis of cyclooxygenase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1425-41 (2007)
Institute For Chemical Biology and Center In Molecular Toxicology
Heme oxygenase inhibition by 2-oxy-substituted 1-(1H-imidazol-1-yl)-4-phenylbutanes: effect of halogen substitution in the phenyl ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3225-34 (2007)
Queen'S University
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3143-51 (2007)
University of Cagliari
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2438-42 (2007)
Astellas Pharma
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1546-57 (2007)
Gsk
Affinity-based ranking of ligands for DPP-4 from mixtures.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2404-7 (2007)
Merck Research Laboratories
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2376-9 (2007)
Novartis Institutes of Biomedical Research
Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2935-43 (2007)
Princeton University
The rational design of inhibitors of nitric oxide formation by inducible nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2505-8 (2007)
Berlex Biosciences
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1875-8 (2007)
Yale University
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2074-9 (2007)
National Institute On Drug Abuse
Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2414-20 (2007)
Chinese Academy of Sciences
Probing acid replacements of thiophene PTP1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2913-20 (2007)
Wyeth Research
Sulfonamide-related conformational effects and their importance in structure-based design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2931-4 (2007)
Glaxosmithkline
Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1627-34 (2007)
Università
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1449-57 (2007)
Università
Inhibition of secreted phospholipase A2. 4-glycerol derivatives of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one with broad activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1618-26 (2007)
Université
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 229-38 (2007)
University of California
Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2608-13 (2007)
Array Biopharma
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2622-8 (2007)
Korea Research Institute of Chemical Technology
Bisphosphonates as inhibitors of Trypanosoma cruzi hexokinase: kinetic and metabolic studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 12377-87 (2007)
Instituto Venezolano De Investigaciones Cient£Ficas
Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3054-64 (2007)
Universit£
N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2448-51 (2007)
University of Kuopio
Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2535-9 (2007)
Neurocrine Biosciences
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2161-5 (2007)
University of Arizona
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1335-46 (2007)
University of Hamburg
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1675-84 (2007)
Korea Research Institute of Bioscience and Biotechnology
Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1028-40 (2007)
University of Illinois
Novel sigma receptor ligands: synthesis and biological profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 951-61 (2007)
University of Catania
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1322-34 (2007)
University of Lille
Acquired echinocandin resistance in a Candida krusei isolate due to modification of glucan synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 1876-8 (2007)
Rutgers University
Morin (3,5,7,2',4'-pentahydroxyflavone) exhibits potent inhibitory actions on urate transport by the human urate anion transporter (hURAT1) expressed in human embryonic kidney cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Drug Metab Dispos 35: 981-6 (2007)
The Chinese University of Hong Kong
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 13033-46 (2007)
The Scripps Research Institute
Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 3065-81 (2007)
University of Ferrara
Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1241-53 (2007)
Sapienza University of Rome
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1213-21 (2007)
Eberhard-Karls-University TüBingen
Identification, synthesis, and biological evaluation of novel pyrazoles as low molecular weight luteinizing hormone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2080-5 (2007)
Merck Serono
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 993-1003 (2007)
Katholieke Universiteit Leuven
Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2907-19 (2007)
University of Montpellier
1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2883-91 (2007)
University of MüNster
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Agric Food Chem 55: 2276-81 (2007)
University of California
Calcitonin gene-related peptide analogues with aza and indolizidinone amino acid residues reveal conformational requirements for antagonist activity at the human calcitonin gene-related peptide 1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1401-8 (2007)
Université
High-throughput screening for human lysosomal beta-N-Acetyl hexosaminidase inhibitors acting as pharmacological chaperones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 14: 153-64 (2007)
Research Institute, Hospital For Sick Children
Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2892-7 (2007)
Umr 5063 Cnrs/Universit£
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2179-83 (2007)
Johnson & Johnson Pharmaceutical Research & Development
1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2523-6 (2007)
University of Antwerp
Sesterterpene sulfates as isocitrate lyase inhibitors from tropical sponge Hippospongia sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2483-6 (2007)
Korea Ocean Research and Development Institute
Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2603-7 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2594-7 (2007)
University of Missouri-Columbia
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2123-5 (2007)
Sun Yat-Sen University
M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2649-55 (2007)
University of Strathclyde
Optimization of halopemide for phospholipase D2 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2310-1 (2007)
Novartis Institutes For Biomedical Research
Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2317-21 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2531-4 (2007)
Johnson and Johnson Pharmaceutical Research and Development
Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2540-4 (2007)
Neuraxon
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2618-21 (2007)
Mitsubishi Pharma
Relationship between quantum-chemical descriptors of proton dissociation and experimental acidity constants of various hydroxylated coumarins. Identification of the biologically active species for xanthine oxidase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1028-31 (2007)
Università
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1044-8 (2007)
Sungshin Women'S University
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 799-806 (2007)
University of Patras
Generation of oxamic acid libraries: antimalarials and inhibitors of Plasmodium falciparum lactate dehydrogenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Comb Chem 9: 292-300 (2007)
University of Mississippi
Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1146-57 (2007)
Berlex Biosciences
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1365-79 (2007)
Pharmaceutical Research Institute
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1414-7 (2007)
Clinical Research Institute of Montreal
Somatostatin receptor-binding peptides suitable for tumor radiotherapy with Re-188 or Re-186. Chemistry and initial biological studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1354-64 (2007)
Diatide Research Laboaratories
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1124-32 (2007)
Astex
Application of fragment screening by X-ray crystallography to beta-secretase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1116-23 (2007)
Astex
Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1635-44 (2007)
The Ohio State University
Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1090-100 (2007)
Glaxosmithkline
Phosph(on)ate as a zinc-binding group in metalloenzyme inhibitors: X-ray crystal structure of the antiviral drug foscarnet complexed to human carbonic anhydrase I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2210-5 (2007)
Universit£
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2643-8 (2007)
Merck Sharp and Dohme Research Laboratories
CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1883-7 (2007)
Berlex Biosciences
Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2492-8 (2007)
Vrije Universiteit Brussel
Guanidinylated neomycin delivers large, bioactive cargo into cells through a heparan sulfate-dependent pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 13585-91 (2007)
University of California
Identification of anesthetic binding sites on human serum albumin using a novel etomidate photolabel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 12038-47 (2007)
Imperial College
Identification of nonpeptide CCR5 receptor agonists by structure-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1294-303 (2007)
Cnrs Umr 7175-Lc1
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1222-30 (2007)
Universit£
Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 2136-42 (2007)
Universit£
Novel malonamide derivatives as potent kappa opioid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1951-5 (2007)
Adolor
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2216-9 (2007)
Wayne State University
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2566-9 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2573-86 (2007)
Università
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2514-27 (2007)
Universit£
Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2126-33 (2007)
Shanghai Jiao Tong University
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1380-400 (2007)
Wyeth Research
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2533-43 (2007)
Università
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2134-8 (2007)
Roche Research Center
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2150-5 (2007)
Pfizer
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2229-32 (2007)
University of Mississippi
Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2118-22 (2007)
Chinese Academy of Sciences
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1166-76 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
Rational design of novel, potent small molecule pan-selectin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1101-15 (2007)
Revotar Biopharmaceuticals
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 1280-7 (2007)
Vertex Pharmaceuticals
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 865-76 (2007)
Pierre Fabre Research Center
N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[(131)I]iodo-5-me thoxybenzyl)acetamide: a potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 848-55 (2007)
National Institute of Radiological Sciences
Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 835-47 (2007)
University of Montpellier
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 828-34 (2007)
Leiden/Amsterdam Center For Drug Research
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 794-806 (2007)
Merck Frosst Canada
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 776-81 (2007)
Elan Pharmaceuticals
Inhibitors of bacterial cystathionine beta-lyase: leads for new antimicrobial agents and probes of enzyme structure and function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 755-64 (2007)
Mcmaster University
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1078-82 (2007)
Abbott Laboratories
Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1041-9 (2007)
Ku Leuven
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 932-9 (2007)
Tokyo Medical and Dental University
Amphipathic benzoic acid derivatives: synthesis and binding in the hydrophobic tunnel of the zinc deacetylase LpxC.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2617-23 (2007)
University of San Francisco
TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 174-82 (2007)
Ku Leuven
An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 104: 2602-7 (2007)
The Scripps Research Institute
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Mol Graph Model 26: 236-45 (2007)
Dalian University
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2631-50 (2007)
Minase Research Institute
Dibenzothiazoles as novel amyloid-imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2789-96 (2007)
Case Western Reserve University
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2184-7 (2007)
Merck Research Laboratories
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2715-35 (2007)
Minase Research Institute
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2587-600 (2007)
University of Tokyo
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1860-4 (2007)
Pharmaceutical Research Institute
A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1916-9 (2007)
Bayer Pharmaceuticals
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2312-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2601-10 (2007)
Dr. Reddys Laboratories
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1903-7 (2007)
Merck Research Laboratories
Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 353-60 (2007)
University of Bonn
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 901-14 (2007)
Gedeon Richter
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1843-9 (2007)
Tibotec
Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2329-33 (2007)
Universit£
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2322-8 (2007)
Merck Research Laboratories
Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2260-6 (2007)
Shanghai Jiao Tong University School of Medicine
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2281-4 (2007)
Schering-Plough Research Institute
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2250-3 (2007)
Vertex Pharmaceuticals
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2759-67 (2007)
Abbott Laboratories
Design, synthesis, inhibitory activity, and SAR studies of pyrrolidine derivatives as neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2749-58 (2007)
Shandong University
Synthesis and characterization of a platinum(II) complex tethered to a ligand of the peripheral benzodiazepine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1019-27 (2007)
Università
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 962-78 (2007)
National Cancer Institute-Frederick
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2305-9 (2007)
Amgen
Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 296-9 (2007)
Chinese Academy of Medical Sciences and Peking Union Medical College
Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 1058-68 (2007)
The Scripps Research Institute
Mechanism of inactivation of plasminogen activator inhibitor-1 by a small molecule inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 9288-96 (2007)
University of Michigan Medical School
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2293-8 (2007)
University of London
High-affinity carbamate analogues of morphinan at opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1508-11 (2007)
Harvard Medical School
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2254-9 (2007)
Glaxosmithkline
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2299-304 (2007)
Amgen
Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1520-2 (2007)
University of Florida
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1865-70 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2312-21 (2007)
Universit£
Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2298-311 (2007)
Universit£
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1956-60 (2007)
Universit£
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2005-12 (2007)
Abbott Laboratories
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1996-9 (2007)
Pfizer
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2068-73 (2007)
Yale University
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1773-8 (2007)
Glaxosmithkline
A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 367: 882-94 (2007)
Astex
The effect of 5-substitution in the pyrimidine ring of dUMP on the interaction with thymidylate synthase: molecular modeling and QSAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2346-58 (2007)
Polish Academy of Sciences
Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2269-82 (2007)
Equipe De Chimie ThéRapeutique
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2223-68 (2007)
Pomona College
Synthesis and biological evaluation of unprecedented classes of spiro-beta-lactams and azido-beta-lactams as acyl-CoA:cholesterol acyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1946-50 (2007)
Università
Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 984-1000 (2007)
Bayer Healthcare Pharmaceuticals
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2031-5 (2007)
Merck Research Laboratories
Novel hydroxamic acid-related phosphinates: inhibition of neutral aminopeptidase N (APN).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1516-9 (2007)
Wroclaw University of Technology
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2036-42 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1466-70 (2007)
Korea Institute of Science and Technology
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 940-50 (2007)
Dartmouth College
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2368-74 (2007)
Clermont Auvergne University
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2375-85 (2007)
Taisho Pharmaceutical
Synthesis and evaluation of 2',4',6'-trihydroxychalcones as a new class of tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2396-402 (2007)
Hokkaido University
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1961-5 (2007)
Abbott Laboratories
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1527-31 (2007)
Ligand Pharmaceuticals
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2022-5 (2007)
Pfizer
Oxazolidinones as novel human CCR8 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1722-5 (2007)
Glaxosmithkline
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 566-84 (2007)
Millennium Pharmaceuticals
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 512-20 (2007)
Medical University
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 489-500 (2007)
Friedrich-Alexander University
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 462-71 (2007)
University of Minnesota Health Science Center
Pharmacophore-based design of sphingosine 1-phosphate-3 receptor antagonists that include a 3,4-dialkoxybenzophenone scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 442-54 (2007)
Toa Eiyo
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 433-41 (2007)
Cephalon
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 429-32 (2007)
Amgen
Monoamine oxidase isoform-dependent tautomeric influence in the recognition of 3,5-diaryl pyrazole inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 425-8 (2007)
Sapienza University of Rome
Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 595-8 (2007)
Universita' Di Siena
Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 765-75 (2007)
National Institute of Immunology
Potentiation of mammary cancer inhibition by combination of antagonists of growth hormone-releasing hormone with docetaxel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 1943-6 (2007)
Veterans Affairs Medical Center
A clickable inhibitor reveals context-dependent autoactivation of p90 RSK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 156-60 (2007)
University of California
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1976-82 (2007)
Tehran University of Medical Sciences
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2441-52 (2007)
Abbott Laboratories
Probing binding requirements of NAD kinase with modified substrate (NAD) analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1512-5 (2007)
University of Minnesota
An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 2026-30 (2007)
Pharmaceutical Research Institute
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1471-4 (2007)
Johnson & Johnson Pharmaceutical Research & Development
A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1675-8 (2007)
Pfizer
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1616-21 (2007)
Kyowa Hakko Kogyo
Carbonic anhydrase inhibitors. Inhibition of transmembrane isozymes XII (cancer-associated) and XIV with anions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1532-7 (2007)
Università
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1523-6 (2007)
Ligand Pharmaceuticals
Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1558-61 (2007)
Nagoya City University
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1788-92 (2007)
Merck Research Laboratories
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 591-4 (2007)
Novartis Pharmaceuticals
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 603-6 (2007)
Incyte
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 641-62 (2007)
Abbott Laboratories
New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 922-31 (2007)
Sapienza University of Rome
Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 8915-25 (2007)
University of North Dakota School of Medicine and Health Sciences
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1646-50 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 2018-21 (2007)
Karo Bio
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1565-9 (2007)
Faculté
Saliniketals A and B, bicyclic polyketides from the marine actinomycete Salinispora arenicola.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 83-8 (2007)
University of California - San Diego
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 627-40 (2007)
Amgen
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 611-26 (2007)
Amgen
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 707-12 (2007)
Universit?????? Degli Studi Di Roma "La Sapienza
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzyme Inhib Med Chem 21: 703-10 (2006)
University of Karachi
Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 9740-7 (2007)
Cnrs-Commissariat à
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1570-4 (2007)
Université
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1679-83 (2007)
Valeant Pharmaceuticals Research and Development
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1671-4 (2007)
Merck Frosst Centre For Therapeutic Research
Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1718-21 (2007)
Pharmacopeia Drug Discovery
Cinnabaramides A-G: analogues of lactacystin and salinosporamide from a terrestrial streptomycete.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 70: 246-52 (2007)
Intermed Discovery Gmbh (Imd)
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 782-93 (2007)
University of Nottingham
Synthesis and cell-based activity of a potent and selective protein tyrosine phosphatase 1B inhibitor prodrug.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 856-64 (2007)
Purdue University
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 807-19 (2007)
Merck Research Laboratories
Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 9657-65 (2007)
Cancer Research Uk Clinical Centre
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 607-10 (2007)
Amgen
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 685-95 (2007)
Gsk
Chromosome-encoded narrow-spectrum Ambler class A beta-lactamase GIL-1 from Citrobacter gillenii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 1365-72 (2007)
Bicetre Hospital
Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1584-9 (2007)
Gsk
Selective L-nitroargininylaminopyrrolidine and L-nitroargininylaminopiperidine neuronal nitric oxide synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1928-38 (2007)
Northwestern University
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1691-4 (2007)
Virginia Commonwealth University
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1765-8 (2007)
Eli Lilly
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1211-5 (2007)
Pharmacopeia Drug Discovery
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1793-8 (2007)
Cephalon
Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nature 445: 541-545 (2007)
The Scripps Research Institute
The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2092-105 (2007)
Procter & Gamble Pharmaceuticals
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1750-4 (2007)
Glaxosmithkline
Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1713-7 (2007)
Glaxosmithkline
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1376-80 (2007)
Schering-Plough Research Institute
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1989-2005 (2007)
Taisho Pharmaceutical
Azetidinones as vasopressin V1a antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2054-80 (2007)
Lehigh University
Novel trifluoroacetophenone derivatives as malonyl-CoA decarboxylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1127-30 (2007)
Chugai Pharma Usa
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1659-62 (2007)
Schering-Plough Research Institute
Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1708-12 (2007)
Central Drug Research Institute
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1243-5 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of thienopyridines as Src-family selective Lck inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1167-71 (2007)
Abbott Bioresearch Center
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1803-7 (2007)
Abbott Laboratories
1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1741-5 (2007)
Glaxosmithkline
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 874-8 (2007)
Abbott Laboratories
Coupling substrate and ion binding to extracellular gate of a sodium-dependent aspartate transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nature 445: 387-93 (2007)
Columbia University
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 404-7 (2007)
Universita Di Pisa
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 399-403 (2007)
University of Illinois At Urbana-Champaign
Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 394-8 (2007)
Central Drug Research Institute
Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 389-93 (2007)
Instituto De QuíMica MéDica
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 381-8 (2007)
Kochi Medical School
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 374-80 (2007)
Universit£
Synthesis and cancer chemopreventive activity of zapotin, a natural product from Casimiroa edulis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 350-5 (2007)
Purdue University
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 344-9 (2007)
Pfizer
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 328-33 (2007)
Hungarian Academy of Sciences
Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 272-82 (2007)
Merck Research Laboratories
Optimization of monocarboxylate transporter 1 blockers through analysis and modulation of atropisomer interconversion properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 254-63 (2007)
Astrazeneca
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 233-40 (2007)
Eli Lilly
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 219-32 (2007)
Massachusetts College of Pharmacy and Health Sciences
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 199-210 (2007)
Achillion Pharmaceuticals
Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone functionalities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 192-8 (2007)
Kyoto University
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 186-91 (2007)
University of Leeds
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 182-5 (2007)
Pfizer
Advances in development of dopaminergic aporphinoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 171-81 (2007)
Chinese Academy of Sciences
Development of selective inhibitors for anti-apoptotic Bcl-2 proteins from BHI-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2167-76 (2007)
University of Minnesota
Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2127-46 (2007)
Berlex
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Nucl Med Mol Imaging 34: 1050-60 (2007)
Columbia University
Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 1577-9 (2007)
Veterans Affairs Medical Center
Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Cancer Ther 6: 163-72 (2007)
Loma Linda University
Modulating effects of a novel skin-lightening agent, alpha-lipoic acid derivative, on melanin production by the formation of DOPA conjugate products.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1967-75 (2007)
Dhc
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 2156-66 (2007)
University of North Carolina At Chapel Hill
Small-molecule agonists for the glucagon-like peptide 1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 937-42 (2007)
Novo Nordisk Als
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 943-8 (2007)
National Center For Drug Screening
Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 2187-97 (2007)
University of Regensburg
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1189-92 (2007)
Wyeth Research
Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1185-8 (2007)
Wyeth Research
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1386-91 (2007)
Merck
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 165-8 (2007)
University of Arizona
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 149-64 (2007)
Abbott Laboratories
Metabolism-based identification of a potent thrombin receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 129-38 (2007)
Schering-Plough Research Institute
New beta-alanine derivatives are orally available glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 113-28 (2007)
Novo Nordisk
Isofagomine- and 2,5-anhydro-2,5-imino-D-glucitol-based glucocerebrosidase pharmacological chaperones for Gaucher disease intervention.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 94-100 (2007)
The Scripps Research Institute
Discovering potassium channel blockers from synthetic compound database by using structure-based virtual screening in conjunction with electrophysiological assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 83-93 (2007)
Chinese Academy of Sciences
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 65-73 (2007)
University of California San Francisco
2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 40-64 (2007)
Wyeth Research
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 21-39 (2007)
Wyeth Research
Discovery and refinement of a new structural class of potent peptide deformylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 50: 10-20 (2007)
Centre National De La Recherche Scientifique
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 6-9 (2007)
Glaxosmithkline
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 50: 2-5 (2007)
Glaxosmithkline
Structure and regulation of the human Nek2 centrosomal kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 6833-42 (2007)
University of Oxford
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1586-605 (2007)
Abbott Laboratories
High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1280-3 (2007)
Harvard Medical School
Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1784-7 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1233-7 (2007)
Bristol-Myers Squibb
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1254-9 (2007)
The Genomics Institute of The Novartis Research Foundation
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1221-5 (2007)
Sapienza University of Rome
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1307-11 (2007)
F. Hoffmann-La Roche
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1200-5 (2007)
Glaxosmithkline
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Drug Metab Dispos 35: 493-500 (2007)
Act
Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1651-8 (2007)
Ewha Womans University
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 1679-93 (2007)
Daiichi Pharmaceutical
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1296-301 (2007)
Glaxosmithkline
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1274-9 (2007)
National Health Research Institutes
Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1422-7 (2007)
Institute of Medical Research
A potent and orally active HIV-1 integrase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1392-8 (2007)
Merck Research Laboratories
Cellular inhibition of protein tyrosine phosphatase 1B by uncharged thioxothiazolidinone derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 8: 179-86 (2007)
Mcgill University
Bioactive oligostilbenoids from the stem bark of Hopea exalata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1800-2 (2006)
Nanjing University
Sodwanone and yardenone triterpenes from a South African species of the marine sponge Axinella inhibit hypoxia-inducible factor-1 (HIF-1) activation in both breast and prostate tumor cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1715-20 (2006)
University of Mississippi
Hyrtiazepine, an azepino-indole-type alkaloid from the Red Sea marine sponge Hyrtios erectus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1676-9 (2006)
Umr 5154 Cnrs
Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli beta-ketoacyl-ACP-synthase III (FabH).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 879-83 (2007)
Portland State University
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1250-3 (2007)
Procter and Gamble Pharmaceuticals
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1302-6 (2007)
F. Hoffmann-La Roche
3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1291-5 (2007)
Korea Research Institute of Chemical Technology
3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1349-54 (2007)
Berlex Biosciences
Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1260-5 (2007)
University of Nebraska Medical Center
Synthesis and HIV-1 integrase inhibitory activity of spiroundecane(ene) derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1362-8 (2007)
Siberian Branch of The Russian Academy of Sciences
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1694-702 (2007)
Lanzhou University
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1369-75 (2007)
Chemical Diversity
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1399-402 (2007)
Friedrich-Schiller-UniversitäT Jena
Thienopyridine urea inhibitors of KDR kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1246-9 (2007)
Abbott Laboratories
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 925-31 (2007)
Mitsubishi Pharma
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 884-9 (2007)
Abbott Laboratories
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1413-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1358-61 (2007)
Wyeth Research
A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1408-12 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1703-7 (2007)
Hoshi University
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 902-6 (2007)
Wyeth Research
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 974-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure of acid beta-glucosidase with pharmacological chaperone provides insight into Gaucher disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 101-7 (2007)
Harvard Medical School
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 104: 270-5 (2007)
Genomics Institute of The Novartis Research Foundation
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 334-43 (2007)
Johnson & Johnson Pharmaceutical Research and Development
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 1: 702-12 (2006)
Rutgers University
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7916-20 (2006)
University of Michigan
Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7912-5 (2006)
Eberhard-Karls-Universit£T
N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7907-11 (2006)
University of Kuopio
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7887-96 (2006)
Boehringer Ingelheim Pharmaceuticals
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7868-76 (2006)
Wyeth Research
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7843-53 (2006)
Abbott Laboratories
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7826-35 (2006)
Dipartimento Di Scienze Farmaceutiche
9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7816-25 (2006)
Westphalian Wilhelms-University
Synthesis and evaluation of multisubstrate bicyclic pyrimidine nucleoside inhibitors of human thymidine phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7807-15 (2006)
Attenuon
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7781-91 (2006)
Daiichi Asubio Medical Research Laboratories
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7766-73 (2006)
Instituto De QuíMica MéDica (Csic)
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7731-9 (2006)
University of Minnesota
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7697-710 (2006)
The Scripps Research Institute
2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7683-96 (2006)
University of Bath
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7636-45 (2006)
University of Edinburgh
Antitubercular nucleosides that inhibit siderophore biosynthesis: SAR of the glycosyl domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7623-35 (2006)
University of Minnesota
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7607-10 (2006)
Laboratorio De Radicales Libres (Iqog, Csic)
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7603-6 (2006)
Schering-Plough Research Institute
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7596-9 (2006)
Bristol-Myers Squibb
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7584-7 (2006)
Merck Research Laboratories
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 3428-32 (2007)
University of Oklahoma Health Sciences Center
3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1284-7 (2007)
Keimyung University
Quinazoline and benzimidazole MCH-1R antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1403-7 (2007)
Argenta Discovery
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 916-20 (2007)
Glaxosmithkline
Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1533-8 (2007)
Sun Yat-Sen University
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1432-7 (2007)
Bristol-Myers Squibb
Novel amidino-substituted benzimidazoles: synthesis of compounds and inhibition of dipeptidyl peptidase III.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 35: 153-69 (2007)
The Josip Juraj Strossmayer University
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 657-61 (2007)
Procter and Gamble Pharmaceuticals
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1438-42 (2007)
Genentech
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 8005-10 (2007)
Merck Research Laboratories
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 103: 19866-71 (2006)
Targegen
Inhibitory effects of phloridzin dihydrate on the activity of mushroom (Agaricus bisporus) tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1568-71 (2007)
Xiamen University
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 907-10 (2007)
Johnson and Johnson Pharmaceutical Research and Development
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1443-6 (2007)
Abbott Laboratories
Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 1: 585-93 (2006)
University of California San Francisco
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 1: 525-33 (2006)
Genentech
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 5536-44 (2007)
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti
Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 8368-79 (2007)
Chul
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1828-47 (2007)
Organon Laboratories
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 1: 43-53 (2006)
Suny Stony Brook
Antiparasitic drug nitazoxanide inhibits the pyruvate oxidoreductases of Helicobacter pylori, selected anaerobic bacteria and parasites, and Campylobacter jejuni.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 868-76 (2007)
University of Virginia Health Systems
Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1212-28 (2007)
University of Tennessee Health Science Center
Parallel solid synthesis of inhibitors of the essential cell division FtsZ enzyme as a new potential class of antibacterials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1330-40 (2007)
Universit£
Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 987-92 (2007)
Griffith University
Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 22-7 (2007)
Gsk
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 937-41 (2007)
Lg Life Sciences
Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1056-61 (2007)
Bayer Pharmaceuticals
Quantitative structure-activity relationship (QSAR) of indoloacetamides as inhibitors of human isoprenylcysteine carboxyl methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1025-32 (2007)
National University of Singapore
13C bis-labeled pyrroles: a tool for the identification of the rat metabolism of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 969-73 (2007)
Glaxosmithkline
Synthesis of a novel inhibitor against MRSA and VRE: preparation from zerumbone ring opening material showing histidine-kinase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1098-101 (2007)
Kinki University
Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1112-6 (2007)
National Research Laboratory of Lipid Metabolism and Atherosclerosis
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 688-91 (2007)
Activesight
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6888-96 (2006)
University of Arizona
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6869-87 (2006)
Abbott Laboratories
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6848-57 (2006)
Purdue University
Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6833-40 (2006)
Universitat De Barcelona
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6819-32 (2006)
Bristol-Myers Squibb
In silico-guided target identification of a scaffold-focused library: 1,3,5-triazepan-2,6-diones as novel phospholipase A2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6768-78 (2006)
Cnrs Umr 7175
Synthesis, radiosynthesis, and biological evaluation of carbon-11 labeled 2beta-carbomethoxy-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6760-7 (2006)
Emory University
Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6726-31 (2006)
Abbott Laboratories
5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6704-15 (2006)
University Hospital of The WestfäLische Wilhelms-UniversitäT
Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6652-5 (2006)
University of Southampton
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6650-1 (2006)
Vrije Universiteit Amsterdam
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6646-9 (2006)
Irbm-Mrl
Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6642-5 (2006)
University of Bologna
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6638-41 (2006)
7Tm Pharma
Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6635-7 (2006)
Karo Bio
Lead discovery and optimization of T-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1409-19 (2007)
Institute of Science and Technology
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7549-53 (2006)
Eberhard-Karls University
Engineering of a VPAC2 receptor peptide agonist to impart dipeptidyl peptidase IV stability and enhance in vivo glucose disposal.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7545-8 (2006)
Bayer Pharmaceuticals
Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7540-4 (2006)
Rheinische Friedrich-Wilhelms-Universitat Bonn
Design and evaluation of hydroxamate derivatives as metal-mediated inhibitors of a protein tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7532-9 (2006)
University of Rhode Island
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7513-7 (2006)
The University of Texas
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7502-12 (2006)
Universit£
Structure-activity relationship analysis of the selective inhibition of transglutaminase 2 by dihydroisoxazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7493-501 (2006)
Stanford University
Progressive docking: a hybrid QSAR/docking approach for accelerating in silico high throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7466-78 (2006)
University of British Columbia
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7450-65 (2006)
Abbott Laboratories
High antiplasmodial activity of novel plasmepsins I and II inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7440-9 (2006)
University of Milan
Fluorinated conformationally restricted gamma-aminobutyric acid aminotransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7404-12 (2006)
Northwestern University
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7373-83 (2006)
Ghent University
Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7366-72 (2006)
Orebro University
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7357-65 (2006)
Ghent University
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7342-56 (2006)
University of Massachusetts Medical School
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7331-41 (2006)
University of Illinois At Urbana - Champaign
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7307-16 (2006)
Albert-Ludwigs-University of Freiburg
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7290-306 (2006)
Adolor
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7278-89 (2006)
Adolor
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7270-3 (2006)
Merck Research Laboratories
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 543-50 (2007)
Gilead Sciences
The pyrophosphate analogue foscarnet traps the pre-translocational state of HIV-1 reverse transcriptase in a Brownian ratchet model of polymerase translocation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 3337-46 (2007)
Mcgill University
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1237-51 (2007)
Kobe Gakuin University
Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 2505-11 (2007)
Activx Biosciences
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 662-7 (2007)
Ionix Pharmaceuticals
Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 4085-93 (2007)
Johnson & Johnson Pharmaceutical
Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 282: 4094-101 (2007)
Johnson & Johnson Pharmaceutical
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1033-6 (2007)
Glaxosmithkline
Design and synthesis of a novel class of dual PPARgamma/delta agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1052-5 (2007)
Eli Lilly
Dibenzocyclooctadiene lignans: a class of novel inhibitors of multidrug resistance-associated protein 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Life Sci 80: 741-8 (2007)
Zhejiang University
Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1311-22 (2007)
Procter & Gamble Pharmaceuticals
DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1146-59 (2006)
University Heights
Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1266-74 (2007)
Instituto Superior T£Cnico
1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1091-7 (2007)
Osi Pharmaceuticals
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1047-51 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Novel carbazole derivatives as NPY Y1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 1043-6 (2007)
Glaxosmithkline
Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides: a late-stage diversification approach to potent 5HT1B antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 939-50 (2006)
Astrazeneca Pharmaceuticals
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1394-408 (2007)
Chinese Academy of Sciences
Design and study of some novel ibuprofen derivatives with potential nootropic and neuroprotective properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 951-61 (2006)
Aristotelian University of Thessaloniki
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1298-310 (2007)
University of Kansas
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 587-92 (2007)
Merck Research Laboratories
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7247-51 (2006)
Nerviano Medical Sciences
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7242-6 (2006)
Wayne State University
Discovering inhibitors of human sirtuin type 2: novel structural scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7239-41 (2006)
University of Kuopio
Structure-activity relationships of a novel series of urotensin II analogues: identification of a urotensin II antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7234-8 (2006)
University of Rouen
Synthesis and radioligand binding studies of methoxylated 1,2,3,4-tetrahydroisoquinolinium derivatives as ligands of the apamin-sensitive Ca2+-activated K+ channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7208-14 (2006)
University of Li£Ge
Discovery of a new class of macrocyclic antagonists to the human motilin receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7190-7 (2006)
Tranzyme Pharma
Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7160-8 (2006)
Uppsala University
Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7150-9 (2006)
Institute of Organic and Bioorganic Chemistry
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7140-9 (2006)
Universit£
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7132-9 (2006)
Biogen Idec
Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7119-31 (2006)
Biogen Idec
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7108-18 (2006)
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7095-107 (2006)
Glaxosmithkline
Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7076-87 (2006)
University of Bonn
Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 7063-75 (2006)
Teikyo University
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 7024-31 (2006)
Universite Montpellier Ii
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6987-7001 (2006)
Human Biomolecular Research Institute
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6977-86 (2006)
University of Prince Edward Island
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6954-7 (2006)
Merck Research Laboratories
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6950-3 (2006)
Central Pharmaceutical Research Institute
Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6946-9 (2006)
Cerep
Triterpene saponins from clematis mandshurica.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1591-5 (2006)
Peking University Health Science Center
Biologically active triterpenoid saponins from Acanthopanax senticosus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1577-81 (2006)
Toho University
Protein tyrosine phosphatase-1B inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1572-6 (2006)
Korea Research Institute of Bioscience and Biotechnology
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 702-13 (2006)
University of Kansas
Synthesis of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 616-25 (2006)
Institutet
Serendipitous discovery of novel bacterial methionine aminopeptidase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proteins 66: 538-46 (2007)
The Procter & Gamble Pharmaceuticals
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 315-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 727-31 (2007)
Ono Pharmaceutical
Highly constrained bicyclic VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 597-601 (2007)
Merck Research Laboratories
Design and syntheses of novel phthalazin-1(2H)-one derivatives as acetohydroxyacid synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Agric Food Chem 54: 9135-9 (2006)
Central China Normal University
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 429-37 (2007)
Valeant Research and Development
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 638-44 (2007)
Universidade Federal Do Rio De Janeiro
Substrate specificity analysis and inhibitor design of homoisocitrate dehydrogenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 1346-55 (2007)
Tokyo Institute of Technology
Forward chemical genetic approach identifies new role for GAPDH in insulin signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 3: 55-9 (2007)
New York University
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 103: 18148-53 (2006)
Johns Hopkins University
Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 13: 1203-15 (2006)
University of Nottingham
Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1448-74 (2007)
Uppsala University
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Anal Biochem 360: 30-40 (2007)
Pfizer
High affinity Grb2-SH3 domain ligand incorporating Cbeta-substituted prolines in a Sos-derived decapeptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1439-47 (2007)
Université
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 641-55 (2006)
Mitsubishi Pharma
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 663-77 (2006)
University of Virginia
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 602-8 (2007)
Targegen
Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 654-6 (2007)
The University of Texas
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 1117-21 (2007)
Merck Research Laboratories
A review of anti-infective and anti-inflammatory chalcones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 125-37 (2007)
Adam Mickiewicz University
Design, parallel synthesis and SAR of novel urotensin II receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 276-85 (2007)
G£Teborg University
TOMOCOMD-CARDD descriptors-based virtual screening of tyrosinase inhibitors: evaluation of different classification model combinations using bond-based linear indices.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1483-503 (2007)
Central University of Las Villas
Structure-activity relationships of 19-norvitamin D analogs having a fluoroethylidene group at the C-2 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1475-82 (2007)
Tokyo Medical and Dental University
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 903-14 (2006)
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 854-67 (2006)
Teikyo University
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 750-5 (2007)
Abbott Laboratories
New approaches to molecular cancer therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 2: 689-700 (2006)
The Institute of Cancer Research
From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 350-3 (2007)
Irbm-Mrl Rome
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 702-6 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 668-72 (2007)
Abbott Laboratories
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 819-22 (2007)
Procter & Gamble Pharmaceuticals
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 789-92 (2007)
Inserm U761 Biostructures and Drug Discovery Lille
MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 832-5 (2007)
Procter & Gamble Pharmaceuticals
Evaluating scoring functions for docking and designing beta-secretase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 823-7 (2007)
Merck Research Laboratories
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 673-8 (2007)
Bayer Healthcare
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 814-8 (2007)
Procter & Gamble Pharmaceuticals
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 363-9 (2007)
Argenta Discovery
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 800-14 (2007)
Paradigm Pharmaceuticals
Discovery of Helicobacter pylori shikimate kinase inhibitors: bioassay and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 656-62 (2006)
Chinese Academy of Sciences
Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 678-85 (2006)
Research Triangle Institute
Core exploration in optimization of chemokine receptor CCR4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 679-82 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 732-5 (2007)
Glaxosmithkline
Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 697-701 (2007)
Ucb Pharma
Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 736-40 (2007)
Incyte
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 868-85 (2006)
Kissei Pharmaceutical
Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 727-34 (2006)
Central Drug Research Institute
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 756-60 (2007)
Pfizer
Pharmacophore identification of KSP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 722-6 (2007)
China Pharmaceutical University
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 337-40 (2007)
Astrazeneca R&D Boston
Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 745-9 (2007)
National Institute On Drug Abuse-Intramural Research Program
Evolution of thiazolidine-based blockers of human Kv1.5 for the treatment of atrial arrhythmias.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 282-4 (2006)
Procter and Gamble Pharmaceuticals
Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 354-7 (2007)
Paradigm Therapeutics
Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 533-7 (2007)
Institute For Degenerative Diseases
Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 394-9 (2007)
Astrazeneca
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 370-5 (2007)
Argenta Discovery
Inhibition of metalloprotease botulinum serotype A from a pseudo-peptide binding mode to a small molecule that is active in primary neurons.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 282: 5004-14 (2007)
National Cancer Institute-Frederick
Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 309-14 (2007)
Merck Research Laboratories
Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 476-81 (2007)
Institute of Science and Technology
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 828-31 (2007)
Merck Research Laboratories
Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 350-3 (2006)
Kyoto Institute of Technology
Design, synthesis, and SAR analysis of novel selective sigma1 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 771-83 (2006)
Università
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 791-9 (2006)
Università
New competitive inhibitors of cytosolic (NADH-dependent) rabbit muscle glycerophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 410-3 (2007)
Paris-Sud University
Simplified staurosporine analogs as potent JAK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 326-31 (2007)
Johnson & Johnson Pharmaceutical Research and Development
Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 807-13 (2007)
Merck Research Laboratories
Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 761-6 (2007)
National Institute of Diabetes and Digestive and Kidney Diseases
Preparation of secolycorines against acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1034-43 (2006)
National Taiwan University
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 886-96 (2007)
Universit£
Design and synthesis of rho kinase inhibitors (III).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1022-33 (2006)
Kirin Brewery
The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 385-9 (2007)
Gsk
Studies towards the identification of a new generation of atypical antipsychotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 400-5 (2007)
Uk. Vinc
Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 243-7 (2007)
Université
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 34: 424-44 (2006)
Medical College of Wiscosin
CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 231-4 (2006)
Berlex Biosciences
Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1014-21 (2006)
Okayama University Graduate School of Medicine
Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 558-61 (2007)
Ucb-Group
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 424-7 (2007)
Glaxosmithkline
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 511-6 (2007)
Schering-Plough Research Institute
Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Antimicrob Agents Chemother 51: 119-27 (2007)
Microbiotix
Ring substituent effects on biological activity of vinyl sulfones as inhibitors of HIV-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1127-37 (2006)
University of California
3D pharmacophore based virtual screening of T-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1091-105 (2006)
Institute of Science and Technology
Novel poly(ADP-ribose) polymerase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 542-5 (2007)
Cephalon
Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 428-33 (2007)
Glaxosmithkline Medicine Research Centre
Deconstructing fragment-based inhibitor discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 2: 720-3 (2006)
TBA
Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1044-55 (2006)
Astellas Pharm
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 142-59 (2006)
Pfizer
A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 63-76 (2006)
University of Lille 2
Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1067-82 (2006)
Organix
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 40-4 (2006)
Abbott Laboratories
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 491-4 (2007)
Universit£
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 527-32 (2007)
Abbott Laboratories
Synthesis and biological evaluation of methanesulfonamide analogues of rofecoxib: Replacement of methanesulfonyl by methanesulfonamido decreases cyclooxygenase-2 selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 1056-61 (2006)
University of Alberta Edmonton
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1514-6 (2006)
Glaxosmithkline
Indoleamine 2,3-dioxygenase inhibitors from the Northeastern Pacific Marine Hydroid Garveia annulata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1496-9 (2006)
University of British Columbia
Microbial transformation and butyrylcholinesterase inhibitory activity of (-)-caryophyllene oxide and its derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1429-34 (2006)
University of Karachi
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 69: 1421-4 (2006)
Uppsala University
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 174-85 (2006)
Chugai Pharmaceutical
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 160-73 (2006)
Astellas Pharma
A Pd(0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 130-41 (2006)
Institut Curie
1-Methylpyridinium-4-(4-phenylmethanethiosulfonate) iodide, MTS-MPP+, a novel scanning cysteine accessibility method (SCAM) reagent for monoamine transporter studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 305-11 (2007)
Purdue University
Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 486-90 (2007)
Pfizer
Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 461-4 (2007)
Pusan National University
Synthesis and biological evaluation of novel T-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 471-5 (2007)
Kyung Hee University
Identification of potent and selective TACE inhibitors via the S1 pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 34-9 (2006)
Wyeth Research
Design and synthesis of a novel photoaffinity ligand for the dopamine and serotonin transporters based on 2beta-carbomethoxy-3beta-biphenyltropane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6621-5 (2006)
National Institute On Drug Abuse-Intramural Research Program
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6607-13 (2006)
Università
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6569-84 (2006)
Abbott Laboratories
Cyclic MrIA: a stable and potent cyclic conotoxin with a novel topological fold that targets the norepinephrine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6561-8 (2006)
University of Queensland
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6549-60 (2006)
Hoffmann-La Roche
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6539-48 (2006)
Griffith University
Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6532-8 (2006)
The Danish University of Pharmaceutical Sciences
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6500-9 (2006)
Palacky University
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6465-88 (2006)
Astrazeneca
Further studies on imidazo[4,5-b]pyridine AT1 angiotensin II receptor antagonists. Effects of the transformation of the 4-phenylquinoline backbone into 4-phenylisoquinolinone or 1-phenylindene scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6451-64 (2006)
Università
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6439-42 (2006)
Abbott Laboratories
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6435-8 (2006)
Pfizer
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Drug Metab Dispos 35: 150-67 (2006)
Bristol-Myers Squibb
Development of a novel dicistronic reporter-selectable hepatitis C virus replicon suitable for high-throughput inhibitor screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Antimicrob Agents Chemother 51: 95-102 (2006)
Pfizer
Identification of selective neuropeptide Y2 peptide agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 538-41 (2007)
Bayer Pharmaceuticals
Intermediate analogue inhibitors of mandelate racemase: N-Hydroxyformanilide and cupferron.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 105-8 (2006)
Dalhousie University
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 501-6 (2007)
Covx Research
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 495-500 (2007)
Abbott Laboratories
Discovery of potent and selective PKC-theta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 225-30 (2006)
Boehringer Ingelheim Pharmaceuticals
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 49-52 (2007)
Merck Research Laboratories
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 507-10 (2007)
Tufts University School of Medicine
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 57-62 (2007)
Schering-Plough Research Institute
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 273-82 (2007)
University of Cape Town
Synthesis of beta-ketophosphonate analogs of glutamyl and glutaminyl adenylate, and selective inhibition of the corresponding bacterial aminoacyl-tRNA synthetases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 295-304 (2007)
Crefsip
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 118-22 (2006)
Wyeth Research
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 15: 403-12 (2007)
Astellas Pharma
Design of potent inhibitors of human beta-secretase. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 78-81 (2006)
Pfizer
Design and synthesis of Rho kinase inhibitors (II).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 350-64 (2006)
Kirin Brewery
Design of bioavailable derivatives of 12-(3-adamantan-1-yl-ureido)dodecanoic acid, a potent inhibitor of the soluble epoxide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 312-23 (2006)
Department of Entomology and University of California Davis Cancer Center
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 205-7 (2007)
Schering-Plough Research Institute
Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 132-5 (2006)
Universit£
Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 136-41 (2006)
University College London
Design of potent inhibitors of human beta-secretase. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 73-7 (2006)
Pfizer
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 161-6 (2006)
Cv Therapeutics
Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biopolymers 84: 595-604 (2006)
University of California Davis
BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem J 401: 29-38 (2007)
University of Dundee
Tri-, tetra- and heptacyclic perylene analogues as new potential antineoplastic agents based on DNA telomerase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 555-62 (2006)
University of Padova
Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 365-73 (2006)
Institute of Science and Technology
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 433-43 (2006)
National Institute of Pharmaceutical Education and Research
Identification of novel, selective and potent Chk2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 172-5 (2006)
Valeant Pharmaceutical Research and Development 3300 Hyland Avenue
2,6-Quinolinyl derivatives as potent VLA-4 antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 17: 142-6 (2007)
Ucb Pharma
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 214-9 (2006)
Seoul National University
N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 176-82 (2007)
Darmstadt University of Technology
Identification of a series of highly potent activators of the Nurr1 signaling pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 193-6 (2006)
Novartis Institutes For Biomedical Research
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6421-4 (2006)
National Health Research Institutes
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6416-20 (2006)
Abbott Laboratories
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6408-11 (2006)
Friedrich-Schiller-UniversitäT Jena
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6391-9 (2006)
National Institute On Drug Abuse-Intramural Research Program
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6371-90 (2006)
Johnson and Johnson Pharmaceutical Research and Development
Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6351-63 (2006)
Juvantia Pharma
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6308-23 (2006)
University of California San Francisco
Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6298-307 (2006)
University of California Berkeley
Impact of species-dependent differences on screening, design, and development of MAO B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6264-72 (2006)
University of Geneva
Conformationally restricted dipeptide amides as potent and selective neuronal nitric oxide synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6254-63 (2006)
Northwestern University
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6209-21 (2006)
University of Newcastle Upon Tyne
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6170-6 (2006)
Neurocrine Biosciences
Synthesis and antiviral activity of 5-substituted cytidine analogues: identification of a potent inhibitor of viral RNA-dependent RNA polymerases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6166-9 (2006)
The Pennsylvania State University
Acylguanidines as small-molecule beta-secretase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6158-61 (2006)
Wyeth Research
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6155-7 (2006)
Eli Lilly
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6151-4 (2006)
Wyeth Research
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6147-50 (2006)
Merck Research Laboratories
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6143-6 (2006)
Ligand Pharmaceuticals
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6139-42 (2006)
University of Michigan
Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Chem Biol 2: 608-17 (2006)
University of Cambridge
Probing cell-division phenotype space and Polo-like kinase function using small molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nat Chem Biol 2: 618-26 (2006)
Rockefeller University
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 281: 38013-21 (2006)
Incyte
Synthesis, biological activity and molecular modelling of new trisubstituted 8-azaadenines with high affinity for A1 adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 1-9 (2007)
Università
SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 189-92 (2006)
Wyeth Research
Natural inhibitors targeting osteoclast-mediated bone resorption.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6178-80 (2006)
Chinese Academy of Sciences
Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 272-7 (2006)
Ucb Pharma
Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 220-4 (2006)
Universit£
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6200-3 (2006)
Universit£
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6165-9 (2006)
Merck Research Laboratories
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 266-71 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 250-4 (2006)
Glaxosmithkline
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 320: 89-98 (2006)
Glaxosmithkline
In silico identification and biochemical characterization of novel inhibitors of NQO1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6246-54 (2006)
University of Manchester
Novel nucleotide triphosphates as potent P2Y2 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 17: 562-5 (2007)
Ucb-Group
Structural correlation between lipophilicity and lipopolysaccharide-sequestering activity in spermine-sulfonamide analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6209-12 (2006)
Mediquest Therapeutics
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 16: 6226-30 (2006)
Abbott Laboratories
Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6213-8 (2006)
Procter & Gamble Pharmaceuticals
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6316-20 (2006)
Boehringer Ingelheim Pharmaceuticals
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 5913-6 (2006)
Fudan University
Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (L)-arginine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 37-53 (2007)
Université
Design, synthesis, biochemical evaluation and antimycobacterial action of phosphonate inhibitors of antigen 85C, a crucial enzyme involved in biosynthesis of the mycobacterial cell wall.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 42: 54-63 (2007)
University of Ljubljana
Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 15: 575-85 (2006)
University of Bologna
Structure-activity relationships of Bacillus cereus and Bacillus anthracis dihydrofolate reductase: toward the identification of new potent drug leads.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Antimicrob Agents Chemother 50: 3435-43 (2006)
University of Connecticut At Storrs
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6328-33 (2006)
Eli Lilly
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6293-7 (2006)
Eli Lilly
Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6133-7 (2006)
Uppsala University
Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6111-9 (2006)
Sungkyunkwan University School of Medicine
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6104-10 (2006)
University of Bristol
Evaluation of azasterols as anti-parasitics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6094-103 (2006)
Cardiff University
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 6074-86 (2006)
Schering-Plough Research Institute
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6046-56 (2006)
Sapienza University of Rome
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6037-45 (2006)
Universit£
Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 6027-36 (2006)
Wyeth
A novel class of potent nonglycosidic and nonpeptidic pan-selectin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 5988-99 (2006)
Johannes Gutenberg University
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 5969-87 (2006)
University of North Carolina At Greensboro
Antibacterial agent discovery using thymidylate synthase biolibrary screening.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 49: 5958-68 (2006)
Unimore
Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 49: 5947-57 (2006)
Universit£
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6241-5 (2006)
Abbott Laboratories
Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 6281-7 (2006)
University of Maryland
Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 16: 5978-81 (2006)
Merck Research Laboratories
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)