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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
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
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
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
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
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
Bioorg Med Chem 16: 838-53 (2008)
Universidade De S£O Paulo
Cytochrome P3A4 inhibitors and other constituents of Fibraurea tinctoria.EBI
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
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
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
J Med Chem 50: 6383-91 (2007)
Research Triangle Institute
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.BDB
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
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
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
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
Bioorg Med Chem 16: 1218-35 (2008)
University Of Jordan
Synthesis and evaluation of novel aromatic substrates and competitive inhibitors of GABA aminotransferase.EBI
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
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
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
J Med Chem 50: 5886-9 (2007)
Pfizer
Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.BDB
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
J Nat Prod 70: 1691-5 (2007)
Seoul National University
New potent indole derivatives as hyaluronidase inhibitors.BDB
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
J Med Chem 50: 5912-25 (2007)
Astrazeneca Pharmaceuticals
Discovery of a novel warhead against beta-secretase through fragment-based lead generation.EBI
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
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
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
Bioorg Med Chem 16: 1359-75 (2008)
Osi Pharmaceuticals
Synthesis and characterization of carnitine nitro-derivatives.EBI
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
Bioorg Med Chem 16: 783-93 (2008)
Emory University
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.EBI
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
Bioorg Med Chem Lett 18: 285-8 (2008)
Gakushuin University
Surveying polypeptide and protein domain conformation and association with FlAsH and ReAsH.EBI
Nat Chem Biol 3: 779-84 (2007)
Yale University
Model structure of the Na+/H+ exchanger 1 (NHE1): functional and clinical implications.EBI
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
Bioorg Med Chem Lett 18: 402-4 (2008)
The University Of Sydney
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.BDB
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
Eur J Med Chem 43: 1469-77 (2008)
Université
GRIND-based 3D-QSAR to predict inhibitory activity for similar enzymes, OSC and SHC.EBI
Eur J Med Chem 43: 1462-8 (2008)
Casmedchem Laboratory
Synthesis and biological activity of imidazopyridine anticoccidial agents: Part II.EBI
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
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
Bioorg Med Chem 16: 1299-308 (2008)
Dainippon Sumitomo Pharma
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 6841-6 (2007)
Eli Lilly
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.EBI
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
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
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
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
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
Bioorg Med Chem 16: 650-7 (2008)
Kyoto University
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.EBI
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
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
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
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
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
J Med Chem 50: 5967-75 (2007)
University Of Southern California
Multiple N-methylation by a designed approach enhances receptor selectivity.EBI
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
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
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
J Med Chem 50: 6059-66 (2007)
Cancercare Manitoba
Interactions of methylene blue with human disulfide reductases and their orthologues from Plasmodium falciparum.EBI
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 6887-90 (2007)
Pfizer
Structure-activity relationships of adenosines with heterocyclic N6-substituents.EBI
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
J Med Chem 50: 6080-94 (2007)
University Of Minnesota
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.EBI
J Med Chem 50: 6144-53 (2007)
University M£Nster
Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.EBI
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
Bioorg Med Chem 16: 981-94 (2008)
Nippon Shinyaku
Spermatinamine, the first natural product inhibitor of isoprenylcysteine carboxyl methyltransferase, a new cancer target.EBI
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
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
Bioorg Med Chem Lett 17: 6832-5 (2007)
Cardiff University
Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).EBI
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
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
Bioorg Med Chem 16: 746-54 (2008)
Research Triangle Institute
Discovery of small-molecule inhibitors of tyrosinase.EBI
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
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
Bioorg Med Chem Lett 17: 6825-31 (2007)
Neurocrine Biosciences
Structure activity relationships of quinoline-containing c-Met inhibitors.EBI
Eur J Med Chem 43: 1321-9 (2008)
Pfizer
Activity of sulfonium bisphosphonates on tumor cell lines.EBI
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
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
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
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
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
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
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
J Med Chem 50: 6154-64 (2007)
University Of Wisconsin-Madison
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.EBI
J Med Chem 50: 6004-15 (2007)
Universidad De La RepúBlica
Cytotoxic metabolites from an Indonesian sponge Lendenfeldia sp.EBI
J Nat Prod 70: 1824-6 (2007)
University Of Mississippi
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.EBI
J Med Chem 50: 5568-70 (2007)
University Of Antwerp
Discovery of small molecule CXCR4 antagonists.EBI
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
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
J Med Chem 50: 5720-5726 (2007)
University Of Southampton
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.EBI
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
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
J Med Chem 50: 5644-54 (2007)
Università
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.EBI
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
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
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
Eur J Med Chem 43: 1412-22 (2008)
Universidade Federal De Minas Gerais
Acetyl-lysine analog peptides as mechanistic probes of protein deacetylases.EBI
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
Bioorg Med Chem 16: 144-56 (2008)
Astellas Pharma
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.BDB
Bioorg Med Chem Lett 17: 6463-6 (2007)
The Scripps Research Institute
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors.EBI
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
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
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
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
J Nat Prod 70: 1790-2 (2007)
Griffith University
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.BDB
Biochemistry 46: 13019-30 (2007)
Pfizer
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis.EBI
J Med Chem 50: 5735-42 (2007)
University Of Kansas
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.BDB
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
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
J Med Chem 50: 5589-99 (2007)
Institute Of Sciences
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase.BDB
J Med Chem 50: 5712-9 (2007)
Pfizer
Mechanisms, biology and inhibitors of deubiquitinating enzymes.EBI
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
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
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
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
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
Bioorg Med Chem Lett 17: 6439-43 (2007)
Universidad De Navarra
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.BDB
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 6448-54 (2007)
Astrazeneca
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.EBI
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
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
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
Eur J Med Chem 43: 1222-9 (2008)
Universit£
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.EBI
Bioorg Med Chem 16: 362-73 (2008)
Universit£
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.EBI
Bioorg Med Chem 16: 530-5 (2008)
Yonsei University
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.EBI
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
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
Bioorg Med Chem Lett 17: 6516-20 (2007)
Institute
A phosphorylated prodrug for the inhibition of Pin1.EBI
Bioorg Med Chem Lett 17: 6615-8 (2007)
Virginia Tech
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.EBI
Bioorg Med Chem Lett 17: 6529-34 (2007)
Pfizer
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.EBI
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
Bioorg Med Chem 16: 336-53 (2008)
Universit£
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.EBI
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
Bioorg Med Chem Lett 17: 6489-92 (2007)
Johnson & Johnson Pharmaceutical Research & Development
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.EBI
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
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
Bioorg Med Chem Lett 17: 6546-52 (2007)
Neurocrine Biosciences
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.EBI
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
J Med Chem 50: 5824-32 (2007)
The Johns Hopkins University
De novo discovery of serotonin N-acetyltransferase inhibitors.EBI
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
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
Nat Chem Biol 3: 722-6 (2007)
Glaxosmithkline
Profiling the enzymatic properties and inhibition of human complement factor B.EBI
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
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
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
Bioorg Med Chem 16: 322-35 (2008)
Clemson University
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.EBI
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
Bioorg Med Chem Lett 17: 6079-85 (2007)
Pfizer
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.EBI
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
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
J Med Chem 50: 5269-5280 (2007)
St. Jude Research Hospital
Interactions of hepatitis B core antigen and peptide inhibitors.EBI
J Med Chem 50: 5620-6 (2007)
Universiti Putra Malaysia
Target specific virtual screening: optimization of an estrogen receptor screening platform.EBI
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
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
J Med Chem 50: 5403-11 (2007)
Sapienza University Of Rome
CYP2C9 structure-metabolism relationships: substrates, inhibitors, and metabolites.EBI
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
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
J Med Chem 50: 5471-84 (2007)
Université
Small molecule inhibitors of integrin alpha2beta1.BDB
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
J Med Chem 50: 5339-56 (2007)
Bristol-Myers Squibb
A surface on the androgen receptor that allosterically regulates coactivator binding.EBI
Proc Natl Acad Sci U S A 104: 16074-9 (2007)
University Of California
Potent oxindole based human beta3 adrenergic receptor agonists.EBI
Bioorg Med Chem Lett 17: 6270-3 (2007)
Eli Lilly
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.EBI
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
Bioorg Med Chem Lett 17: 6066-9 (2007)
Glaxosmithkline
Substituted 2-pyrrolinone inhibitors of HIV-1 integrase.EBI
Bioorg Med Chem Lett 17: 6155-9 (2007)
University Of Southern California
Novel scaffold for cathepsin K inhibitors.EBI
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
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
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
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
J Med Chem 50: 5281-92 (2007)
University Of Gent
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.EBI
Bioorg Med Chem 16: 390-9 (2008)
University Of Iowa
Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.EBI
Bioorg Med Chem Lett 17: 6212-5 (2007)
Pedagogical University
Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum.EBI
Bioorg Med Chem 15: 7803-8 (2007)
Hoshi University
Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.EBI
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
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
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
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
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
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
J Med Chem 50: 5245-8 (2007)
Wyeth Research
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.BDB
J Med Chem 50: 5311-23 (2007)
Cnrs
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.EBI
Bioorg Med Chem 15: 7576-80 (2007)
Purdue University
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.EBI
Bioorg Med Chem 15: 7581-9 (2007)
Università
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.EBI
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
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
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
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
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
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
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
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
Bioorg Med Chem 15: 7325-36 (2007)
Meiji Seika Kaisha
Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.EBI
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
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
Bioorg Med Chem Lett 17: 6261-5 (2007)
Université
New functional assay of P-glycoprotein activity using Hoechst 33342.EBI
Bioorg Med Chem 15: 7470-9 (2007)
University Of Bonn
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.EBI
Bioorg Med Chem Lett 17: 6290-4 (2007)
Schering-Plough Research Institute
Androstene-3,5-dienes as ER-beta selective SERMs.EBI
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
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
Bioorg Med Chem Lett 17: 6387-91 (2007)
Institute Of Science
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.EBI
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
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
Bioorg Med Chem Lett 17: 6373-7 (2007)
Development Center For Biotechnology
2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.EBI
Bioorg Med Chem Lett 17: 6266-9 (2007)
Johnson & Johnson
Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.EBI
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
Bioorg Med Chem 15: 7391-8 (2007)
University Of Mysore
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.EBI
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
J Med Chem 50: 5176-82 (2007)
University Of Bath
Macrolactins O-R, glycosylated 24-membered lactones from Bacillus sp. AH159-1.EBI
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
J Med Chem 50: 5253-6 (2007)
Pfizer
Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.BDB
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
J Med Chem 50: 5202-16 (2007)
Bayer Pharmaceuticals
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.BDB
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Bioorg Med Chem 15: 7865-77 (2007)
Università
Two new phenylpiperazines with atypical antipsychotic potential.EBI
Bioorg Med Chem Lett 17: 5749-53 (2007)
Institute For Biological Research
Synthesis of novel anilinoquinolines as c-fms inhibitors.EBI
Bioorg Med Chem Lett 17: 6257-60 (2007)
Glaxosmithkline
Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors.EBI
Eur J Med Chem 43: 1248-60 (2008)
The University Of Manchester
4-thiazolidinone--a biologically active scaffold.EBI
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
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
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
Bioorg Med Chem 15: 7361-7 (2007)
Central Drug Research Institute
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.EBI
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
Bioorg Med Chem Lett 17: 6326-9 (2007)
Astrazeneca
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.EBI
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
Bioorg Med Chem Lett 17: 5863-7 (2007)
Mitsubishi Pharma
Amino-caprolactam derivatives as gamma-secretase inhibitors.EBI
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
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
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
Bioorg Med Chem 15: 7408-25 (2007)
Universidad De Santiago De Chile
Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists.EBI
Bioorg Med Chem Lett 17: 5964-8 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of potent T-type calcium channel blocker.EBI
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
Bioorg Med Chem Lett 17: 6019-25 (2007)
University Of Aarhus
Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.EBI
Bioorg Med Chem Lett 17: 5928-33 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.EBI
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
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
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
J Biol Chem 282: 32549-60 (2007)
Lund University
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.EBI
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
Bioorg Med Chem Lett 17: 5754-7 (2007)
Rti International
Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors.EBI
Bioorg Med Chem Lett 17: 5876-80 (2007)
Purdue University
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.EBI
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
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
J Med Chem 50: 5147-60 (2007)
Schering-Plough Research Institute
Brunneins A-C, beta-carboline alkaloids from Cortinarius brunneus.EBI
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
Bioorg Med Chem 15: 7809-29 (2007)
Institute Of Pharmaceutical Industry
Myricetin inhibits Escherichia coli DnaB helicase but not primase.EBI
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
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
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
Bioorg Med Chem Lett 17: 5902-6 (2007)
Texas Tech University
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.EBI
Bioorg Med Chem Lett 17: 5825-30 (2007)
Amgen
The selectivity of protein kinase inhibitors: a further update.EBI
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
J Med Chem 50: 4882-97 (2007)
University Of Bologna
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.EBI
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
J Med Chem 50: 5043-7 (2007)
Università
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.BDB
J Med Chem 50: 4928-38 (2007)
Montana State University
Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.EBI
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
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
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
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
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
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
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
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
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
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
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
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
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
J Med Chem 50: 4917-27 (2007)
Università
Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.EBI
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
J Nat Prod 70: 1462-6 (2007)
University Of Mississippi
Novel, potent THC/anandamide (hybrid) analogs.EBI
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
Bioorg Med Chem 15: 6956-74 (2007)
Jagiellonian University Medical College
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.EBI
Bioorg Med Chem 15: 7248-57 (2007)
Friedrich-Alexander University
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.EBI
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
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
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
Bioorg Med Chem Lett 17: 5812-8 (2007)
Targegen
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI
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
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
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
Bioorg Med Chem Lett 17: 5783-9 (2007)
Nih
Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.EBI
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
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
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
Bioorg Med Chem Lett 17: 5983-8 (2007)
Pfizer
Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.EBI
Bioorg Med Chem Lett 17: 5940-3 (2007)
University Of Texas Medical Branch
Conformationally constrained analogues of 2-arachidonoylglycerol.EBI
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
Bioorg Med Chem Lett 17: 5768-71 (2007)
Kobe Gakuin University
5'-halogenated analogs of oxymorphindole.EBI
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
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
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
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
Bioorg Med Chem 15: 7258-73 (2007)
Johann Wolfgang Goethe University
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI
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
Bioorg Med Chem Lett 17: 5590-4 (2007)
Université
Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.EBI
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
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
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
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
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
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
Bioorg Med Chem 15: 6975-84 (2007)
Assiut University
Pyrazole-based cathepsin S inhibitors with improved cellular potency.EBI
Bioorg Med Chem Lett 17: 5525-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality.EBI
Bioorg Med Chem Lett 17: 5614-9 (2007)
University Of Minnesota
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.EBI
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
Bioorg Med Chem Lett 17: 5704-8 (2007)
Corcept Therapeutics
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.EBI
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
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
Bioorg Med Chem Lett 17: 5638-42 (2007)
Pfizer
3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1.EBI
Eur J Med Chem 43: 1025-34 (2008)
Biocampus
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 5573-6 (2007)
Chugai Pharmaceutical
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.EBI
Bioorg Med Chem Lett 17: 5600-4 (2007)
Eli Lilly
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.EBI
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
Bioorg Med Chem Lett 17: 5563-6 (2007)
Eli Lilly
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI
Bioorg Med Chem Lett 17: 5577-81 (2007)
Astellas Pharma
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.EBI
Bioorg Med Chem Lett 17: 5620-3 (2007)
Arena Pharmaceuticals
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.EBI
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
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
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
Bioorg Med Chem Lett 17: 5533-6 (2007)
Pfizer
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 5677-82 (2007)
Merck Research Laboratories
Synthesis and biological evaluation of a C5-biphenyl thiolactomycin library.EBI
Bioorg Med Chem Lett 17: 5643-6 (2007)
University Of Birmingham
Novel anti-infection agents: small-molecule inhibitors of bacterial transcription factors.EBI
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
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
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
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
Bioorg Med Chem 15: 6819-29 (2007)
Johannes Gutenberg University
Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores.EBI
Bioorg Med Chem Lett 17: 5325-9 (2007)
Johnson & Johnson Pharmaceutical Research And Development
A refined agonist pharmacophore for protease activated receptor 2.EBI
Bioorg Med Chem Lett 17: 5552-7 (2007)
University Of Queensland
Nucleation of an allosteric response via ligand-induced loop folding.BDB
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
Bioorg Med Chem 15: 6796-801 (2007)
University Of Alberta
Thiazole-diamides as potent gamma-secretase inhibitors.EBI
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
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
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
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
J Med Chem 50: 5012-23 (2007)
Universidad Complutense
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening.BDB
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
Bioorg Med Chem Lett 17: 5390-5 (2007)
Merck Research Laboratories
Thiophene substituted acylguanidines as BACE1 inhibitors.EBI
Bioorg Med Chem Lett 17: 5353-6 (2007)
Wyeth Research
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.EBI
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
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
J Med Chem 50: 5039-42 (2007)
Universit£
2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.EBI
Bioorg Med Chem Lett 17: 5357-60 (2007)
Inha University
Novel ATP-competitive kinesin spindle protein inhibitors.EBI
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
J Med Chem 50: 4630-41 (2007)
Universit£
A Ser678Pro substitution in Fks1p confers resistance to echinocandin drugs in Aspergillus fumigatus.EBI
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
J Biol Chem 282: 30699-706 (2007)
University Of Utah
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.BDB
Bioorg Med Chem 15: 6649-58 (2007)
Incyte
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.EBI
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
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
Bioorg Med Chem Lett 17: 5396-9 (2007)
Pfizer
Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide.EBI
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
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
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
J Med Chem 50: 4656-64 (2007)
Université
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.EBI
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
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
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
Bioorg Med Chem Lett 17: 5349-52 (2007)
Eli Lilly
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).EBI
Bioorg Med Chem Lett 17: 5455-61 (2007)
Bristol-Myers Squibb
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.EBI
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
Bioorg Med Chem Lett 17: 5361-5 (2007)
National Cancer Institute
Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists.BDB
Chem Biol Drug Des 70: 268-72 (2007)
Pfizer
Crystal structure of the T315I mutant of AbI kinase.BDB
Chem Biol Drug Des 70: 171-81 (2007)
Ariad Pharmaceuticals
Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases.EBI
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
Bioorg Med Chem Lett 17: 5370-3 (2007)
Universit£
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos.EBI
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
J Med Chem 50: 4728-45 (2007)
Wyeth Research
Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.EBI
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
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
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
J Med Chem 50: 4648-55 (2007)
Universit£
Novel small-molecule inhibitors of transmissible gastroenteritis virus.EBI
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
Antimicrob Agents Chemother 51: 4181-3 (2007)
Chu Clermont-Ferrand
Quinuclidine derivatives as potential antiparasitics.EBI
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
Bioorg Med Chem Lett 17: 5479-82 (2007)
Pharmacia
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.BDB
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
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
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
Eur J Med Chem 43: 1071-80 (2008)
Shri G.S. Institute Of Technology And Science
Pyrimidine benzamide-based thrombopoietin receptor agonists.EBI
Bioorg Med Chem Lett 17: 5447-54 (2007)
Pfizer
Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.EBI
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
Eur J Med Chem 43: 862-71 (2008)
Nanjing University
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.BDB
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
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
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
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
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
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
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
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
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
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
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
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
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
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
J Med Chem 50: 4471-81 (2007)
University Of Southern California
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.BDB
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
Proc Natl Acad Sci U S A 104: 13827-32 (2007)
University Of Utah
Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors.EBI
Bioorg Med Chem Lett 17: 5462-4 (2007)
Amorepacific
New amido derivatives as potential BKCa potassium channel activators. XI.EBI
Eur J Med Chem 43: 792-9 (2008)
Universit£
Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.EBI
Bioorg Med Chem 15: 6535-48 (2007)
Inha University
Identification of dissociated non-steroidal glucocorticoid receptor agonists.EBI
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
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
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
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
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
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
J Med Chem 50: 4516-27 (2007)
University Of Dublin
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake.EBI
Science 317: 1390-3 (2007)
New York University School Of Medicine
Towards predictive inhibitor design for the EGFR autophosphorylation activity.EBI
Eur J Med Chem 43: 781-91 (2008)
Korea Institute Of Science And Technology
Dual acting antioxidant A1 adenosine receptor agonists.EBI
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
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
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
Bioorg Med Chem Lett 17: 5414-8 (2007)
The University Of Tokyo
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.EBI
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
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
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
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
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
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
J Biol Chem 282: 29241-7 (2007)
Utrecht University
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.EBI
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
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
Bioorg Med Chem 15: 6596-607 (2007)
Woosuk University
Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.EBI
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
Bioorg Med Chem Lett 17: 5032-5 (2007)
Griffith University
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.BDB
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
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
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
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
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
J Med Chem 50: 4543-7 (2007)
Institute Of Science And Technology
Structural and mechanistic basis of penicillin-binding protein inhibition by lactivicins.EBI
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
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
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
J Med Chem 50: 4135-46 (2007)
National Institute On Drug Abuse-Intramural Research Program
C1'-cycloalkyl side chain pharmacophore in tetrahydrocannabinols.EBI
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
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
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
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
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
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
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
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
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
Antimicrob Agents Chemother 51: 3498-504 (2007)
Gilead Sciences
Plasmid-encoded ACC-4, an extended-spectrum cephalosporinase variant from Escherichia coli.EBI
Antimicrob Agents Chemother 51: 3763-7 (2007)
Institute
The phenolic diterpene totarol inhibits multidrug efflux pump activity in Staphylococcus aureus.EBI
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
Bioorg Med Chem 15: 6425-42 (2007)
Wyeth Research
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.EBI
Bioorg Med Chem Lett 17: 5019-24 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
In vitro PAI-1 inhibitory activity of oxalamide derivatives.EBI
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
J Med Chem 50: 4003-4015 (2007)
Nci-Fcrdc
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.EBI
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
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
J Pharmacol Exp Ther 323: 285-93 (2007)
Abbott Laboratories
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.EBI
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
J Med Chem 50: 4162-76 (2007)
Abbott Laboratories
Discovery and optimization of p38 inhibitors via computer-assisted drug design.EBI
J Med Chem 50: 4016-26 (2007)
Boehringer Ingelheim Pharmaceuticals
New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET.EBI
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
J Biol Chem 282: 28096-105 (2007)
Michigan State University
Rational design, synthesis, and biological evaluation of progesterone-modified MRI contrast agents.BDB
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
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
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
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
Biochemistry 46: 9551-63 (2007)
Abbott Laboratories
Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.BDB
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
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
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
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
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 5041-8 (2007)
Bristol-Myers Squibb
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists.EBI
Bioorg Med Chem Lett 17: 5133-5 (2007)
Taisho Pharmaceutical
Splicing factor SF3b as a target of the antitumor natural product pladienolide.BDB
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
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
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
Antimicrob Agents Chemother 51: 4036-43 (2007)
Ambrilia Biopharma
Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase.EBI
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
Bioorg Med Chem Lett 17: 5191-8 (2007)
Merck
Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays.EBI
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 5245-50 (2007)
Pfizer
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.BDB
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
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
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
J Med Chem 50: 3964-8 (2007)
Università
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.EBI
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
Bioorg Med Chem Lett 17: 5165-70 (2007)
Neurocrine Biosciences
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.EBI
Bioorg Med Chem Lett 17: 5218-21 (2007)
Glaxosmithkline
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.EBI
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
Bioorg Med Chem Lett 17: 5214-7 (2007)
Glaxosmithkline
Discovery and SAR studies of novel GlyT1 inhibitors.EBI
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
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
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
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
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
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
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
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
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
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
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
J Med Chem 50: 3897-905 (2007)
Brigham Young University
Novel antagonists of the thioesterase domain of human fatty acid synthase.BDB
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
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
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
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
Bioorg Med Chem 15: 6071-9 (2007)
The Ohio State University
Mycophenolic acid as a latent agonist of PPARgamma.EBI
Bioorg Med Chem Lett 17: 4767-70 (2007)
Hokkaido University
Pyridinylimidazole inhibitors of Tie2 kinase.EBI
Bioorg Med Chem Lett 17: 4756-60 (2007)
Glaxosmithkline
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.EBI
Bioorg Med Chem Lett 17: 4812-8 (2007)
Mahidol University
Bioactive peroxides as potential therapeutic agents.EBI
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
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
J Biol Chem 282: 27126-32 (2007)
University Of WÜRzburg
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.EBI
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
Bioorg Med Chem Lett 17: 4737-45 (2007)
Glaxosmithkline
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.EBI
Bioorg Med Chem Lett 17: 4795-8 (2007)
Merck Research Laboratories
Orally bioavailable potent soluble epoxide hydrolase inhibitors.EBI
J Med Chem 50: 3825-40 (2007)
University Of California Davis
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.EBI
J Med Chem 50: 3786-94 (2007)
Jerini
Hydroxyethylene isosteres of selective neuronal nitric oxide synthase inhibitors.BDB
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
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
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
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
J Nat Prod 70: 1207-9 (2007)
Chungbuk National University
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.EBI
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
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
J Med Chem 50: 3427-30 (2007)
TBA
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.EBI
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
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
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
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
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
Bioorg Med Chem 15: 6242-52 (2007)
Universidade Federal Da Bahia
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.EBI
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
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
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
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
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
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
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
Eur J Med Chem 43: 604-13 (2008)
Chinese Academy Of Sciences
Synthesis and adenosine receptor binding studies of some novel triazolothienopyrimidines.EBI
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
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
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
J Med Chem 50: 3482-8 (2007)
University Of Hamburg
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.EBI
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
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
Bioorg Med Chem Lett 17: 4829-31 (2007)
University Of Maryland
Indanylacetic acids as PPAR-delta activator insulin sensitizers.EBI
Bioorg Med Chem Lett 17: 4369-73 (2007)
Bayer Research Center
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.EBI
Bioorg Med Chem Lett 17: 4837-40 (2007)
Biovitrum
Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK.EBI
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
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
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
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
J Med Chem 50: 3423-6 (2007)
TBA
Interactions of ceftobiprole with beta-lactamases from molecular classes A to D.EBI
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
J Med Chem 50: 3465-81 (2007)
National Cancer Institute-Frederick
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.EBI
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
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
Bioorg Med Chem 15: 6253-61 (2007)
Stanford University
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.EBI
Bioorg Med Chem Lett 17: 4415-8 (2007)
Pfizer
The identification of potent, selective, and bioavailable cathepsin S inhibitors.BDB
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
Science 316: 1759-1761 (2007)
Anacor Pharmaceuticals
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.EBI
Science 317: 516-9 (2007)
Harvard Medical School
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.EBI
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
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
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
Bioorg Med Chem Lett 17: 4419-27 (2007)
Bristol-Myers Squibb
Agonist lead identification for the high affinity niacin receptor GPR109a.EBI
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
Bioorg Med Chem Lett 17: 4895-900 (2007)
The University Of Tokyo
New chemical tools for investigating human mitotic kinesin Eg5.EBI
Bioorg Med Chem 15: 6474-88 (2007)
Cnrs-Université
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.EBI
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
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
Bioorg Med Chem Lett 17: 4934-7 (2007)
Université
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.BDB
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
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
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
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
J Med Chem 50: 3730-42 (2007)
Bristol-Myers Squibb
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.EBI
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
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
J Med Chem 50: 3515-27 (2007)
Amgen
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.BDB
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
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
Chem Biol 14: 613-21 (2007)
University Of Tokyo
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.EBI
J Nat Prod 70: 1118-21 (2007)
Griffith University
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.EBI
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
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
Bioorg Med Chem Lett 17: 4437-41 (2007)
Boehringer Ingelheim (Canada)
Aminopyrrolidineamide inhibitors of site-1 protease.EBI
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
J Med Chem 50: 3651-60 (2007)
Abbott Laboratories
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.EBI
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
J Med Chem 50: 3434-41 (2007)
Università
Synthesis and biological activities of isogranulatimide analogues.EBI
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
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
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
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
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
J Med Chem 50: 3596-603 (2007)
The University Of Iowa
Dual aromatase-steroid sulfatase inhibitors.BDB
J Med Chem 50: 3540-60 (2007)
University Of Bath
Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.EBI
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
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
J Med Chem 50: 3314-21 (2007)
Purdue University
SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.EBI
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
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
Bioorg Med Chem 15: 5811-8 (2007)
Cairo University
Benzo[b]thiophene-based histone deacetylase inhibitors.EBI
Bioorg Med Chem Lett 17: 4562-7 (2007)
Merck Research Laboratories
The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.BDB
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
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
Bioorg Med Chem Lett 17: 4495-9 (2007)
Kyorin Pharmaceutical
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.EBI
Bioorg Med Chem Lett 17: 4509-13 (2007)
Schering-Plough Research Institute
Inhibitors of anthrax lethal factor.EBI
Bioorg Med Chem Lett 17: 4575-8 (2007)
Purdue University
Aza analogues of equol: novel ligands for estrogen receptor beta.EBI
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 4538-44 (2007)
Pfizer
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.EBI
Bioorg Med Chem Lett 17: 4531-7 (2007)
Pfizer
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.EBI
Bioorg Med Chem Lett 17: 4450-5 (2007)
Glaxosmithkline
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.EBI
Eur J Med Chem 43: 166-73 (2008)
Sun Yat-Sen University
Enzymatic therapeutic index of acyclovir. Viral versus human polymerase gamma specificity.EBI
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
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
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
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
J Med Chem 50: 3256-66 (2007)
National Institute Of Mental Health
Enaminone amides as novel orally active GABAA receptor modulators.EBI
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
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
Bioorg Med Chem Lett 17: 3880-5 (2007)
Vernalis (R&D)
A novel arginine methyltransferase inhibitor with cellular activity.EBI
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
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
J Med Chem 50: 3388-91 (2007)
Research Triangle Institute
RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.EBI
Nature 447: 864-868 (2007)
Columbia University
Exploitation of structural and regulatory diversity in glutamate racemases.EBI
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
J Biol Chem 282: 25436-44 (2007)
Jacobus Pharmaceutical
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.BDB
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
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
Bioorg Med Chem Lett 17: 4527-30 (2007)
Southern Research Institute
Reversine increases the plasticity of lineage-committed mammalian cells.EBI
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
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
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
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
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
Bioorg Med Chem 15: 5519-28 (2007)
Gilead Sciences
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.EBI
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
Bioorg Med Chem Lett 17: 4599-603 (2007)
Pfizer
A chemometric study of the 5-HT(1A) receptor affinities presented by arylpiperazine compounds.EBI
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
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
Bioorg Med Chem 15: 5590-603 (2007)
Neurocrine Biosciences
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.BDB
Bioorg Med Chem 15: 5576-89 (2007)
Pfizer
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.EBI
Bioorg Med Chem Lett 17: 4670-7 (2007)
Glaxosmithkline
Design of a partial PPARdelta agonist.EBI
Bioorg Med Chem Lett 17: 4625-9 (2007)
Novo Nordisk
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.EBI
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
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
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
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
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
Bioorg Med Chem Lett 17: 4646-9 (2007)
Pharmacia
New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold.EBI
J Med Chem 50: 3397-401 (2007)
Vrije Universiteit Brussel
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.BDB
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
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
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
J Biol Chem 282: 23231-9 (2007)
Novartis
Design of novel histone deacetylase inhibitors.EBI
Bioorg Med Chem Lett 17: 4619-24 (2007)
Merck Research Laboratories
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.EBI
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
J Med Chem 50: 3159-62 (2007)
Ewha Womans University
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors.EBI
J Med Chem 50: 3274-82 (2007)
Purdue University
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.EBI
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
J Biol Chem 282: 23841-53 (2007)
University Of California
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors.EBI
Bioorg Med Chem Lett 17: 4271-4 (2007)
Sungkyunkwan University
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.EBI
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
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
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
J Med Chem 50: 3163-6 (2007)
University Of Michigan
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.BDB
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
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
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
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
Bioorg Med Chem 15: 5563-75 (2007)
Dipartimento Di Scienze Farmaceutiche
Extension of Drosophila melanogaster life span with a GPCR peptide inhibitor.EBI
Nat Chem Biol 3: 415-9 (2007)
California Institute Of Technology
Activation of inhibitors by sortase triggers irreversible modification of the active site.EBI
J Biol Chem 282: 23129-39 (2007)
University Of Chicago
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.EBI
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
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
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
Bioorg Med Chem 15: 5090-104 (2007)
Shimane University
Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development.EBI
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
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
Bioorg Med Chem Lett 17: 4308-15 (2007)
Abbott Laboratories
Primary amides as selective inhibitors of cathepsin K.EBI
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
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
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
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
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
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
Chem Biol Drug Des 69: 331-7 (2007)
Chemdiv
Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.BDB
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
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
J Med Chem 50: 3138-3142 (2007)
Universita Degli Studi
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.EBI
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
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
J Biol Chem 282: 20847-53 (2007)
Institute For Medical Research
Isolation of glycosidase-inhibiting hyacinthacines and related alkaloids from Scilla socialis.EBI
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
J Med Chem 50: 3101-12 (2007)
James Black Foundation
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitorsBDB
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
J Med Chem 50: 2931-41 (2007)
Pfizer
Small-molecule activators of RNase L with broad-spectrum antiviral activity.EBI
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
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
J Biol Chem 282: 20836-46 (2007)
Merck Research Laboratories
Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids.EBI
Bioorg Med Chem Lett 17: 4187-90 (2007)
Tranzyme Pharma
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.EBI
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
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
Bioorg Med Chem 15: 5177-90 (2007)
University Of Tokyo
Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.EBI
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
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
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 3814-8 (2007)
Berlex Biosciences
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.EBI
Bioorg Med Chem Lett 17: 4333-7 (2007)
Wyeth Research
Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents.EBI
Bioorg Med Chem Lett 17: 4338-42 (2007)
Yale University
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.EBI
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
Bioorg Med Chem Lett 17: 3925-9 (2007)
Shionogi
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.EBI
J Med Chem 50: 3086-100 (2007)
Abbott Laboratories
Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria.EBI
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
J Biol Chem 282: 23089-95 (2007)
Yale University
Alkyl-CoA disulfides as inhibitors and mechanistic probes for FabH enzymes.BDB
Chem Biol 14: 513-24 (2007)
Portland State University
Structure-activity relationships of semisynthetic mumbaistatin analogs.EBI
Bioorg Med Chem 15: 5207-18 (2007)
Stanford University
QSAR study of selective ligands for the thyroid hormone receptor beta.EBI
Bioorg Med Chem 15: 5251-61 (2007)
University Of Insubria
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.EBI
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
Bioorg Med Chem Lett 17: 3864-7 (2007)
Glaxosmithkline
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.EBI
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
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
J Med Chem 50: 2990-3003 (2007)
Abbott Laboratories
The biology and chemistry of hyperlipidemia.EBI
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
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
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
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
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
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
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
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
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
Bioorg Med Chem 15: 5262-74 (2007)
University Of Aarhus
Synthesis and evaluation of homo-bivalent GnRHR ligands.EBI
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
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
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
Bioorg Med Chem Lett 17: 3769-73 (2007)
Zhengzhou University
Inhibitory effect of 2-arylbenzofurans from Erythrina addisoniae on protein tyrosine phosphatase-1B.EBI
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
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
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
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
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 3630-5 (2007)
Pfizer
Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 3595-8 (2007)
Seoul National University
Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.EBI
Bioorg Med Chem Lett 17: 3652-6 (2007)
Adolor
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.EBI
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
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
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
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
J Med Chem 50: 2818-41 (2007)
Cardiome Pharma
Fawcettimine-related alkaloids from Lycopodium serratum.EBI
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
Antimicrob Agents Chemother 51: 2445-53 (2007)
Achillion Pharmaceuticals
Pyrophosphorolytic excision of nonobligate chain terminators by hepatitis C virus NS5B polymerase.EBI
Antimicrob Agents Chemother 51: 2920-8 (2007)
Mcgill University
Discovery of structurally diverse HIV-1 integrase inhibitors based on a chalcone pharmacophore.EBI
Bioorg Med Chem 15: 4985-5002 (2007)
University Of Southern California
Inhibition of IGF-1R and lipoxygenase by nordihydroguaiaretic acid (NDGA) analogs.EBI
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
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
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
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
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
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
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
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
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
J Med Chem 50: 2886-95 (2007)
Universit£
Novel heterocyclic thyromimetics. Part 2.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 3962-8 (2007)
Università
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.BDB
Bioorg Med Chem Lett 17: 3562-9 (2007)
Kalypsys
A new class of histamine H3 receptor antagonists derived from ligand based design.EBI
Bioorg Med Chem Lett 17: 3670-5 (2007)
F. Hoffmann-La Roche
The discovery of long acting beta2-adrenoreceptor agonists.EBI
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
Bioorg Med Chem Lett 17: 3624-9 (2007)
Pfizer
Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors.EBI
Bioorg Med Chem Lett 17: 3957-61 (2007)
University Of Tokyo
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.EBI
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
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
J Med Chem 50: 2753-66 (2007)
Kobe Gakuin University
Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides.EBI
J Nat Prod 70: 1010-5 (2007)
Department Of Chemistry And Applied Biosciences
Diarylquinolines target subunit c of mycobacterial ATP synthase.EBI
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
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
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
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
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
Bioorg Med Chem Lett 17: 3618-23 (2007)
Abbott Laboratories
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.EBI
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
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
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
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
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
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
J Med Chem 50: 2622-39 (2007)
Burnham Institute For Medical Research
Sodium channel blockers.EBI
J Med Chem 50: 2583-8 (2007)
Purdue Pharma
Kv7 (KCNQ) channel modulators and neuropathic pain.EBI
J Med Chem 50: 2576-82 (2007)
Neurosearch
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.EBI
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
J Med Chem 50: 2589-96 (2007)
Glaxosmithkline
Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium.EBI
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
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
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
Antimicrob Agents Chemother 51: 2552-8 (2007)
Institute Of Science
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.EBI
Antimicrob Agents Chemother 51: 2403-11 (2007)
University Of California
RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.EBI
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
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
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
Proc Natl Acad Sci U S A 104: 8520-5 (2007)
Abbott Laboratories
3D-QSAR studies on malonyl coenzyme A decarboxylase inhibitors.EBI
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
Bioorg Med Chem Lett 17: 4044-8 (2007)
Abbott Laboratories
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI
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
Bioorg Med Chem Lett 17: 4053-6 (2007)
Wyeth Research
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.EBI
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
Bioorg Med Chem Lett 17: 3575-80 (2007)
Pfizer
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.EBI
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
Bioorg Med Chem Lett 17: 3636-41 (2007)
Merck Research Laboratories
Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.EBI
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
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
Bioorg Med Chem 15: 4643-50 (2007)
Università
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.EBI
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
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
J Nat Prod 70: 795-801 (2007)
Chiang Mai University
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).BDB
J Med Chem 50: 2647-54 (2007)
Pfizer
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors.BDB
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
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
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
J Med Chem 50: 2597-600 (2007)
Glaxosmithkline
Carbonic anhydrases as targets for medicinal chemistry.EBI
Bioorg Med Chem 15: 4336-50 (2007)
Universit£
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.EBI
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
Bioorg Med Chem Lett 17: 3696-701 (2007)
Universit£
Plant P5C reductase as a new target for aminomethylenebisphosphonates.EBI
J Agric Food Chem 55: 4340-7 (2007)
University Of Ferrara
Isoform-selective inhibition of the human UDP-glucuronosyltransferase 2B7 by isolongifolol derivatives.EBI
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
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
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
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
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
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
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
J Med Chem 50: 2732-6 (2007)
Almirall
2D QSAR studies on thyroid hormone receptor ligands.EBI
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
Bioorg Med Chem Lett 17: 3354-61 (2007)
Merck Research Laboratories
Discovery of new C3aR ligands. Part 1: arginine derivatives.EBI
Bioorg Med Chem Lett 17: 3258-61 (2007)
Ucb Pharma
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.EBI
Bioorg Med Chem Lett 17: 3736-40 (2007)
Ajinomoto
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.EBI
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
J Mol Biol 369: 829-40 (2007)
Imperial College
A fragment-based approach for the discovery of isoform-specific p38alpha inhibitors.BDB
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
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
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
Bioorg Med Chem Lett 17: 3322-9 (2007)
Curacyte Discovery
Benzopyran sulfonamides as KV1.5 potassium channel blockers.EBI
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
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
J Med Chem 50: 2640-6 (2007)
Johann Wolfgang Goethe-UniversitäT
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.EBI
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
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
Bioorg Med Chem Lett 17: 3778-83 (2007)
Schering-Plough Research Institute
Novel inhibitors of fatty acid amide hydrolase.BDB
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
Bioorg Med Chem Lett 17: 3463-7 (2007)
Ucb Pharma
Discovery of new C3aR ligands. Part 2: amino-piperidine derivatives.EBI
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
Eur J Med Chem 43: 43-52 (2008)
Yantai University
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.EBI
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-ResiBDB
J Med Chem 50: 2370-84 (2007)
Bar-Ilan University
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.EBI
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
J Med Chem 50: 2520-6 (2007)
Merck Research Laboratories
Nicotinic acid receptor agonists differentially activate downstream effectors.EBI
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
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
Eur J Med Chem 43: 81-92 (2008)
Jadavpur University
Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.EBI
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
Bioorg Med Chem 15: 4256-64 (2007)
Aureus Pharma
Synthesis and glycogen phosphorylase inhibitor activity of 2,3-dihydrobenzo[1,4]dioxin derivatives.EBI
Bioorg Med Chem 15: 4048-56 (2007)
University Of Debrecen
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.EBI
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
J Nat Prod 70: 872-5 (2007)
Griffith University
Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.BDB
J Med Chem 50: 2289-92 (2007)
Astex
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.BDB
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
Bioorg Med Chem Lett 17: 3729-32 (2007)
Harvard Medical School
Squalene-derived flexible linkers for bioactive peptides.EBI
Bioorg Med Chem Lett 17: 3310-3 (2007)
University Of Arizona
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.EBI
Bioorg Med Chem Lett 17: 3754-9 (2007)
Cerep
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.EBI
Bioorg Med Chem Lett 17: 3339-43 (2007)
Amgen
Bridged androstenediol analogs as ER-beta selective SERMs.EBI
Bioorg Med Chem Lett 17: 2944-8 (2007)
Merck Research Laboratories
Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.EBI
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
Eur J Med Chem 42: 1317-24 (2007)
Technische UniversitÄT Braunschweig
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.EBI
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
J Med Chem 50: 2742-6 (2007)
University Of Turku
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.EBI
J Med Chem 50: 2497-505 (2007)
Universidade De Vigo
Enhanced substituted resorcinol hydrophobicity augments tyrosinase inhibition potency.EBI
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
J Med Chem 50: 2385-90 (2007)
University Of California San Francisco
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.BDB
J Med Chem 50: 2341-51 (2007)
Pfizer
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.EBI
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
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
Bioorg Med Chem Lett 17: 3367-72 (2007)
Tanabe Research Laboratories
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 3335-8 (2007)
Institute Of Biotechnology
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.EBI
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
Chem Biol Drug Des 69: 204-11 (2007)
Shanghai Jiao Tong University
Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases.BDB
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
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
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
Antimicrob Agents Chemother 51: 2028-34 (2007)
Glsynthesis
Biochemical characterization of PER-2 and genetic environment of blaPER-2.EBI
Antimicrob Agents Chemother 51: 2359-65 (2007)
Universidad De Buenos Aires
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.EBI
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
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
Bioorg Med Chem Lett 17: 3435-9 (2007)
Daiichi Asubio Pharma
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.EBI
Bioorg Med Chem Lett 17: 3378-83 (2007)
Pfizer
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.EBI
Bioorg Med Chem Lett 17: 3388-91 (2007)
Abbott Laboratories
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).EBI
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
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
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
Bioorg Med Chem Lett 17: 3349-53 (2007)
Pfizer
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).EBI
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
Bioorg Med Chem 15: 4077-84 (2007)
Astrazeneca
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.EBI
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
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
Bioorg Med Chem Lett 17: 3384-7 (2007)
Merck Research Laboratories
Synthesis and biological activity of imidazopyridine anticoccidial agents: part I.EBI
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
J Med Chem 50: 2399-407 (2007)
Purdue University
Target-based approach to inhibitors of histone arginine methyltransferases.EBI
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
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
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
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
Bioorg Med Chem 15: 4247-55 (2007)
Zhengzhou University
Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin.EBI
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
Bioorg Med Chem Lett 17: 3023-7 (2007)
Schering-Plough Research Institute
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.EBI
Bioorg Med Chem Lett 17: 3006-9 (2007)
Merck
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.EBI
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
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
J Med Chem 50: 2264-8 (2007)
Bayer Pharmaceuticals
Virtual screening for novel openers of pancreatic K(ATP) channels.EBI
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
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
J Med Chem 50: 2011-29 (2007)
Abbott Laboratories
Serum differentially alters the antifungal properties of echinocandin drugs.EBI
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
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
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
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
Bioorg Med Chem Lett 17: 2927-30 (2007)
Glaxosmithkline
Synthesis of bridged piperazines with sigma receptor affinity.EBI
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
J Med Chem 50: 2003-6 (2007)
Virginia Tech
Novel aminoethylbiphenyls as 5-HT7 receptor ligands.EBI
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 3130-5 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques.EBI
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
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
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
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
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
Bioorg Med Chem 15: 3649-60 (2007)
Janssen-Cilag
PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).EBI
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
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
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
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
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
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
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
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
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
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
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
Bioorg Med Chem 15: 3684-91 (2007)
Texas A&M University
Polyphenols based on isoflavones as inhibitors of Helicobacter pylori urease.EBI
Bioorg Med Chem 15: 3703-10 (2007)
Nanjing University
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.EBI
Bioorg Med Chem Lett 17: 3048-52 (2007)
Kyoto Pharmaceutical University
PDE-10A inhibitors as insulin secretagogues.EBI
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
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
Bioorg Med Chem 15: 3854-68 (2007)
Université
Structure based de novo design of novel glycogen synthase kinase 3 inhibitors.EBI
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
Bioorg Med Chem 15: 3748-55 (2007)
Universit£
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors.EBI
Bioorg Med Chem 15: 3783-800 (2007)
Pfizer
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.EBI
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
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
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
Bioorg Med Chem Lett 17: 3077-80 (2007)
Ucb Pharma
Cellular characterization of a novel focal adhesion kinase inhibitor.EBI
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
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
Bioorg Med Chem 15: 3883-8 (2007)
Kyushu University
Small molecule antagonists of the CC chemokine receptor 4 (CCR4).EBI
Bioorg Med Chem Lett 17: 3141-5 (2007)
Millennium Pharmaceuticals
4-substituted indazoles as new inhibitors of neuronal nitric oxide synthase.EBI
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
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
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
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
Proteins 67: 981-90 (2007)
University College London
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.EBI
Bioorg Med Chem 15: 3368-72 (2007)
University Of Chile
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.BDB
Bioorg Med Chem 15: 3321-33 (2007)
Wyeth Research
Discovery of a novel small molecule binding site of human survivin.EBI
Bioorg Med Chem Lett 17: 3122-9 (2007)
Abbott Laboratories
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.EBI
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
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
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
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
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
J Med Chem 50: 1993-7 (2007)
The New York School Of Medicine
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.EBI
Bioorg Med Chem Lett 17: 3208-11 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.EBI
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
Bioorg Med Chem Lett 17: 2706-11 (2007)
Bayer Healthcare
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.BDB
Bioorg Med Chem Lett 17: 2899-903 (2007)
Gnf
Neuroprotective principles from Gastrodia elata.EBI
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
J Med Chem 50: 1850-64 (2007)
University Of Alberta
Synthesis and SAR studies of a novel class of S1P1 receptor antagonists.EBI
Bioorg Med Chem 15: 3548-64 (2007)
Sankyo
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.EBI
Bioorg Med Chem 15: 3450-6 (2007)
Institute Of Biological Chemistry And The Genomics Research Center
Design of potent PPARalpha agonists.EBI
Bioorg Med Chem Lett 17: 3198-202 (2007)
Novo Nordisk
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.EBI
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
Bioorg Med Chem Lett 17: 3212-6 (2007)
Université
Fluorinated NSC as a Cdc25 inhibitor.EBI
Bioorg Med Chem Lett 17: 2351-4 (2007)
Sejong University
Covalent reactions of wortmannin under physiological conditions.BDB
Chem Biol 14: 321-8 (2007)
Massachusetts General Hospital
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.EBI
J Nat Prod 70: 859-62 (2007)
Tahitian Noni International
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.BDB
J Med Chem 50: 1876-85 (2007)
St. Jude Research Hospital
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.EBI
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
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
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
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
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
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
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
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
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
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
J Med Chem 50: 1865-75 (2007)
Universit£
Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens.EBI
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
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
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
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
J Biol Chem 282: 15799-811 (2007)
University Of Copenhagen
Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives.EBI
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-pyrrEBI
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
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
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
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
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
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
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
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
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
Bioorg Med Chem Lett 17: 2355-60 (2007)
The Scripps Research Institute
Development of integrase inhibitors for treatment of AIDS: an overview.EBI
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
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
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
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
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
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.