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Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1575-86 (2004)
Pfizer
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1547-52 (2004)
Purdue Pharma
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1536-46 (2004)
Uppsala University
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1514-26 (2004)
University of Arizona
New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1475-86 (2004)
Harvard Medical School
Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1448-64 (2004)
Universit£
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1434-47 (2004)
Universit£
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1400-12 (2004)
Southern Research Institute
Structure-based optimization of novel azepane derivatives as PKB inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 1375-90 (2004)
Roche Diagnostics
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1351-9 (2004)
Sapienza University of Rome
Design and synthesis of new templates derived from pyrrolopyrimidine as selective multidrug-resistance-associated protein inhibitors in multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1339-50 (2004)
Xenova
Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1329-38 (2004)
Xenova
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 1325-8 (2004)
Morphochem
Synthesis of a potent transition-state inhibitor of 5'-deoxy-5'-methylthioadenosine phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1322-4 (2004)
Biocryst Pharmaceuticals
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1319-21 (2004)
Glaxosmithkline
A non-peptide NK1 receptor agonist showing subpicomolar affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1315-8 (2004)
Università
Selective optimization of side activities: another way for drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1303-14 (2004)
Prestwick Chemical
Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cancer Res 64: 1802-10 (2004)
The University of Birmingham
Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 101: 3569-74 (2004)
Tohoku University
FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 310: 326-33 (2004)
University of Arizona
Biologically active compounds from Aphyllophorales (polypore) fungi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 67: 300-10 (2004)
The University of Mississippi
In vitro characterization of 5-carboxyl-2,4-di-benzamidobenzoic acid (NS3763), a noncompetitive antagonist of GLUK5 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 309: 1003-10 (2004)
Neurosearch
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Med 10: 262-7 (2004)
Vertex Pharmaceuticals
Design and synthesis of novel small molecule N/OFQ receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1347-51 (2004)
Purdue Pharma
A series of heterocyclic inhibitors of phenylalanyl-tRNA synthetases with antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1343-6 (2004)
Cubist Pharmaceuticals
A series of spirocyclic analogues as potent inhibitors of bacterial phenylalanyl-tRNA synthetases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1339-42 (2004)
Cubist Pharmaceuticals
Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1333-7 (2004)
Liaoning Normal University
Orally active PDE4 inhibitors with therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1323-7 (2004)
Minase Research Institute
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1317-21 (2004)
Merck Research Laboratories
Penicillin-derived inhibitors that simultaneously target both metallo- and serine-beta-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1299-304 (2004)
Southern Methodist University
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the alpha 2 delta subunit of voltage gated calcium channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1295-8 (2004)
Merck Research Laboratories
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1291-4 (2004)
Schering-Plough Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1269-72 (2004)
Maxim Pharmaceuticals
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1265-8 (2004)
Merck Research Laboratories
Novel non-peptidic neuropeptide Y Y2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1239-42 (2004)
Johnson & Johnson Pharmaceutical Research and Development
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1229-34 (2004)
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1221-7 (2004)
Millennium Pharmaceuticals
Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1213-6 (2004)
Pfizer
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1205-7 (2004)
Nci-Frederick
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1201-3 (2004)
Merck Frosst Centre For Therapeutic Research
Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1197-200 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel quinazoline-quinoline alkaloids with cytotoxic and DNA topoisomerase II inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1193-6 (2004)
Toho University
A novel class of apical sodium-dependent bile acid transporter inhibitors: the amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1183-6 (2004)
Sankyo
Potent imidazole and triazole CB1 receptor antagonists related to SR141716.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1151-4 (2004)
Neurocrine Biosciences
New heteroarylbenzenesulphonamides as matrix metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 1119-21 (2004)
Universit£
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Sci 94: 197-202 (2004)
Kyorin University
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 309: 903-20 (2004)
Institut De Recherches Servier
Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 1272-9 (2004)
Universita Degli Studi Di Firenze
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1259-71 (2004)
Neurocrine Biosciences
Chemical and functional identification and characterization of novel sulfated alpha-conotoxins from the cone snail Conus anemone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1234-41 (2004)
The University of Queensland
Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1207-13 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1193-206 (2004)
University of Colorado
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1175-82 (2004)
Glaxosmithkline
Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1153-60 (2004)
University of Leipzig
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1122-35 (2004)
Emory University
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1098-109 (2004)
Sapienza University of Rome
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1085-97 (2004)
Abbott Laboratories
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1081-4 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1075-8 (2004)
Central Pharmaceutical Research Institute
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Structure 12: 215-26 (2004)
University of Dundee
Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 279: 18727-32 (2004)
Vertex Pharmaceuticals
Importance of phenolic address groups in opioid kappa receptor selective antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1070-3 (2004)
Research Triangle Institute
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1060-9 (2004)
University of Tromsø
Inhibition of adenosine deaminase by novel 5:7 fused heterocycles containing the imidazo[4,5-e][1,2,4]triazepine ring system: a structure-activity relationship study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1044-50 (2004)
University of Maryland
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1031-43 (2004)
University of Bonn
Prediction of ligand binding affinity and orientation of xenoestrogens to the estrogen receptor by molecular dynamics simulations and the linear interaction energy method.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 1018-30 (2004)
Vrije Universiteit Amsterdam
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 993-8 (2004)
University of Tennessee At Memphis
Synthesis, SAR, crystal structure, and biological evaluation of benzoquinoliziniums as activators of wild-type and mutant cystic fibrosis transmembrane conductance regulator channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 962-72 (2004)
Université
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 935-46 (2004)
University of Athens
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 928-34 (2004)
Sapienza University of Rome
Effects of C2-alkylation, N-alkylation, and N,N'-dialkylation on the stability and estrogen receptor interaction of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 915-27 (2004)
Free University of Berlin
Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 907-14 (2004)
Astrazeneca R&D
5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 900-6 (2004)
Pfizer
Recognition of privileged structures by G-protein coupled receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 888-99 (2004)
Novo Nordisk
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 871-87 (2004)
Astrazeneca
A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 859-70 (2004)
Uppsala University
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 792-804 (2004)
Amorepacific R&D Center
Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 788-91 (2004)
National Cancer Institute-Frederick
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 769-87 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and SAR exploration of dinapsoline analogues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 12: 715-34 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Imaging reversal of multidrug resistance in living mice with bioluminescence: MDR1 P-glycoprotein transports coelenterazine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 101: 1702-7 (2004)
Washington University
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biol Psychiatry 55: 320-2 (2004)
Emory University
Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 817-21 (2004)
F. Hoffmann-La Roche
3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 813-6 (2004)
Glaxosmithkline
The design and synthesis of sulfonamides as caspase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 809-12 (2004)
Pfizer
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 805-8 (2004)
Merck Frosst Canada
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 797-800 (2004)
Shire Biochem
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 793-6 (2004)
Shire Biochem
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 787-91 (2004)
Seoul National University
Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 783-6 (2004)
Bayer Research Center
Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 779-82 (2004)
Kyoto University
Bile acid amides derived from chiral amino alcohols: novel antimicrobials and antifungals.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 773-7 (2004)
National Chemical Laboratory (Csir-Ncl)
Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 767-71 (2004)
Institut De Recherches Servier
Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 761-5 (2004)
Berlex Biosciences
Benzene-di-N-octylcarbamates as conformationally constrained phospholipase A(2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 751-5 (2004)
National Chung-Hsing University
Fluorinated dihydroquinolines as potent n-NOS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 743-6 (2004)
Schering
Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 739-42 (2004)
Boehringer Ingelheim (Canada)
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 727-9 (2004)
Nps Pharmaceuticals
Design of small molecule ketoamide-based inhibitors of cathepsin K.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 719-22 (2004)
Glaxosmithkline
Inhibition of alpha-chymotrypsin with thiol-bearing substrate analogues in the presence of zinc ion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 701-5 (2004)
Pohang University of Science and Technology
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 689-93 (2004)
Abbott Laboratories
Peptidyl aldehydes as slow-binding inhibitors of dual-specificity phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 685-7 (2004)
The Ohio State University
2-hydroxy-4-isopropylbenzaldehyde, a potent partial tyrosinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 681-3 (2004)
University of California
Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 677-80 (2004)
Merck Sharp & Dohme Research Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 673-6 (2004)
Abbott Laboratories
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 667-71 (2004)
Drexel University College of Medicine
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 657-61 (2004)
Nerviano
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 639-43 (2004)
Merck Research Laboratories
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 605-9 (2004)
Kingston University
Rational design and synthesis of selective BACE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 601-4 (2004)
Merck Research Laboratories
Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 597-9 (2004)
Universidad De Navarra
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 591-6 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 585-9 (2004)
Universidad De Santiago De Compostela
Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 571-3 (2004)
University of California Los Angeles
Plakolide A, a new gamma-lactone from the marine sponge Plakortis sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 67: 110-1 (2004)
Harbor Branch Oceanographic Institution
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 744-55 (2004)
Eli Lilly
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 735-43 (2004)
Biological Research Center of The Hungarian Academy of Sciences
4-[5-Fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]phenyl]-3,4,5,6- tetrahydro-2H-pyran-4-carboxamide, an orally active inhibitor of 5-lipoxygenase with improved pharmacokinetic and toxicology characteristics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 720-5 (2004)
Pfizer
Potent and selective conformationally restricted neuronal nitric oxide synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 703-10 (2004)
Northwestern University
Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 673-80 (2004)
National Center For Genetic Engineering and Biotechnology At Thailand
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 663-72 (2004)
Leiden University
Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 656-62 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 644-55 (2004)
National Cancer Institute-Frederick
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 627-43 (2004)
Solvay Pharma
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 612-26 (2004)
Globe Pharmaceutical R and Abbott Laboratories
Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 600-11 (2004)
University of Illinois
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 588-99 (2004)
Glaxosmithkline
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 550-7 (2004)
University of Marburg
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 530-49 (2004)
Ucb Pharma
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 519-29 (2004)
Astrazeneca Pharmaceuticals
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 497-508 (2004)
Florida A and M University
Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 369: 151-9 (2004)
UniversitÄT WÜRzburg
In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 483: 301-8 (2004)
University of Innsbruck
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 309: 404-13 (2004)
Johnson & Johnson Pharmaceutical
Structural basis for dipeptide amide isoform-selective inhibition of neuronal nitric oxide synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Struct Mol Biol 11: 54-9 (2004)
University of California Irvine
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 309: 348-55 (2004)
Wyeth Research
Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 467-74 (2004)
The Ohio State University
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 456-66 (2004)
Eli Lilly
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 446-55 (2004)
University of Maryland
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 432-45 (2004)
Yale University
Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 400-10 (2004)
Novo Nordisk
Application of CoMFA and CoMSIA 3D-QSAR and docking studies in optimization of mercaptobenzenesulfonamides as HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 385-99 (2004)
University of Southern California
Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 345-54 (2004)
National Center For Genetic Engineering and Biotechnology At Thailand
Evaluation of P1'-diversified phosphinic peptides leads to the development of highly selective inhibitors of MMP-11.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 325-36 (2004)
University of Athens
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 303-24 (2004)
Abbott Laboratories
Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 296-302 (2004)
Research Triangle Institute
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 281-4 (2004)
Research Triangle Institute
Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 483: 37-43 (2004)
Yamanouchi Pharmaceutical
A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 126: 34-5 (2004)
Fujisawa Pharmaceutical
Thermodynamics of the molecular and chiral recognition of cycloalkanols and camphor by modified beta-cyclodextrins possessing simple aromatic tethers.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Org Chem 69: 173-80 (2004)
Nankai University
Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 10: 1183-93 (2003)
UniversitÀ
New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 549-52 (2003)
Cv Therapeutics
2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 545-8 (2003)
Pharmacopeia
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 535-9 (2003)
Cv Therapeutics
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 531-4 (2003)
Johnson & Johnson Pharmaceutical Research and Development
Binding of an imidazopyridoindole at imidazoline I2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 527-9 (2003)
Virginia Commonwealth University
3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 523-6 (2003)
Virginia Commonwealth University
Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 515-8 (2003)
Wyeth Research
Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 499-504 (2003)
Discovery Research-Dr. Reddy'S Laboratories
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 491-3 (2003)
Instituto De QuíMica MéDica
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 449-53 (2003)
The Scripps Research Institute
1,2-Diaryl-1-ethanone and pyrazolo [4,3-c] quinoline-4-one as novel selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 445-8 (2003)
Dr. Reddy'S Laboratories
Effects of fluorine substitution of cytosine analogues on the binding affinity to HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 437-40 (2003)
The University of Georgia
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 413-6 (2004)
Technische Universitat Braunschweig
A novel series of potent and selective IKK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 409-12 (2003)
Celltech R&D
N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 405-8 (2003)
Astrazeneca
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 397-400 (2004)
Abbott Laboratories
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 383-7 (2003)
Pharmaceutical Research Institute
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 377-81 (2003)
Amgen
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 369-72 (2003)
University of Paris
A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 357-60 (2003)
Novartis Institute For Biomedical Research
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 351-5 (2004)
Merck Research Laboratories
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 343-6 (2004)
Bristol-Myers Squibb
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 337-41 (2003)
Bruker-Axs
Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 333-6 (2003)
Taisho Pharmaceutical
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 325-8 (2003)
Ribotargets
Parallel solid-phase synthesis of disubstituted (5-biphenyltetrazolyl) hydantoins and thiohydantoins targeting the growth hormone secretagogue receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 317-20 (2003)
Novo Nordisk
4,5-Disubstituted-1,3-oxazolidin-2-imine derivatives: a new class of orally bioavailable nitric oxide synthase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 313-6 (2003)
Dainippon Pharmaceutical
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 309-12 (2003)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 262-72 (2003)
Universita Degli Studi Di Firenze
Cyclodextrin-derived diorganyl tellurides as glutathione peroxidase mimics and inhibitors of thioredoxin reductase and cancer cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 233-9 (2004)
Uppsala University
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 196-209 (2003)
Johnson and Johnson Pharmaceutical Research and Development
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 175-87 (2003)
University of Illinois At Urbana-Champaign
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 165-74 (2003)
Harvard Medical School
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 158-64 (2004)
Elan Pharmaceuticals
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 143-57 (2003)
Universit£
NMR structural characterization of peptide inhibitors bound to the Hepatitis C virus NS3 protease: design of a new P2 substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 123-32 (2003)
Boehringer Ingelheim (Canada)
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 110-22 (2004)
Uppsala University
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 101-9 (2003)
Central Pharmaceutical Research Institute
Design, synthesis, molecular modeling studies, and calpain inhibitory activity of novel alpha-ketoamides incorporating polar residues at the P1'-position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 72-9 (2003)
University of Tennessee Health Science Center
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 37-44 (2004)
University of Queensland
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 47: 22-36 (2004)
Universitat Hamburg
Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 18-21 (2003)
Boehringer Ingelheim (Canada)
Discovery of alpha,gamma-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 14-7 (2003)
Italy. Vinc
Self-association of okadaic acid upon complexation with potassium ion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 47: 10-3 (2003)
Instituto Universitario De Bio-Organica Antonio Gonzalez
Isolation and structure elucidation of Sch 642305, a novel bacterial DNA primase inhibitor produced by Penicillium verrucosum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1527-30 (2003)
Schering-Plough Research Institute
Secondary mutations M36I and A71V in the human immunodeficiency virus type 1 protease can provide an advantage for the emergence of the primary mutation D30N.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 42: 15029-35 (2003)
University of Florida College of Medicine
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 283-7 (2003)
Methylgene
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 275-8 (2003)
Glaxosmithkline
Synthesis and nicotinic receptor activity of a hydroxylated tropane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 271-3 (2003)
University of Wollongong
Structure-activity relationships of novel potent MurF inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 267-70 (2003)
Abbott Laboratories
Novel P4 truncated tripeptidyl alpha-ketoamides as HCV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 263-6 (2003)
Eli Lilly
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 257-61 (2003)
Eli Lilly
Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 251-6 (2003)
Eli Lilly
P3 cap modified Phe*-Ala series BACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 245-50 (2003)
Eli Lilly
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 239-43 (2003)
Eli Lilly
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 231-4 (2003)
Universit£
Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 225-9 (2003)
University of Montpellier
Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 217-23 (2003)
Universit£
Novel targeting strategy based on multimeric ligands for drug delivery and molecular imaging: homooligomers of alpha-MSH.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 211-5 (2003)
University of Arizona
Highly potent PDE4 inhibitors with therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 207-10 (2004)
Minase Research Institute
Inactivation of gamma-aminobutyric acid aminotransferase by (S)-4-amino-4,5-dihydro-2-furancarboxylic acid does not proceed by the expected aromatization mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 203-6 (2003)
Northwestern University
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 195-202 (2003)
Wake Forest University School of Medicine
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 187-90 (2003)
Sugen
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 181-5 (2003)
Sri International
Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 177-80 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 167-70 (2003)
Eli Lilly
The difluoromethylene group as a replacement for the labile oxygen in steroid sulfates: a new approach to steroid sulfatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 151-5 (2003)
University of Waterloo
An electrochemical device for the assay of the interaction between a dioxin receptor and its various ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 137-41 (2003)
Kyushu University
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 119-24 (2003)
Boehringer Ingelheim (Canada)
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 14: 111-4 (2004)
Glaxosmithkline
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 95-8 (2003)
Pfizer
Investigation of novel fumagillin analogues as angiogenesis inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 91-4 (2003)
Gilead Sciences
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 87-90 (2003)
Amgen
The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 81-5 (2003)
Inotek Pharmaceuticals
Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 77-9 (2003)
The Ohio State University
Novel O-glycosyl amino acid mimetics as building blocks for O-glycopeptides act as inhibitors of galactosidases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 73-5 (2003)
University of Hamburg
A facile synthesis of 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, a selective 15-lipoxygenase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 63-5 (2003)
Tamkang University
Peptide deformylase inhibitors with activity against respiratory tract pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 59-62 (2003)
British Biotech Pharmaceuticals
Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 55-8 (2003)
4Sc
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 47-50 (2003)
Chinese Academy of Sciences
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 43-6 (2003)
Merck
Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 37-41 (2003)
Wyeth Research
New orally active PDE4 inhibitors with therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 29-32 (2004)
Minase Research Institute
Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 14: 21-4 (2003)
Pfizer
Characterization of uremic toxin transport by organic anion transporters in the kidney.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kidney Int 65: 162-74 (2004)
University of Tokyo
2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5834-43 (2003)
The Danish University of Pharmaceutical Sciences
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5812-24 (2003)
Vrije Universiteit Amsterdam
Generation of bis-cationic heterocyclic inhibitors of Bacillus subtilis HPr kinase/phosphatase from a ditopic dynamic combinatorial library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5803-11 (2003)
Isis-Universit£
Novel lavendamycin analogues as potent HIV-reverse transcriptase inhibitors: synthesis and evaluation of anti-reverse transcriptase activity of amide and ester analogues of lavendamycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5773-80 (2003)
Ball State University
Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5752-62 (2003)
Technische UniversitäT MüNchen
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5745-51 (2003)
In2Gen
Parallel solid-phase synthesis and evaluation of inhibitors of Streptomyces coelicolor type II dehydroquinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5735-44 (2003)
Universidad De Santiago De Compostela
Three-dimensional quantitative structure-activity relationship analyses of peptide substrates of the mammalian H+/peptide cotransporter PEPT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5725-34 (2003)
Martin-Luther-University Halle-Wittenberg
Computer modeling of selective regions in the active site of nitric oxide synthases: implication for the design of isoform-selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5700-11 (2003)
Northwestern University
Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5691-9 (2003)
Yale University
Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5663-73 (2003)
Quorex Pharmaceuticals
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5651-62 (2003)
Leo Pharma
Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5638-50 (2003)
Universidad Complutense
Rational design of an indolebutanoic acid derivative as a novel aldose reductase inhibitor based on docking and 3D QSAR studies of phenethylamine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5619-27 (2003)
Yonsei University
Novel sst(4)-selective somatostatin (SRIF) agonists. 4. Three-dimensional consensus structure by NMR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5606-18 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5597-605 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5587-96 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5579-86 (2003)
Salk Institute
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5567-70 (2003)
University of Wisconsin-Milwaukee
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 482: 335-7 (2003)
Virginia Commonwealth University
Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase D.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 1342-8 (2003)
University of Pittsburgh
Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 1295-308 (2003)
Glaxosmithkline
Characterization of human alpha 4 beta 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 1283-94 (2003)
Barrow Neurological Institute
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Int J Biochem Cell Biol 36: 247-57 (2004)
National University of Singapore
Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4505-9 (2003)
University of Florida
Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4501-4 (2003)
Wyeth Research
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4497-9 (2003)
Banyu Tsukuba Research Institute
Novel mechanism of inhibiting beta-lactamases by sulfonylation using beta-sultams.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4489-92 (2003)
The University of Huddersfield
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4477-80 (2003)
Eli Lilly
Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4467-71 (2003)
Johnson & Johnson Pharmaceutical Research & Development
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4459-62 (2003)
Adolor
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4431-5 (2003)
Merck Research Laboratories
Binding of beta-carbolines at 5-HT(2) serotonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4421-5 (2003)
Virginia Commonwealth University
Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4415-9 (2003)
Centre De Recherche De Paris
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4409-13 (2003)
Nps Pharmaceuticals
Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4405-8 (2003)
Università
Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4389-93 (2003)
Seoul National University
Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4385-8 (2003)
Merck Research Laboratories
Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4381-4 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D-QSAR studies on natural acetylcholinesterase inhibitors of Sarcococca saligna by comparative molecular field analysis (CoMFA).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4375-80 (2003)
University of Innsbruck
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4365-9 (2003)
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4361-4 (2003)
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4355-9 (2003)
Biogen
beta-alanine dipeptides as MC4R agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4341-4 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of statine-containing BACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4335-9 (2003)
Eli Lilly
Catechol-substituted L-chicoric acid analogues as HIV integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4331-4 (2003)
Institute of Science & Technology
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4321-6 (2003)
Nagoya City University
6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4313-6 (2003)
Novartis Forschungsinstitut
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4299-304 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4293-7 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Lysine sulfonamides as novel HIV-protease inhibitors: optimization of the Nepsilon-acyl-phenyl spacer.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 4289-92 (2003)
Pharmacor
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4285-8 (2003)
Merck Research Laboratories
B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4281-4 (2003)
Eli Lilly
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4277-9 (2003)
Fujisawa Pharmaceutical
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4273-6 (2003)
Kyoto Pharmaceutical University
Muscarinic mechanisms of antipsychotic atypicality.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Prog Neuropsychopharmacol Biol Psychiatry 27: 1125-43 (2003)
Eli Lilly
Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5546-51 (2003)
Mcgill University Health Center/Royal Victoria Hospital
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5512-32 (2003)
Faes Farma
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5505-11 (2003)
University of Bath
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5484-504 (2003)
Nitromed
Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5471-7 (2003)
University of Montpellier
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5445-57 (2003)
Vrije Universiteit
Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5416-27 (2003)
Taisho Pharmaceutical
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5375-88 (2003)
Cephalon
Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5365-74 (2003)
State University of Groningen
Application of the lambda-dynamics method to evaluate the relative binding free energies of inhibitors to HCV protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5360-4 (2003)
Schering-Plough Research Institute
Molecular model of the alpha(IIb)beta(3) integrin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5316-25 (2003)
Merck Research Laboratories
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5298-315 (2003)
Pharmaceutical Research Institute
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5294-7 (2003)
Merck Research Laboratories
Design, synthesis, and biological activity of a difluoro-substituted, conformationally rigid vigabatrin analogue as a potent gamma-aminobutyric acid aminotransferase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5292-3 (2003)
Northwestern University
A new acylated oleanane triterpenoid from Couepia polyandra that inhibits the lyase activity of DNA polymerase beta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1463-5 (2003)
Virginia Polytechnic Institute and State University
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cancer Res 63: 7861-9 (2003)
Abbott Laboratories
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4229-33 (2003)
Morphochem
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 4217-21 (2003)
Gsk
Novel oxazolidinone-quinolone hybrid antimicrobials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4213-6 (2003)
Vicuron Pharmaceuticals
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4205-8 (2003)
Daiichi Pharmaceutical
Semi-synthetic glycopeptide antibacterials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4165-8 (2003)
Theravance
Multidrug resistance to HIV-1 protease inhibition requires cooperative coupling between distal mutations.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 42: 13659-66 (2003)
The Johns Hopkins University
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5271-6 (2003)
Industrial Research
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5258-70 (2003)
University of Colorado
5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5249-57 (2003)
Abbott Laboratories
Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5208-21 (2003)
Instituto Biomar
Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5196-207 (2003)
Universidad Aut£Noma De Madrid
Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 5184-95 (2003)
Aventis Pharma
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5171-83 (2003)
University of Illinois At Urbana-Champaign
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5162-70 (2003)
Harvard Medical School
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5139-52 (2003)
Forbes Norris Als/Mda Research Center
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5121-4 (2003)
Eli Lilly
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5117-20 (2003)
Glaxosmithkline R&D
Rapid diversity-oriented synthesis in microtiter plates for in situ screening of HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 4: 1246-8 (2003)
The Scripps Research Institute
Two antiviral compounds from the plant Stylogne cauliflora as inhibitors of HCV NS3 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2925-8 (2003)
Schering-Plough Research Institute
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2921-4 (2003)
Neurogen
Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2907-11 (2003)
University of California Irvine
Linearized and truncated microcystin analogues as inhibitors of protein phosphatases 1 and 2A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2903-6 (2003)
University of California Irvine
Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2895-8 (2003)
Roche Research Center
Antitumor agents. Part 226: synthesis and cytotoxicity of 2-phenyl-4-quinolone acetic acids and their esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2891-3 (2003)
University of North Carolina
Cage amines as the stopper inhibitors of cholinesterases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2887-90 (2003)
National Chung-Hsing University
Differentially functionalized diamines as novel ligands for the NPY2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2883-5 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2875-8 (2003)
University of Antwerp
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2867-73 (2003)
Universit£
MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2843-6 (2003)
Umr/Cnrs 6013
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2833-6 (2003)
Sankyo
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2829-32 (2003)
Sankyo
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2825-8 (2003)
University of Bristol
Pharmacological and genetic characterization of two selective serotonin transporter ligands: 2-[2-(dimethylaminomethylphenylthio)]-5-fluoromethylphenylamine (AFM) and 3-amino-4-[2-(dimethylaminomethyl-phenylthio)]benzonitrile (DASB).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 308: 481-6 (2004)
National Institutes of Health
Synthesis of a diverse library of mechanism-based cysteine protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Comb Chem 5: 869-80 (2003)
University of California Berkeley
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 302: 875-878 (2003)
Pfizer
High affinity, bioavailable 3-amino-1,4-benzodiazepine-based gamma-secretase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4143-5 (2003)
Merck Sharp & Dohme Research Laboratories
Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4133-7 (2003)
Organix
A new class of glycogen phosphorylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4125-8 (2003)
Merck Research Laboratories
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4121-4 (2003)
Novartis Institute of Biomedical Research
Inhibitory effects on mitochondrial complex I of semisynthetic mono-tetrahydrofuran acetogenin derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4101-5 (2003)
Universidad De Valencia
Utility of boron clusters for drug design. Relation between estrogen receptor binding affinity and hydrophobicity of phenols bearing various types of carboranyl groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4089-92 (2003)
Tohoku Pharmaceutical University
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4085-8 (2003)
Toa Eiyo
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4071-5 (2003)
Ligand Pharmaceuticals
Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4059-63 (2003)
Vertex Pharmaceuticals
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4047-50 (2003)
Astrazeneca R&D Charnwood
Novel P2X7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4043-6 (2003)
Astrazeneca
2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4031-4 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 4027-30 (2003)
Merck Research Laboratories
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4015-7 (2003)
Yale University
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4007-10 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 4001-5 (2003)
Abbott Laboratories
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3997-4000 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3983-7 (2003)
Merck Research Laboratories
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3979-82 (2003)
Merck Research Laboratories
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3975-8 (2003)
Memorial Sloan-Kettering Cancer Center
Synthesis of 2-fluoronoraristeromycin and its inhibitory activity against Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3963-5 (2003)
Gifu University
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3947-50 (2003)
Abbott Laboratories
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3939-42 (2003)
Eli Lilly
Heterocyclic ketones as inhibitors of histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3909-13 (2003)
Abbott Laboratories
Green tea catechins as a BACE1 (beta-secretase) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3905-8 (2003)
Kyungpook National University
Human organic anion transporter 3 (hOAT3) can operate as an exchanger and mediate secretory urate flux.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cell Physiol Biochem 13: 249-56 (2003)
Georg-August-Universit£T
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5091-4 (2003)
Novartis Research Institute Vienna
Molecular docking studies of natural cholinesterase-inhibiting steroidal alkaloids from Sarcococca saligna.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5087-90 (2003)
University of Innsbruck
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5074-82 (2003)
Duquesne University
Synthesis and biological evaluation of 5-substituted derivatives of the potent antiherpes agent (north)-methanocarbathymine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5045-54 (2003)
National Cancer Institute-Frederick
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 5005-14 (2003)
University of Antwerp (Uia)
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4974-87 (2003)
Niddk
Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4965-73 (2003)
University of Arizona
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4952-64 (2003)
Glaxosmithkline Pharmaceuticals
Synthesis, characterization, and biological properties of 8-azido- and 8-amino-substituted 2',5'-oligoadenylates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4926-32 (2003)
Gunma University
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4910-25 (2003)
Pharmaceutical Research Institute
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4895-903 (2003)
University of Bologna
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4883-94 (2003)
Novo Nordisk
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4872-82 (2003)
University of Alberta
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4847-59 (2003)
Niddk
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4834-7 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4826-9 (2003)
Sapienza University of Rome
Semiplenamides A-G, fatty acid amides from a Papua New Guinea collection of the marine cyanobacterium Lyngbya semiplena.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1364-8 (2003)
Oregon State University
Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1338-44 (2003)
Merck Research Laboratories
Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 45: 935-44 (2003)
Eli Lilly
Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Am Heart J 146: 591-604 (2003)
University of Maryland Hospital
Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4799-802 (2003)
Wayne State University School of Medicine
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4790-8 (2003)
Merck Research Laboratories
Potent inhibition of NTPase/helicase of the West Nile Virus by ring-expanded ("fat") nucleoside analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4776-89 (2003)
University of Maryland
Finding discriminating structural features by reassembling common building blocks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4770-5 (2003)
Leadscope
Adenosine kinase inhibitors. 3. Synthesis, SAR, and antiinflammatory activity of a series of l-lyxofuranosyl nucleosides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4750-60 (2003)
Metabasis Therapeutics
Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4714-27 (2003)
Cardiff University
Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4702-13 (2003)
Roche Palo Alto
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4696-701 (2003)
Pharmacia
Molecular determinants of steroid inhibition for the mouse constitutive androstane receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4687-95 (2003)
University of Kuopio
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4676-86 (2003)
Boehringer Ingelheim Pharmaceuticals
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4669-75 (2003)
Boehringer Ingelheim Pharmaceuticals
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4657-68 (2003)
University of Tennessee Health Sciences Center
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3 beta) from a library of compound searching.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4631-3 (2003)
Instituto De Quimica Medica (Csic)
Human beta-secretase (BACE) and BACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4625-30 (2003)
Elan Pharmaceuticals
Sulphonamide-based small molecule VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3875-8 (2003)
Molecumetics
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3859-61 (2003)
Gedeon Richter
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3841-6 (2003)
Eli Lilly
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3835-9 (2003)
Eli Lilly
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3821-5 (2003)
Abbott Laboratories
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3817-20 (2003)
Abbott Laboratories
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3813-6 (2003)
Merck Frosst Centre For Therapeutic Research
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3797-800 (2003)
Wyeth Research
Aryl piperazine melanocortin MC4 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3793-6 (2003)
Neurocrine Biosciences
Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3783-7 (2003)
Universit£
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3779-82 (2003)
Florida A&M University
The total synthesis of an aurone isolated from Uvaria hamiltonii: aurones and flavones as anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3759-63 (2003)
Cardiff University
Exploring selectivity requirements for COX-2 versus COX-1 binding of 3,4-diaryloxazolones using E-state index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3753-7 (2003)
Jadavpur University
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3727-30 (2003)
Pfizer
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3721-5 (2003)
Pharmacia
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3715-8 (2003)
Merck
Identification of a novel class of inhibitor of human and Escherichia coli thymidine phosphorylase by in silico screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3705-9 (2003)
University of Manchester
Biphenyl-based analogues of thiolactomycin, active against Mycobacterium tuberculosis mtFabH fatty acid condensing enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3685-8 (2003)
The University of Birmingham
Biological evaluation of sphingomyelin analogues as inhibitors of sphingomyelinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3681-4 (2003)
Taisho Pharmaceutical
Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3673-7 (2003)
Novartis Research Institute Vienna
Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3661-3 (2003)
Imperial College
Identification of potent and novel small-molecule inhibitors of caspase-3.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3651-5 (2003)
Sunesis Pharmaceuticals
Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3643-5 (2003)
University of Basel
Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 307: 947-54 (2003)
Cornell University
Characterization of the transport of the bicyclic peptide phalloidin by human hepatic transport proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Naunyn Schmiedebergs Arch Pharmacol 368: 415-20 (2003)
Deutsches Krebsforschungszentrum
Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 278: 49773-9 (2003)
Probiodrug
Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 10: 837-46 (2003)
Brigham and Women'S Hospital
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4609-24 (2003)
Novartis Institute For Biomedical Research
New prolyl oligopeptidase inhibitors developed from dicarboxylic acid bis(l-prolyl-pyrrolidine) amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4543-51 (2003)
University of Kuopio
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4533-42 (2003)
Glaxosmithkline
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4525-32 (2003)
Glaxosmithkline
Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4501-15 (2003)
Lindsley F. Kimball Research Institute
Identification and prediction of promiscuous aggregating inhibitors among known drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4477-86 (2003)
Northwestern University
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4463-76 (2003)
University of London
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4428-49 (2003)
Glaxosmithkline
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4405-18 (2003)
Bristol-Myers Squibb
Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4393-404 (2003)
Technische Universit£T M£Nchen
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4377-92 (2003)
University of Michigan
Biological activity of tropolone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biol Pharm Bull 26: 1487-90 (2003)
Osaka Organic Chemical Industry
WAY-855 (3-amino-tricyclo[2.2.1.02.6]heptane-1,3-dicarboxylic acid): a novel, EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptake.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 140: 839-46 (2003)
Wyeth Research
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 42: 11451-9 (2003)
Merck Research Laboratories
New bioactive diterpene polyesters from Euphorbia decipiens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1221-4 (2003)
University of Karachi
Constituents from the leaves of Phellodendron amurense var. wilsonii and their bioactivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1207-11 (2003)
National Cheng Kung University
Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1191-6 (2003)
Kyoto Pharmaceutical University
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3623-6 (2003)
Idun Pharmaceuticals
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3617-22 (2003)
Neurocrine Biosciences
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3611-6 (2003)
Purdue Pharma
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3601-5 (2003)
Pharmacor
Design and synthesis of novel CCR3 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3597-600 (2003)
Roche Palo Alto
Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3593-6 (2003)
Pfizer
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3565-9 (2003)
Georgetown University Medical Center
3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3557-60 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3541-4 (2003)
Merck Research Laboratories
Synthesis and evaluation of tripeptidyl alpha-ketoamides as human rhinovirus 3C protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3531-6 (2003)
Eli Lilly
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3527-30 (2003)
University of Cape Town
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3491-5 (2003)
Pharmacia
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3487-90 (2003)
University of Tennessee-Memphis
Pyrimido[1,2-b]-1,2,4,5-tetrazin-6-ones as HCMV protease inhibitors: a new class of heterocycles with flavin-like redox properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3483-6 (2003)
Wyeth Research
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3477-82 (2003)
Merck Research Laboratories
An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3465-70 (2003)
Northwestern University
Synthesis and glycosidase inhibitory activity of some N-substituted 6-deoxy-5a-carba-beta-DL- and L-galactopyranosylamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3461-3 (2003)
Keio University
Design and synthesis of small chemical inhibitors containing different scaffolds for lck SH2 domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3455-9 (2003)
Mogam Biotechnology Research Institute
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3419-21 (2003)
Nps Pharmaceuticals
Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3405-8 (2003)
Merck Research Laboratories
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3401-4 (2003)
University of Virginia
The rabbit motilin receptor: molecular characterisation and pharmacology.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 140: 948-54 (2003)
Glaxosmithkline
Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 865-75 (2003)
The Danish University of Pharmaceutical Sciences
Differential activation of formyl peptide receptor signaling by peptide ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 841-7 (2003)
Pohang University of Science and Technology
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)