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10999999 83 Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.EBI J Med Chem 43: 3453-73 (2000) COR Therapeutics, Inc. 2D 3D TSV
10999489 29 2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.EBI Bioorg Med Chem Lett 10: 2141-4 (2000) University of Amsterdam 2D 3D TSV
10999488 34 7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.EBI Bioorg Med Chem Lett 10: 2137-40 (2000) Celltech-Chiroscience Ltd, Abington, Cambridge, UK. 2D 3D TSV
10999484 38 Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.EBI Bioorg Med Chem Lett 10: 2119-22 (2000) Neurogen Corporation 2D 3D TSV
10999482 52 Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.EBI Bioorg Med Chem Lett 10: 2111-4 (2000) Merck Research Laboratories 2D 3D TSV
10999477 40 Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.EBI Bioorg Med Chem Lett 10: 2087-90 (2000) Kyoto University 2D 3D TSV
10999475 43 Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.EBI Bioorg Med Chem Lett 10: 2079-81 (2000) Pharmacia 2D 3D TSV
10999473 26 Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.EBI Bioorg Med Chem Lett 10: 2071-4 (2000) Institute 2D 3D TSV
10999472 4 Computational binding studies of human pp60c-src SH2 domain with a series of nonpeptide, phosphophenyl-containing ligands.EBI Bioorg Med Chem Lett 10: 2067-70 (2000) Yale University 2D 3D TSV
10999471 2 A novel inhibitor of human telomerase derived from 10H-indolo[3,2-b]quinoline.EBI Bioorg Med Chem Lett 10: 2063-6 (2000) Reading University 2D 3D TSV
10999468 30 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.EBI Bioorg Med Chem Lett 10: 2051-4 (2000) Bayer Research Center 2D 3D TSV
10999467 19 Discovery of a new class of p38 kinase inhibitors.EBI Bioorg Med Chem Lett 10: 2047-50 (2000) Bayer Research Center 2D 3D TSV
10998351 24 Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI Biochem J 351: 95-105 (2001) University of Dundee 2D 3D TSV
10998059 168 Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.BDB Eur J Biochem 267: 5983-94 (2000) CNRS 2D 3D TSV
10991999 13 Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.BDB J Pharmacol Exp Ther 295: 337-45 (2000) CoCensys, Inc. 2D 3D TSV
10991998 32 Cannabinoid agonist signal transduction in rat brain: comparison of cannabinoid agonists in receptor binding, G-protein activation, and adenylyl cyclase inhibition.BDB J Pharmacol Exp Ther 295: 328-36 (2000) Wake Forest University 2D 3D TSV
10991988 4 Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1.EBI J Pharmacol Exp Ther 295: 261-5 (2000) Kyoto University Hospital 2D 3D TSV
10991983 21 Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.BDB J Pharmacol Exp Ther 295: 226-32 (2000) Albany Medical College 2D 3D TSV
10991954 12 Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.EBI J Pharmacol Exp Ther 295: 10-5 (2000) Gilead Sciences 2D 3D TSV
10987445 140 Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.EBI Bioorg Med Chem Lett 10: 2041-4 (2001) Friedrich-Alexander University 2D 3D TSV
10987444 16 Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1.EBI Bioorg Med Chem Lett 10: 2037-9 (2001) Novartis Institute for Biomedical Research 2D 3D TSV
10987441 10 Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.EBI Bioorg Med Chem Lett 10: 2023-6 (2001) Université de la Méditerranée 2D 3D TSV
10987435 27 Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.EBI Bioorg Med Chem Lett 10: 1995-9 (2001) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10987434 41 Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.EBI Bioorg Med Chem Lett 10: 1991-4 (2001) Wyeth-Ayerst Research 2D 3D TSV
10987430 86 Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.EBI Bioorg Med Chem Lett 10: 1975-8 (2001) Merck Research Laboratories Rahway 2D 3D TSV
10987429 69 Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.EBI Bioorg Med Chem Lett 10: 1971-3 (2001) Merck Research Laboratories 2D 3D TSV
10987424 30 The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.EBI Bioorg Med Chem Lett 10: 1949-52 (2001) AstraZeneca Pharmaceuticals 2D 3D TSV
10987423 83 Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.EBI Bioorg Med Chem Lett 10: 1943-8 (2001) Merck Research Laboratories 2D 3D TSV
10987417 48 Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.EBI Bioorg Med Chem Lett 10: 1917-20 (2001) Merck Research Laboratories 2D 3D TSV
10987415 18 Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.EBI Bioorg Med Chem Lett 10: 1909-11 (2001) University of Canterbury 2D 3D TSV
10980448 3 Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.BDB Chem Biol 7: 677-82 (2000) Pfizer Inc 2D 3D TSV
10978197 3 Workup-dependent formation of 5-lipoxygenase inhibitory boswellic acid analogues.EBI J Nat Prod 63: 1058-61 (2000) Institute of Pharmaceutical Sciences 2D 3D TSV
10978192 5 Privileged molecules for protein binding identified from NMR-based screening.EBI J Med Chem 43: 3443-7 (2000) Abbott Laboratories 2D 3D TSV
10978189 115 Structure-activity studies including a Psi(CH(2)-NH) scan of peptide YY (PYY) active site, PYY(22-36), for interaction with rat intestinal PYY receptors: development of analogues with potent in vivo activity in the intestine.EBI J Med Chem 43: 3420-7 (2000) University of Cincinnati Medical Center 2D 3D TSV
10978188 85 Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.EBI J Med Chem 43: 3408-19 (2000) CoCensys, Inc. 2D 3D TSV
10978187 4 Synthesis and biological activity of a novel 11a-homo (cyclohexyl) prostaglandin.EBI J Med Chem 43: 3400-7 (2000) Alcon Laboratories, Inc. 2D 3D TSV
10978186 45 Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.EBI J Med Chem 43: 3386-99 (2000) Merck Research Laboratories 2D 3D TSV
10978184 3 Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.EBI J Med Chem 43: 3372-6 (2000) Suntory Biomedical Research Limited 2D 3D TSV
10978183 40 Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.EBI J Med Chem 43: 3351-71 (2000) BASF Bioresearch Corporation 2D 3D TSV
10974196 31 Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.BDB Biochem Pharmacol 60: 885-98 (2000) Parke-Davis Pharmaceutical Research 2D 3D TSV
10973807 2 Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate.EBI Biochem Biophys Res Commun 275: 831-8 (2000) Tohoku University School of Medicine 2D 3D TSV
10969992 3 Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents.EBI Bioorg Med Chem Lett 10: 1887-91 (2000) Università degli Studi 2D 3D TSV
10969990 12 Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides.EBI Bioorg Med Chem Lett 10: 1879-82 (2000) Institute of Science and Technology 2D 3D TSV
10969989 45 Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.EBI Bioorg Med Chem Lett 10: 1875-8 (2000) Shionogi & Co., Ltd. 2D 3D TSV
10969988 4 Aminoalkyl adenylate and aminoacyl sulfamate intermediate analogues differing greatly in affinity for their cognate Staphylococcus aureus aminoacyl tRNA synthetases.EBI Bioorg Med Chem Lett 10: 1871-4 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10969987 63 1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.EBI Bioorg Med Chem Lett 10: 1867-70 (2000) SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com 2D 3D TSV
10969986 123 1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.EBI Bioorg Med Chem Lett 10: 1863-6 (2000) SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com 2D 3D TSV
10969978 9 A solid-phase synthesis for beta-turn mimetics of sialyl Lewis X.EBI Bioorg Med Chem Lett 10: 1827-30 (2000) Nippon Organon K.K. 2D 3D TSV
10969976 13 Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.BDB Bioorg Med Chem Lett 10: 1819-22 (2000) Korea Research Institute of Bioscience and Biotechnology 2D 3D TSV
10969974 4 Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of four stereoisomeric analogues of the natural product SB-219383.EBI Bioorg Med Chem Lett 10: 1811-4 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10969973 103 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.EBI Bioorg Med Chem Lett 10: 1807-10 (2000) Eli Lilly and Company Ltd 2D 3D TSV
10969972 39 CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.EBI Bioorg Med Chem Lett 10: 1803-6 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10969967 34 Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.EBI Bioorg Med Chem Lett 10: 1783-5 (2000) Yale University 2D 3D TSV
10966754 9 3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.EBI J Med Chem 43: 3348-50 (2000) University of Bristol 2D 3D TSV
10966753 5 Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.EBI J Med Chem 43: 3344-7 (2000) The University of Michigan Medical School 2D 3D TSV
10966752 60 New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.EBI J Med Chem 43: 3335-43 (2000) Freie Universität Berlin 2D 3D TSV
10966747 7 Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.EBI J Med Chem 43: 3283-94 (2000) Georgetown University Medical Center 2D 3D TSV
10966743 51 4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.BDB J Med Chem 43: 3244-56 (2000) Wyeth-Ayerst Research 2D 3D TSV
10966741 12 Crystal structures of human factor Xa complexed with potent inhibitors.BDB J Med Chem 43: 3226-32 (2000) Aventis Pharma 2D 3D TSV
10966739 28 Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.EBI J Med Chem 43: 3209-17 (2000) National Cancer Institute 2D 3D TSV
10964567 30 Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.BDB J Mol Biol 302: 155-70 (2000) CNRS 2D 3D TSV
10963748 3 The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor.BDB Neuropharmacology 39: 2044-53 (2000) University of Frankfurt 2D 3D TSV
10956228 13 Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.EBI J Med Chem 43: 3193-6 (2000) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10956225 106 Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.EBI J Med Chem 43: 3168-85 (2000) Pfizer Inc. 2D 3D TSV
10956223 41 Use of an additional hydrophobic binding site, the Z site, in the rational drug design of a new class of stronger trypanothione reductase inhibitor, quaternary alkylammonium phenothiazines.EBI J Med Chem 43: 3148-56 (2000) University of Manchester 2D 3D TSV
10956222 105 Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).BDB J Med Chem 43: 3134-47 (2000) University of Auckland 2D 3D TSV
10956221 46 Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.EBI J Med Chem 43: 3125-33 (2000) Duquesne University 2D 3D TSV
10956220 93 Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.EBI J Med Chem 43: 3118-24 (2000) Universita' di Firenze 2D 3D TSV
10956219 26 Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.EBI J Med Chem 43: 3111-7 (2000) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10956218 12 Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.EBI J Med Chem 43: 3103-10 (2000) Centre for Addiction and Mental Health 2D 3D TSV
10956215 52 1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.EBI J Med Chem 43: 3074-84 (2000) Virginia Commonwealth University 2D 3D TSV
10956211 14 GRID/CPCA: a new computational tool to design selective ligands.EBI J Med Chem 43: 3033-44 (2000) Boehringer Ingelheim Pharma KG 2D 3D TSV
10956210 85 DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors.EBI J Med Chem 43: 3020-32 (2000) Eli Lilly and Company 2D 3D TSV
10956209 79 CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.EBI J Med Chem 43: 3005-19 (2000) University of Texas 2D 3D TSV
10956208 121 Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.EBI J Med Chem 43: 2992-3004 (2000) University of Catania 2D 3D TSV
10956207 43 2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.EBI J Med Chem 43: 2982-91 (2000) Organix Inc. 2D 3D TSV
10956205 11 Identification of a chemical tool for the orphan nuclear receptor FXR.EBI J Med Chem 43: 2971-4 (2000) Glaxo Wellcome Research& Development 2D 3D TSV
10956202 51 Synthesis and evaluation of peptidomimetics as selective inhibitors and active site probes of nitric oxide synthases.EBI J Med Chem 43: 2938-45 (2000) Northwestern University 2D 3D TSV
10956198 2 Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists.EBI J Med Chem 43: 2906-14 (2000) State University of New York 2D 3D TSV
10956197 34 Adenosine kinase inhibitors. 2. Synthesis, enzyme inhibition, and antiseizure activity of diaryltubercidin analogues.EBI J Med Chem 43: 2894-905 (2000) Metabasis Therapeutics Inc 2D 3D TSV
10956196 39 Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues.EBI J Med Chem 43: 2883-93 (2000) Metabasis Therapeutics Inc 2D 3D TSV
10956195 38 Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).EBI J Med Chem 43: 2871-82 (2000) University Centre for Pharmacy 2D 3D TSV
10956194 152 Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.EBI J Med Chem 43: 2860-70 (2000) Vanderbilt University School of Medicine 2D 3D TSV
10956192 31 Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.EBI J Med Chem 43: 2837-50 (2000) AstraZeneca R&D Södertälje 2D 3D TSV
10956191 31 Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.EBI J Med Chem 43: 2831-6 (2000) Institute of Science 2D 3D TSV
10956190 11 Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.EBI J Med Chem 43: 2824-30 (2000) Institute of Science 2D 3D TSV
10956189 98 A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.EBI J Med Chem 43: 2814-23 (2000) Universit£ di Pisa 2D 3D TSV
10956187 18 Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.BDB J Med Chem 43: 2797-804 (2000) University of Newcastle 2D 3D TSV
10956186 43 A refined 3-dimensional QSAR of cytochrome P450 2C9: computational predictions of drug interactions.EBI J Med Chem 43: 2789-96 (2000) Washington State University 2D 3D TSV
10956183 19 De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.EBI J Med Chem 43: 2775-8 (2000) Synaptic Pharmaceutical Corporation 2D 3D TSV
10945872 14 Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.BDB J Pharmacol Exp Ther 294: 1154-65 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10944518 27 The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.BDB J Biol Chem 275: 36043-8 (2000) Federal Institute of Technology of Zurich 2D 3D TSV
10937745 7 Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.EBI Bioorg Med Chem Lett 10: 1771-3 (2000) Queen's University Belfast 2D 3D TSV
10937743 10 Grignard-mediated synthesis and preliminary biological evaluation of novel 3-substituted farnesyl diphosphate analogues.EBI Bioorg Med Chem Lett 10: 1763-6 (2000) Wayne State University 2D 3D TSV
10937738 38 Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.EBI Bioorg Med Chem Lett 10: 1745-8 (2000) University of Barcelona 2D 3D TSV
10937736 35 Nonbenzamidine compounds as selective factor Xa inhibitors.EBI Bioorg Med Chem Lett 10: 1737-9 (2000) Aventis Pharmaceuticals 2D 3D TSV
10937734 30 Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.BDB Bioorg Med Chem Lett 10: 1729-31 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10937733 70 Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.EBI Bioorg Med Chem Lett 10: 1723-7 (2000) Merck Research Laboratories 2D 3D TSV
10937732 15 6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.EBI Bioorg Med Chem Lett 10: 1719-21 (2000) NPS Allelix Corp. 2D 3D TSV
10937729 21 5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.EBI Bioorg Med Chem Lett 10: 1707-9 (2000) NPS Allelix Corp. 2D 3D TSV
10937725 18 Anhydride modified cantharidin analogues: synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity.EBI Bioorg Med Chem Lett 10: 1687-90 (2000) The University of Newcastle 2D 3D TSV
10937724 56 Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.EBI Bioorg Med Chem Lett 10: 1681-6 (2000) Georgetown University Medical Center 2D 3D TSV
10937721 9 Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.EBI Bioorg Med Chem Lett 10: 1669-71 (2000) University of Tokyo 2D 3D TSV
10937720 24 Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.EBI Bioorg Med Chem Lett 10: 1665-8 (2000) Sankyo Co., Ltd. 2D 3D TSV
10937715 45 Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate.EBI Bioorg Med Chem Lett 10: 1645-8 (2000) Signal Pharmaceuticals, Inc. 2D 3D TSV
10937714 19 N-acylated alpha-(3-pyridylmethyl)-beta-aminotetralin antagoinists of the human neuropeptide Y Y5 receptor.EBI Bioorg Med Chem Lett 10: 1641-3 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10937713 186 Solid-phase synthesis of an arylsulfone hydroxamate library.EBI Bioorg Med Chem Lett 10: 1637-40 (2000) Rhone Poulenc Rorer 2D 3D TSV
10937710 81 Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI Bioorg Med Chem Lett 10: 1625-8 (2000) Merck & Co. 2D 3D TSV
10937709 87 Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.EBI Bioorg Med Chem Lett 10: 1621-4 (2000) Merck & Co. 2D 3D TSV
10926521 15 Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.BDB J Mol Biol 301: 465-75 (2000) Max-Planck-Institut fuer Biochemie 2D 3D TSV
10915062 2 Michael adducts of ascorbic acid as inhibitors of protein phosphatase 2A and inducers of apoptosis.EBI Bioorg Med Chem Lett 10: 1605-8 (2000) Universität Göttingen 2D 3D TSV
10915060 54 Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.EBI Bioorg Med Chem Lett 10: 1597-600 (2000) University of Regensburg 2D 3D TSV
10915056 8 Difluoroketones as inhibitors of matrix metalloprotease-13.EBI Bioorg Med Chem Lett 10: 1581-4 (2000) Pfizer Inc. 2D 3D TSV
10915054 6 Kinetic characterisation of ene-diol-based inhibitors of alpha-amylase.EBI Bioorg Med Chem Lett 10: 1575-6 (2000) University of Canterbury 2D 3D TSV
10915052 20 The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.EBI Bioorg Med Chem Lett 10: 1567-70 (2000) Novartis Horsham Research Centre 2D 3D TSV
10915051 43 The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.EBI Bioorg Med Chem Lett 10: 1563-6 (2000) Novartis Horsham Research Centre 2D 3D TSV
10915050 14 Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.EBI Bioorg Med Chem Lett 10: 1559-62 (2000) Inha University 2D 3D TSV
10915049 22 1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.EBI Bioorg Med Chem Lett 10: 1555-8 (2000) Novartis Institute for Biomedical Research 2D 3D TSV
10915044 4 Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes.EBI Bioorg Med Chem Lett 10: 1535-8 (2000) Wyeth-Ayerst Research 2D 3D TSV
10915043 69 Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.EBI Bioorg Med Chem Lett 10: 1531-4 (2000) Merck Research Laboratories 2D 3D TSV
10915042 3 Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.EBI Bioorg Med Chem Lett 10: 1527-30 (2000) Merck Research Laboratories 2D 3D TSV
10915041 2 Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase.EBI Bioorg Med Chem Lett 10: 1523-6 (2000) Department of Chemistry, The University of Montana, Missoula 59812, USA. 2D 3D TSV
10915040 84 Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.EBI Bioorg Med Chem Lett 10: 1519-22 (2000) Procter & Gamble Pharmaceuticals 2D 3D TSV
10915035 16 Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors.EBI Bioorg Med Chem Lett 10: 1497-9 (2000) Millennium Pharmaceutical 2D 3D TSV
10908357 9 Recognition of a cognate RNA aptamer by neomycin B: quantitative evaluation of hydrogen bonding and electrostatic interactions.BDB Nucleic Acids Res 28: 2935-42 (2000) The Ohio State University 2D 3D TSV
10903938 20 Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.BDB Chem Biol 7: 493-504 (2000) Novartis Pharmaceuticals 2D 3D TSV
10901697 1 Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.EBI Drug Metab Dispos 28: 895-8 (2000) Vanderbilt University School of Medicine 2D 3D TSV
10900230 11 Agonist-directed trafficking of porcine alpha(2A)-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates G(s).BDB J Pharmacol Exp Ther 294: 539-47 (2000) University of Michigan 2D 3D TSV
10893314 24 Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.EBI J Med Chem 43: 2759-69 (2000) University of Minnesota 2D 3D TSV
10893311 62 Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.EBI J Med Chem 43: 2738-44 (2000) National Center for Genetic Engineering and Biotechnology 2D 3D TSV
10893310 5 Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.EBI J Med Chem 43: 2731-7 (2000) Arizona State University 2D 3D TSV
10893308 102 In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.EBI J Med Chem 43: 2703-18 (2000) Merck Research Laboratories 2D 3D TSV
10893307 26 [Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.EBI J Med Chem 43: 2698-702 (2000) University of California 2D 3D TSV
10893306 21 Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.EBI J Med Chem 43: 2685-97 (2000) Université de Lille 2 2D 3D TSV
10893305 8 Synthesis and antitumor activity of new benzoheterocyclic derivatives of distamycin A.EBI J Med Chem 43: 2675-84 (2000) Universit£ di Ferrara 2D 3D TSV
10893303 100 Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.BDB J Med Chem 43: 2655-63 (2000) SUGEN, Inc. 2D 3D TSV
10893301 270 Ligands for glutamate receptors: design and therapeutic prospects.EBI J Med Chem 43: 2609-45 (2000) The Royal Danish School of Pharmacy 2D 3D TSV
10891120 7 Novel nonsubstrate inhibitors of human thymidine phosphorylase, a potential target for tumor-dependent angiogenesis.EBI J Med Chem 43: 2601-7 (2000) Istituto di Genetica Biochimica ed Evoluzionistica 2D 3D TSV
10891118 6 Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.EBI J Med Chem 43: 2586-90 (2000) University of Northern Colorado 2D 3D TSV
10891114 28 Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter.EBI J Med Chem 43: 2547-56 (2000) Strasbourg 1 University 2D 3D TSV
10891111 56 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.EBI J Med Chem 43: 2523-9 (2000) Eisai Company, Ltd. 2D 3D TSV
10891110 87 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.EBI J Med Chem 43: 2514-22 (2000) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10891109 19 Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.BDB J Med Chem 43: 2506-13 (2000) Palacky University 2D 3D TSV
10891107 3 Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.EBI J Med Chem 43: 2489-92 (2000) University of Minnesota 2D 3D TSV
10891096 10 Structure-based design and solid-phase parallel synthesis of phosphorylated nonpeptides to explore hydrophobic binding at the Src SH2 domain.BDB J Comb Chem 2: 305-13 ARIAD Pharmaceuticals, Inc. 2D 3D TSV
10890171 6 Synthesis and biological activities of an alpha-methyl and a beta-methyl carbapenem and the corresponding unsubstituted compound.EBI Bioorg Med Chem Lett 10: 1389-91 (2000) University of Munich 2D 3D TSV
10890169 48 N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.EBI Bioorg Med Chem Lett 10: 1381-4 (2000) Merck Sharp & Dohme Research Laboratories 2D 3D TSV
10890168 9 Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.EBI Bioorg Med Chem Lett 10: 1377-80 (2000) Zentrum für Pharmaforschung 2D 3D TSV
10890163 2 Convergent synthesis of ribonuclease L-active 2',5'-oligoadenylate-peptide nucleic acids.EBI Bioorg Med Chem Lett 10: 1357-60 (2000) National Institute of Diabetes and Digestive antd Kidney Diseases 2D 3D TSV
10890162 52 Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.EBI Bioorg Med Chem Lett 10: 1351-5 (2000) Hoechst Marion Roussel 2D 3D TSV
10890161 11 Synthesis and uptake of nitric oxide-releasing drugs by the P2 nucleoside transporter in Trypanosoma equiperdum.EBI Bioorg Med Chem Lett 10: 1347-50 (2000) Universit£ de Toulouse III 2D 3D TSV
10890154 14 Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.EBI Bioorg Med Chem Lett 10: 1315-6 (2000) Kitasato University 2D 3D TSV
10888340 4 Synthesis of N-diisopropyl phosphoryl benzyltetrahydroisoquinoline, a new class of mitochondrial complexes I and III inhibitors.EBI Bioorg Med Chem Lett 10: 1491-4 (2000) Universidad de Valencia 2D 3D TSV
10888337 1 Potent new leucine aminopeptidase inhibitor of novel structure synthesised by a modified Wadsworth-Emmons (Horner) Wittig procedure.EBI Bioorg Med Chem Lett 10: 1481-2 (2000) The Queen's University of Belfast 2D 3D TSV
10888335 5 Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.EBI Bioorg Med Chem Lett 10: 1471-5 (2000) The Scripps Research Institute 2D 3D TSV
10888334 10 N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist.EBI Bioorg Med Chem Lett 10: 1467-70 (2000) Novartis Pharma AG 2D 3D TSV
10888332 31 Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors.EBI Bioorg Med Chem Lett 10: 1459-62 (2000) Nippon Roche Research Center 2D 3D TSV
10888331 16 Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers.EBI Bioorg Med Chem Lett 10: 1455-7 (2000) Korea Research Institute of Bioscience and Biotechnology 2D 3D TSV
10888329 22 Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.EBI Bioorg Med Chem Lett 10: 1447-50 (2000) Università di Perugia 2D 3D TSV
10888328 17 An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.EBI Bioorg Med Chem Lett 10: 1443-6 (2000) Georgetown University Medical Center 2D 3D TSV
10888326 12 Synthesis of tetrakis(multifluoro-4-pyridyl)porphin derivatives as acetylcholinesterase inhibitors.EBI Bioorg Med Chem Lett 10: 1435-8 (2000) Seoul National University 2D 3D TSV
10888325 90 Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.EBI Bioorg Med Chem Lett 10: 1431-4 (2000) Merck Research Laboratories 2D 3D TSV
10888324 48 Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.EBI Bioorg Med Chem Lett 10: 1427-9 (2000) Merck Research Laboratories 2D 3D TSV
10888319 5 Antifungal rapamycin analogues with reduced immunosuppressive activity.EBI Bioorg Med Chem Lett 10: 1405-8 (2000) Abbott Laboratories 2D 3D TSV
10882376 7 A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.EBI J Med Chem 43: 2479-83 (2000) Rational Drug Design Laboratories 2D 3D TSV
10882373 15 6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1.EBI J Med Chem 43: 2457-63 (2000) University of Michigan 2D 3D TSV
10882371 8 Deoxy sugar analogues of triciribine: correlation of antiviral and antiproliferative activity with intracellular phosphorylation.EBI J Med Chem 43: 2438-48 (2000) University of Michigan 2D 3D TSV
10882369 20 Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.EBI J Med Chem 43: 2419-29 (2000) Purdue University 2D 3D TSV
10882365 4 A rational approach to the design and synthesis of a new bradykinin B(1) receptor antagonist.EBI J Med Chem 43: 2387-94 (2000) Universités Montpellier I et II 2D 3D TSV
10882364 19 Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.EBI J Med Chem 43: 2382-6 (2000) Universités Montpellier I et II 2D 3D TSV
10882362 2 Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.EBI J Med Chem 43: 2362-70 (2000) The James Black Foundation 2D 3D TSV
10882361 18 Synthesis and biological evaluation of bombesin constrained analogues.EBI J Med Chem 43: 2356-61 (2000) CNRS-Universités Montpellier I & II 2D 3D TSV
10882360 17 CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.EBI J Med Chem 43: 2350-5 (2000) AstraZeneca R&D Boston 2D 3D TSV
10882359 11 17beta-O-Aminoalkyloximes of 5beta-androstane-3beta,14beta-diol with digitalis-like activity: synthesis, cardiotonic activity, structure-activity relationships, and molecular modeling of the Na(+),K(+)-ATPase receptor.EBI J Med Chem 43: 2332-49 (2000) Prassis Istituto di Ricerche Sigma-Tau 2D 3D TSV
10882358 62 Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.EBI J Med Chem 43: 2324-31 (2000) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10882357 87 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.BDB J Med Chem 43: 2310-23 (2000) Novartis Pharmaceuticals 2D 3D TSV
10882355 5 Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.EBI J Med Chem 43: 2297-9 (2000) Amgen 2D 3D TSV
10882354 19 Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.EBI J Med Chem 43: 2293-6 (2000) Pfizer Inc. 2D 3D TSV
10882008 93 2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.BDB Bioorg Med Chem 8: 957-75 (2000) Alcon Research, Ltd. 2D 3D TSV
10869410 62 S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.BDB J Pharmacol Exp Ther 293: 1048-62 (2000) Centre de Recherches de Croissy 2D 3D TSV
10869408 6 Trans-stimulation effects of folic acid derivatives on methotrexate transport by rat renal organic anion transporter, OAT-K1.EBI J Pharmacol Exp Ther 293: 1034-9 (2000) Kyoto University Hospital 2D 3D TSV
10869375 23 Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.BDB J Pharmacol Exp Ther 293: 771-8 (2000) R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10869205 2 The application of HPLC with on-line coupled UV/MS-biochemical detection for isolation of an acetylcholinesterase inhibitor from narcissus 'Sir Winston Churchill'.EBI J Nat Prod 63: 803-6 (2000) Leiden University 2D 3D TSV
10869198 1 Antifungal substances against pathogenic fungi, talaroconvolutins, from talaromyces convolutus.EBI J Nat Prod 63: 768-72 (2000) Hoshi University 2D 3D TSV
10869194 9 Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.EBI J Nat Prod 63: 753-6 (2000) Seoul National University 2D 3D TSV
10869191 15 Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases.EBI J Nat Prod 63: 739-45 (2000) Heinrich-Heine-Universität 2D 3D TSV
10869183 12 Thermodynamics of sequence-specific binding of PNA to DNA.BDB Biochemistry 39: 7781-91 (2000) Chalmers University of Technology 2D 3D TSV
10866404 9 Discovery of a potent, non-triketone type inhibitor of 4-hydroxyphenylpyruvate dioxygenase.EBI Bioorg Med Chem Lett 10: 1297-8 (2000) Tunghai Christian University 2D 3D TSV
10866403 8 Total synthesis of pyrrolizidines 223H', 239K', 265H', and 267H' found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor.EBI Bioorg Med Chem Lett 10: 1293-5 (2000) Toyama Medical and Pharmaceutical University 2D 3D TSV
10866400 18 4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.EBI Bioorg Med Chem Lett 10: 1281-4 (2000) Research Triangle Institute 2D 3D TSV
10866399 10 Conformationally-restricted ligands for the histamine H1 receptor.EBI Bioorg Med Chem Lett 10: 1277-9 (2000) University of Bath 2D 3D TSV
10866395 33 SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI Bioorg Med Chem Lett 10: 1261-4 (2000) Novartis Pharma AG 2D 3D TSV
10866394 30 Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.BDB Bioorg Med Chem Lett 10: 1257-60 (2000) Gilead Sciences Inc. 2D 3D TSV
10866393 24 Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.EBI Bioorg Med Chem Lett 10: 1253-6 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10866391 10 The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.EBI Bioorg Med Chem Lett 10: 1245-8 (2000) CCIPE-Faculte de Pharmacie 2D 3D TSV
10866390 7 (+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist.EBI Bioorg Med Chem Lett 10: 1241-4 (2000) Novartis Pharma AG 2D 3D TSV
10866387 1 'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.EBI Bioorg Med Chem Lett 10: 1227-31 (2000) Kyoto Pharmaceutical University 2D 3D TSV
10866385 13 Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.EBI Bioorg Med Chem Lett 10: 1219-21 (2000) The Oxford Centre for Molecular Sciences 2D 3D TSV
10866377 9 Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.EBI Bioorg Med Chem Lett 10: 1185-8 (2000) Universit£ di Napoli Federico II 2D 3D TSV
10866375 50 Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.EBI Bioorg Med Chem Lett 10: 1175-9 (2000) Novartis Pharma AG 2D 3D TSV
10866374 11 The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.EBI Bioorg Med Chem Lett 10: 1171-3 (2000) Roche Research Center 2D 3D TSV
10866373 8 Cyclic thioether peptide mimetics as VCAM-VLA-4 antagonists.EBI Bioorg Med Chem Lett 10: 1167-9 (2000) Roche Research Center 2D 3D TSV
10866372 7 Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists.EBI Bioorg Med Chem Lett 10: 1163-5 (2000) Roche Research Center 2D 3D TSV
10866371 12 Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.BDB Bioorg Med Chem Lett 10: 1159-62 (2000) GlaxoSmithKline 2D 3D TSV
10854830 4 Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1.EBI Eur J Pharmacol 398: 193-7 (2000) Kyoto University Hospital 2D 3D TSV
10854287 4 Behaviroal, pharmacological, and molecular characterization of an amphibian cannabinoid receptor.BDB J Neurochem 75: 413-23 (2000) Oregon State University 2D 3D TSV
10853677 36 Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.EBI Bioorg Med Chem Lett 10: 997-9 (2000) Celltech Chiroscience 2D 3D TSV
10853676 13 Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.EBI Bioorg Med Chem Lett 10: 993-5 (2000) Celltech Chiroscience 2D 3D TSV
10853674 32 Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.EBI Bioorg Med Chem Lett 10: 983-7 (2000) Corvas International, Inc. 2D 3D TSV
10853673 22 Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.EBI Bioorg Med Chem Lett 10: 979-81 (2000) University of Wales 2D 3D TSV
10853669 102 Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI Bioorg Med Chem Lett 10: 963-6 (2000) Berlex Biosciences 2D 3D TSV
10853668 52 Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.EBI Bioorg Med Chem Lett 10: 957-61 (2000) Berlex Biosciences 2D 3D TSV
10853665 104 Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.EBI Bioorg Med Chem Lett 10: 945-9 (2000) Novartis Pharma AG 2D 3D TSV
10853661 25 Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.EBI Bioorg Med Chem Lett 10: 923-7 (2000) National Cancer Institute 2D 3D TSV
10853660 23 Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.EBI Bioorg Med Chem Lett 10: 919-21 (2000) NPS Allelix Corp. 2D 3D TSV
10853656 24 5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.EBI Bioorg Med Chem Lett 10: 903-5 (2000) NPS Allelix Corp. 2D 3D TSV
10853654 18 Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.EBI Bioorg Med Chem Lett 10: 895-7 (2000) Iowa State University 2D 3D TSV
10853650 36 Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.EBI Bioorg Med Chem Lett 10: 875-9 (2000) Yoshitomi Pharmaceutical Industries, Ltd. 2D 3D TSV
10853647 63 Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.EBI Bioorg Med Chem Lett 10: 859-63 (2000) Kyoto University 2D 3D TSV
10853646 80 The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.EBI Bioorg Med Chem Lett 10: 853-7 (2000) Southern Methodist University 2D 3D TSV
10853645 34 The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.EBI Bioorg Med Chem Lett 10: 847-51 (2000) Southern Methodist University 2D 3D TSV
10853644 14 SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.EBI Bioorg Med Chem Lett 10: 843-5 (2000) Tunghai Christian University 2D 3D TSV
10851239 7 Characterization of the human cysteinyl leukotriene 2 receptor.BDB J Biol Chem 275: 30531-6 (2000) University of Virginia 2D 3D TSV
10843593 3 Polyoxygenated dysidea sterols that inhibit the binding of [I125] IL-8 to the human recombinant IL-8 receptor type A.EBI J Nat Prod 63: 694-7 (2000) Griffith University 2D 3D TSV
10843231 129 Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV.EBI Bioorg Med Chem Lett 10: 1117-20 (2000) Universit£ degli Studi 2D 3D TSV
10843230 20 Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.EBI Bioorg Med Chem Lett 10: 1113-5 (2000) Yale University 2D 3D TSV
10843229 92 Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.EBI Bioorg Med Chem Lett 10: 1109-11 (2000) R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10843226 45 First pharmacophoric hypothesis for 5-HT7 antagonism.EBI Bioorg Med Chem Lett 10: 1097-100 (2000) Universidad Complutense 2D 3D TSV
10843225 36 Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.EBI Bioorg Med Chem Lett 10: 1093-6 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10843224 28 High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor.EBI Bioorg Med Chem Lett 10: 1089-92 (2000) Università di Catania 2D 3D TSV
10843222 17 Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton.EBI Bioorg Med Chem Lett 10: 1081-4 (2000) University of Tokyo 2D 3D TSV
10843221 4 Examination of N-hydroxylation as a prerequisite mechanism of nitric oxide synthase inactivation.EBI Bioorg Med Chem Lett 10: 1077-80 (2000) University at Buffalo 2D 3D TSV
10843219 20 Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.EBI Bioorg Med Chem Lett 10: 1069-72 (2000) Merck Research Laboratories 2D 3D TSV
10843217 24 Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.EBI Bioorg Med Chem Lett 10: 1063-6 (2000) R.W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10843211 38 Structure-activity relationship studies of flavopiridol analogues.EBI Bioorg Med Chem Lett 10: 1037-41 (2000) Mitotix Inc. 2D 3D TSV
10843204 1 Synthesis of glycolipid analogues that disrupt binding of HIV-1 gp120 to galactosylceramide.EBI Bioorg Med Chem Lett 10: 1011-4 (2000) Cornell University 2D 3D TSV
10843203 12 Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.EBI Bioorg Med Chem Lett 10: 1007-10 (2000) Glaxo Wellcome 2D 3D TSV
10841807 6 Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues.EBI J Med Chem 43: 2280-4 (2000) Laboratorios Menarini 2D 3D TSV
10841802 4 Novel inhibitors of nucleoside triphosphate diphosphohydrolases: chemical synthesis and biochemical and pharmacological characterizations.EBI J Med Chem 43: 2239-47 (2000) Universit£ de Sherbrooke 2D 3D TSV
10841801 33 Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.EBI J Med Chem 43: 2227-38 (2000) Vrije Universiteit 2D 3D TSV
10841800 4 Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.EBI J Med Chem 43: 2217-26 (2000) NeuroSearch A/S 2D 3D TSV
10841798 64 Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.EBI J Med Chem 43: 2196-203 (2000) National Institute of Diabetes 2D 3D TSV
10841797 110 Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI J Med Chem 43: 2183-95 (2000) The R.W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10841794 12 Structure-activity relationships in a series of bisquaternary bisphthalimidine derivatives modulating the muscarinic M(2)-receptor allosterically.EBI J Med Chem 43: 2155-64 (2000) University of W�rzburg 2D 3D TSV
10841791 8 Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations.EBI J Med Chem 43: 2124-34 (2000) Universit£ di Napoli"Federico II" 2D 3D TSV
10841790 24 Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.EBI J Med Chem 43: 2115-23 (2000) Istituto di Chimica Farmaceutica e Tossicologica 2D 3D TSV
10841789 48 Developing a dynamic pharmacophore model for HIV-1 integrase.EBI J Med Chem 43: 2100-14 (2000) University of California 2D 3D TSV
10832613 26 [3H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D3 receptors.BDB Naunyn Schmiedebergs Arch Pharmacol 361: 569-72 (2000) Croissy-sur-Seine Paris 2D 3D TSV
10825466 2 Role of organic cation transporters in the renal secretion of nucleosides.EBI Biochem Pharmacol 60: 215-9 (2000) The University of Texas M. D. Anderson Cancer Center 2D 3D TSV
10821800 61 Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors.BDB Br J Pharmacol 130: 692-8 (2000) Friedrich-Schiller-University Jena 2D 3D TSV
10821720 8 7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.EBI J Med Chem 43: 2079-81 (2000) University of Bonn 2D 3D TSV
10821718 69 Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.EBI J Med Chem 43: 2064-71 (2000) Georgetown University Medical Center 2D 3D TSV
10821717 29 Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety.EBI J Med Chem 43: 2049-63 (2000) Takeda Chemical Industries, Ltd. 2D 3D TSV
10821715 34 A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family.EBI J Med Chem 43: 2031-9 (2000) University of California 2D 3D TSV
10821714 29 Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.BDB J Med Chem 43: 2019-30 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10821713 23 SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.BDB J Med Chem 43: 2007-18 (2000) University of Bologna 2D 3D TSV
10821712 18 Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.EBI J Med Chem 43: 1993-2006 (2000) NeoGenesis, Inc. 2D 3D TSV
10821708 138 4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.EBI J Med Chem 43: 1958-68 (2000) Lilly, S.A. 2D 3D TSV
10821707 26 Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives.EBI J Med Chem 43: 1949-57 (2000) CNRS UMR 8532 2D 3D TSV
10821705 27 Synthesis and evaluation of"AZT-HEPT","AZT-pyridinone", and"ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.EBI J Med Chem 43: 1927-39 (2000) UMR 176 CNRS/Institut Curie 2D 3D TSV
10821704 22 Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).EBI J Med Chem 43: 1910-26 (2000) Institute of Cancer Research 2D 3D TSV
10821703 8 Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists.EBI J Med Chem 43: 1901-9 (2000) Jagiellonian University 2D 3D TSV
10820137 13 Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.EBI Drug Metab Dispos 28: 655-60 (2000) Vanderbilt University School of Medicine 2D 3D TSV
10818260 13 Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806.BDB Neuropharmacology 39: 1443-50 (2000) University of Cambridge 2D 3D TSV
10794706 24 Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.EBI J Med Chem 43: 1892-7 (2000) CoCensys, Inc. 2D 3D TSV
10794705 13 Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.BDB J Med Chem 43: 1886-91 (2000) Universita degli Studi di Roma La Sapienza 2D 3D TSV
10794704 1 Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.EBI J Med Chem 43: 1878-85 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10794702 340 Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.EBI J Med Chem 43: 1858-65 (2000) Università degli Studi 2D 3D TSV
10794701 48 Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.EBI J Med Chem 43: 1852-7 (2000) University of Bristol 2D 3D TSV
10794700 40 1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.BDB J Med Chem 43: 1841-51 (2000) Universitat des Saarlandes 2D 3D TSV
10794697 13 Multivariate data analysis using D-optimal designs, partial least squares, and response surface modeling: A directional approach for the analysis of farnesyltransferase inhibitors.EBI J Med Chem 43: 1807-16 (2000) Rhône-Poulenc Rorer S.A. 2D 3D TSV
10794696 233 Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.EBI J Med Chem 43: 1793-806 (2000) Universit£ degli Studi 2D 3D TSV
10794694 32 Design of a Gag pentapeptide analogue that binds human cyclophilin A more efficiently than the entire capsid protein: new insights for the development of novel anti-HIV-1 drugs.EBI J Med Chem 43: 1770-9 (2000) D�partement D'Ing�nierie et D'Etudes des Prot�ines 2D 3D TSV
10794692 15 Characterization of the binding site of the histamine H(3) receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide.EBI J Med Chem 43: 1754-61 (2000) Vrije Universiteit 2D 3D TSV
10794691 8 Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.EBI J Med Chem 43: 1741-53 (2000) Marshall University School of Medicine and Huntington VA Medical Center 2D 3D TSV
10794689 10 Design and synthesis of conformationally constrained glucagon analogues.EBI J Med Chem 43: 1714-22 (2000) University of Arizona 2D 3D TSV
10794688 16 New proline mimetics: synthesis of thrombin inhibitors incorporating cyclopentane- and cyclopentenedicarboxylic acid templates in the P2 position. Binding conformation investigated by X-ray crystallography.EBI J Med Chem 43: 1705-13 (2000) Link£ping University 2D 3D TSV
10794686 19 Probing the conformation of the sugar transport inhibitor phlorizin by 2D-NMR, molecular dynamics studies, and pharmacophore analysis.EBI J Med Chem 43: 1692-8 (2000) Max-Planck-Institut f£r molekulare Physiologie 2D 3D TSV
10794685 42 Molecular determinants of MAO selectivity in a series of indolylmethylamine derivatives: biological activities, 3D-QSAR/CoMFA analysis, and computational simulation of ligand recognition.EBI J Med Chem 43: 1684-91 (2000) Universitat Autònoma de Barcelona 2D 3D TSV
10794684 34 Substituted benzamide inhibitors of human rhinovirus 3C protease: structure-based design, synthesis, and biological evaluation.EBI J Med Chem 43: 1670-83 (2000) Agouron Pharmaceuticals Inc. 2D 3D TSV
10794683 36 Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration.EBI J Med Chem 43: 1664-9 (2000) Novo Nordisk A/S 2D 3D TSV
10794682 4 N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration.EBI J Med Chem 43: 1661-3 (2000) Pfizer Inc. 2D 3D TSV
10794681 43 Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.EBI J Med Chem 43: 1641-60 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10785418 10 Halogenated boldine derivatives with enhanced monoamine receptor selectivity.EBI J Nat Prod 63: 480-4 (2000) Universidad de Chile 2D 3D TSV
10782696 67 ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.EBI Bioorg Med Chem Lett 10: 831-4 (2000) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10782692 8 Leukotriene B4 photoaffinity probes: design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes.EBI Bioorg Med Chem Lett 10: 811-4 (2000) UPRESA-CNRS 5074 2D 3D TSV
10782691 1 Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.EBI Bioorg Med Chem Lett 10: 805-9 (2000) Laboratoires UPSA 2D 3D TSV
10782686 13 The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.EBI Bioorg Med Chem Lett 10: 783-6 (2000) Wyeth-Ayerst Research 2D 3D TSV
10782685 9 Synthesis of a cyanopeptide-analogue with trypsin activating properties.EBI Bioorg Med Chem Lett 10: 779-81 (2000) Institute of Pharmacy, Ernst-Moritz-Arndt-University, Pharmaceutical/Medicinal Chemistry, Greifswald, Germany. radau@pharmazie.uni-greifswald.de 2D 3D TSV
10782682 10 QSAR of 1,1'-(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors: a different approach for antiproliferative drug design.EBI Bioorg Med Chem Lett 10: 767-70 (2000) Granada 2D 3D TSV
10782677 73 Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI Bioorg Med Chem Lett 10: 745-9 (2000) Corvas International, Inc. 2D 3D TSV
10782674 65 N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.EBI Bioorg Med Chem Lett 10: 729-33 (2000) Hoffmann-La Roche Inc. 2D 3D TSV
10782673 17 N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.EBI Bioorg Med Chem Lett 10: 725-7 (2000) Roche Research Center 2D 3D TSV
10782670 11 Alpha-ketoamides, alpha-ketoesters and alpha-diketones as HCV NS3 protease inhibitors.EBI Bioorg Med Chem Lett 10: 711-3 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10782669 7 Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.EBI Bioorg Med Chem Lett 10: 707-10 (2000) NIDDK 2D 3D TSV
10782666 46 The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.EBI Bioorg Med Chem Lett 10: 695-8 (2000) Wyeth-Ayerst Research 2D 3D TSV
10782664 42 Isoxazolines and isoxazoles as factor Xa inhibitors.EBI Bioorg Med Chem Lett 10: 685-9 (2000) The DuPont Pharmaceuticals Company 2D 3D TSV
10780918 27 Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.EBI J Med Chem 43: 1611-9 (2000) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10780916 134 Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).EBI J Med Chem 43: 1586-603 (2000) Abbott Laboratories 2D 3D TSV
10780914 37 Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.EBI J Med Chem 43: 1573-6 (2000) University of Minnesota 2D 3D TSV
10780912 7 Structural studies on bioactive compounds. 32. Oxidation of tyrphostin protein tyrosine kinase inhibitors with hypervalent iodine reagents.EBI J Med Chem 43: 1550-62 (2000) University of Nottingham 2D 3D TSV
10780910 44 Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.EBI J Med Chem 43: 1533-40 (2000) Université Paris-Sud 2D 3D TSV
10780908 40 AMP deaminase inhibitors. 4. Further N3-substituted coformycin aglycon analogues: N3-alkylmalonates as ribose 5'-monophosphate mimetics.EBI J Med Chem 43: 1519-24 (2000) Metabasis Therapeutics Inc. 2D 3D TSV
10780907 63 AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues.EBI J Med Chem 43: 1508-18 (2000) Metabasis Therapeutics Inc. 2D 3D TSV
10780906 94 AMP deaminase inhibitors. 2. Initial discovery of a non-nucleotide transition-state inhibitor series.EBI J Med Chem 43: 1495-507 (2000) Metabasis Therapeutics Inc. 2D 3D TSV
10780903 6 Study on selectin blocker. 8. Lead discovery of a non-sugar antagonist using a 3D-pharmacophore model.EBI J Med Chem 43: 1476-83 (2000) Nippon Organon K.K. 2D 3D TSV
10780900 5 A study of the relationship between biological activity and prolyl amide isomer geometry in oxytocin using 5-tert-butylproline to augment the Cys(6)-Pro(7) amide cis-isomer population.EBI J Med Chem 43: 1448-55 (2000) Université de Montréal 2D 3D TSV
10780899 16 GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.EBI J Med Chem 43: 1427-47 (2000) University of Sydney 2D 3D TSV
10779411 24 Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.BDB Chem Biol 7: 299-312 (2000) Axys Pharmaceutical 2D 3D TSV
10779381 34 [(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.BDB Mol Pharmacol 57: 968-75 (2000) University of Ferrara 2D 3D TSV
10777579 12 Thermodynamic consequences of grafting enhanced affinity toward the mutated antigen onto an antibody. The case of anti-lysozyme antibody, HyHEL-10.BDB J Biol Chem 275: 12813-20 (2000) Tohoku University 2D 3D TSV
10777500 4 Distinct Ca2+ binding properties of novel C2 domains of plant phospholipase dalpha and beta.BDB J Biol Chem 275: 19700-6 (2000) Kansas State University 2D 3D TSV
10773045 45 Characterization of a tropane radioligand, [(3)H]2beta-propanoyl-3beta-(4-tolyl) tropane ([(3)H]PTT), for dopamine transport sites in rat brain.BDB J Pharmacol Exp Ther 293: 686-96 (2000) Wake Forest University 2D 3D TSV
10773005 2 Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.EBI J Pharmacol Exp Ther 293: 376-82 (2000) Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology 2D 3D TSV
10762053 2 Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.EBI Bioorg Med Chem Lett 10: 681-4 (2000) Università di Ferrara 2D 3D TSV
10762051 66 Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties.EBI Bioorg Med Chem Lett 10: 673-6 (2000) Universit£ degli Studi 2D 3D TSV
10762050 4 Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties.EBI Bioorg Med Chem Lett 10: 669-72 (2000) INSERM 2D 3D TSV
10762046 7 Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.EBI Bioorg Med Chem Lett 10: 653-5 (2000) National Cancer Institute 2D 3D TSV
10762045 65 The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity.EBI Bioorg Med Chem Lett 10: 649-52 (2000) Pharmacia & Upjohn Company 2D 3D TSV
10762042 8 Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.EBI Bioorg Med Chem Lett 10: 637-9 (2000) C.N.R.S. 2D 3D TSV
10762041 6 Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi.EBI Bioorg Med Chem Lett 10: 631-5 (2000) Université Lille II 2D 3D TSV
10762040 22 Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.EBI Bioorg Med Chem Lett 10: 627-30 (2000) University of Tennessee 2D 3D TSV
10762039 3 Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.EBI Bioorg Med Chem Lett 10: 623-5 (2000) Eisai Co., Ltd. 2D 3D TSV
10762038 3 Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.EBI Bioorg Med Chem Lett 10: 619-22 (2000) Eisai Co. Ltd. 2D 3D TSV
10762037 6 Synthesis of a novel class of cdc25A inhibitors from vitamin D3.EBI Bioorg Med Chem Lett 10: 615-7 (2000) The University of Tokyo 2D 3D TSV
10757731 3 Two new prenylated 3-benzoxepin derivatives as cyclooxygenase inhibitors from Perilla frutescens var. acuta.EBI J Nat Prod 63: 403-5 (2000) Columbia University 2D 3D TSV
10757728 2 Isolation of psammaplin A 11'-sulfate and bisaprasin 11'-sulfate from the marine sponge Aplysinella rhax.EBI J Nat Prod 63: 393-5 (2000) Griffith University 2D 3D TSV
10757727 2 Three new triterpenoids from Peganum nigellastrum.EBI J Nat Prod 63: 390-2 (2000) Toho University 2D 3D TSV
10757710 5 Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.EBI J Nat Prod 63: 318-21 (2000) Griffith University 2D 3D TSV
10757709 8 Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.EBI J Nat Prod 63: 315-7 (2000) Leiden University 2D 3D TSV
10755640 2 18F-labeled FECNT: a selective radioligand for PET imaging of brain dopamine transporters.BDB Nucl Med Biol 27: 1-12 (2000) Emory University 2D 3D TSV
10754449 5 In vitro pharmacological profile of SK-896, a new human motilin analogue.BDB Pharmacology 60: 128-35 (2000) Sanwa Kagaku Kenkyusho Co., Ltd. 2D 3D TSV
10753480 27 Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI J Med Chem 43: 1423-6 (2001) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10753476 84 Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.EBI J Med Chem 43: 1398-408 (2001) INSERM 2D 3D TSV
10753475 61 Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.EBI J Med Chem 43: 1380-97 (2001) University of Auckland 2D 3D TSV
10753473 14 Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.EBI J Med Chem 43: 1359-66 (2001) Hungarian Academy of Sciences 2D 3D TSV
10753471 64 Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.EBI J Med Chem 43: 1339-49 (2001) Uppsala University 2D 3D TSV
10753470 95 High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.EBI J Med Chem 43: 1329-38 (2001) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10753467 118 Novel benzofuran and benzothiophene biphenyls as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.EBI J Med Chem 43: 1293-310 (2001) Wyeth-Ayerst Research 2D 3D TSV
10753466 15 Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.BDB J Med Chem 43: 1282-92 (2000) Institut Curie 2D 3D TSV
10753465 8 Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing.EBI J Med Chem 43: 1271-81 (2001) University of Queensland 2D 3D TSV
10753463 5 N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.EBI J Med Chem 43: 1257-63 (2001) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10753461 13 Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.EBI J Med Chem 43: 1251-2 (2001) University of Minnesota 2D 3D TSV
10747922 12 Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study.BDB J Biol Chem 275: 16139-45 (2000) Swiss Federal Institute of Technology 2D 3D TSV
10746010 54 Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.BDB J Comb Chem 1: 207-15 SmithKline Beecham Pharmaceuticals 2D 3D TSV
10743959 48 N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.EBI Bioorg Med Chem Lett 10: 509-12 (2000) Yoshitomi Pharmaceutical Industries, Ltd. 2D 3D TSV
10743958 4 Solid phase synthesis of diamides as potential bone resorption inhibitors.EBI Bioorg Med Chem Lett 10: 503-7 (2000) AstraZeneca R&D M£lndal 2D 3D TSV
10743957 98 Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.EBI Bioorg Med Chem Lett 10: 499-502 (2000) Università degli Studi 2D 3D TSV
10743955 2 Selection of a potent inhibitor of trihydroxynaphthalene reductase by sorting disease control data.EBI Bioorg Med Chem Lett 10: 491-4 (2000) DuPont Central Research and Development 2D 3D TSV
10743953 1 The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.EBI Bioorg Med Chem Lett 10: 483-6 (2000) State University of New York 2D 3D TSV
10743952 2 The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives.EBI Bioorg Med Chem Lett 10: 477-81 (2000) State University of New York 2D 3D TSV
10743951 9 Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.EBI Bioorg Med Chem Lett 10: 473-6 (2000) Albany Molecular Research 2D 3D TSV
10743949 76 (1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.EBI Bioorg Med Chem Lett 10: 465-8 (2000) Università di Perugia 2D 3D TSV
10743948 22 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.EBI Bioorg Med Chem Lett 10: 461-4 (2000) Ewha Womans University 2D 3D TSV
10743947 12 Synthesis and characterization of a novel class of protein tyrosine phosphatase inhibitors.EBI Bioorg Med Chem Lett 10: 457-60 (2000) New York University 2D 3D TSV
10743946 7 Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities.EBI Bioorg Med Chem Lett 10: 453-5 (2000) Medical University of South Carolina 2D 3D TSV
10743945 21 Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.EBI Bioorg Med Chem Lett 10: 449-52 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10743944 68 Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.EBI Bioorg Med Chem Lett 10: 443-7 (2000) Merck Research Laboratories 2D 3D TSV
10743942 7 Design and synthesis of mimics of S-adenosyl-L-homocysteine as potential inhibitors of erythromycin methyltransferases.EBI Bioorg Med Chem Lett 10: 433-7 (2000) Université de Montréal 2D 3D TSV
10743939 63 Synthesis and biological activities of NB-506 analogues modified at the glucose group.EBI Bioorg Med Chem Lett 10: 419-22 (2000) Banyu Tsukuba Research Institute 2D 3D TSV
10743938 103 Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.EBI Bioorg Med Chem Lett 10: 415-8 (2000) Ligand Pharmaceuticals 2D 3D TSV
10743937 66 Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.EBI Bioorg Med Chem Lett 10: 411-4 (2000) Ligand Pharmaceuticals 2D 3D TSV
10743936 2 Irreversible inhibition of type I dehydroquinase by substrates for type II dehydroquinase.EBI Bioorg Med Chem Lett 10: 407-9 (2000) University Chemical Laboratory 2D 3D TSV
10741563 4 Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.EBI Bioorg Med Chem Lett 10: 605-7 (2000) University of Bristol 2D 3D TSV
10741562 60 1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2.EBI Bioorg Med Chem Lett 10: 601-4 (2000) The R.W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10741561 48 Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.EBI Bioorg Med Chem Lett 10: 597-600 (2000) Glaxo Wellcome Research and Development 2D 3D TSV
10741557 26 Naphthyl ketones: a new class of Janus kinase 3 inhibitors.EBI Bioorg Med Chem Lett 10: 575-9 (2000) AstraZeneca 2D 3D TSV
10741555 9 2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.EBI Bioorg Med Chem Lett 10: 567-9 (2000) Universität Hamburg 2D 3D TSV
10741553 8 Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.EBI Bioorg Med Chem Lett 10: 559-62 (2000) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10741546 66 Parallel synthesis of a series of subtype-selective NMDA receptor antagonists.EBI Bioorg Med Chem Lett 10: 527-9 (2000) Parke-Davis Pharmaceutical Research 2D 3D TSV
10741545 36 Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.EBI Bioorg Med Chem Lett 10: 523-6 (2000) Pfizer Inc 2D 3D TSV
10737756 1 Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.EBI J Med Chem 43: 1234-41 (2000) Merck Research Laboratories 2D 3D TSV
10737754 30 Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.EBI J Med Chem 43: 1215-22 (2000) Georgetown University Medical Center 2D 3D TSV
10737750 7 SH2-directed ligands of the Lck tyrosine kinase.EBI J Med Chem 43: 1173-9 (2000) The Albert Einstein College of Medicine 2D 3D TSV
10737749 182 Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.EBI J Med Chem 43: 1165-72 (2000) National Institute of Diabetes 2D 3D TSV
10737748 81 1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.EBI J Med Chem 43: 1158-64 (2000) Universita' di Firenze 2D 3D TSV
10737747 54 5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.EBI J Med Chem 43: 1149-57 (2000) Merck KGaA 2D 3D TSV
10737745 20 Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.EBI J Med Chem 43: 1135-42 (2000) ARIAD Gene Therapeutics 2D 3D TSV
10737744 146 Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.EBI J Med Chem 43: 1123-34 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10737742 23 2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.BDB J Med Chem 43: 1094-108 (2000) Boehringer Ingelheim Pharmaceuticals Inc. 2D 3D TSV
10737741 50 Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.EBI J Med Chem 43: 1085-93 (2000) National Institute on Drug Abuse-Intramural Research Program 2D 3D TSV
10737740 57 Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.EBI J Med Chem 43: 1071-84 (2000) Freie Universit£t Berlin 2D 3D TSV
10737739 11 Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.EBI J Med Chem 43: 1062-70 (2000) National Eye Institute 2D 3D TSV
10737738 78 Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.EBI J Med Chem 43: 1050-61 (2000) King's College London 2D 3D TSV
10737736 19 Pyrrolidine inhibitors of human cytosolic phospholipase A(2).EBI J Med Chem 43: 1041-4 (2000) Shionogi & Company, Ltd. 2D 3D TSV
10732980 96 Protease inhibitors. Part 8: synthesis of potent Clostridium histolyticum collagenase inhibitors incorporating sulfonylated L-alanine hydroxamate moieties.BDB Bioorg Med Chem 8: 637-45 (2000) Universita degli Studi di Firenze 2D 3D TSV
10732965 25 Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives.BDB Bioorg Med Chem 8: 497-506 (2000) University of Bologna 2D 3D TSV
10729360 1 Inhibition of the P-glycoprotein- and multidrug resistance protein-mediated efflux of anthracyclines and calceinacetoxymethyl ester by PAK-104P.EBI Eur J Pharmacol 391: 207-16 (2000) Universit£ Paris Nord 2D 3D TSV
10715167 8 Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.BDB J Med Chem 43: 1034-40 (2000) Upjohn 2D 3D TSV
10715164 57 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.EBI J Med Chem 43: 1011-8 (2000) Virginia Commonwealth University 2D 3D TSV
10715163 35 New azolidinediones as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.EBI J Med Chem 43: 995-1010 (2000) Wyeth-Ayerst Research 2D 3D TSV
10715162 59 Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.EBI J Med Chem 43: 984-94 (2000) CoCensys, Inc. 2D 3D TSV
10715159 112 Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.EBI J Med Chem 43: 945-52 (2000) Procter and Gamble Pharmaceuticals 2D 3D TSV
10715158 31 Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?EBI J Med Chem 43: 921-44 (2000) National Cancer Institute 2D 3D TSV
10715157 16 Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.EBI J Med Chem 43: 911-20 (2000) National Cancer Institute 2D 3D TSV
10715156 35 Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.EBI J Med Chem 43: 900-10 (2000) Rhône-Poulenc Rorer 2D 3D TSV
10715152 155 5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.EBI J Med Chem 43: 843-58 (2000) Warner-Lambert Company 2D 3D TSV
10715151 22 Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands.EBI J Med Chem 43: 829-42 (2000) National Institute of Diabetes 2D 3D TSV
10715150 5 Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling.EBI J Med Chem 43: 819-28 (2000) Salk Institute 2D 3D TSV
10715149 46 Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI J Med Chem 43: 807-18 (2000) Salk Institute 2D 3D TSV
10715148 27 Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI J Med Chem 43: 797-806 (2000) Salk Institute 2D 3D TSV
10715147 41 Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists.EBI J Med Chem 43: 784-96 (2000) Salk Institute 2D 3D TSV
10715145 9 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.EBI J Med Chem 43: 775-7 (2000) Searle Research and Development 2D 3D TSV
10715144 5 Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.EBI J Med Chem 43: 772-4 (2000) Georgetown University Medical Center 2D 3D TSV
10715143 16 1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.EBI J Med Chem 43: 769-71 (2000) Novartis Institute for Medical Sciences 2D 3D TSV
10715142 35 alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI J Med Chem 43: 765-8 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10714510 36 The discovery and synthesis of highly potent, A2a receptor agonists.EBI Bioorg Med Chem Lett 10: 403-6 (2000) Glaxo Wellcome Medicines Research Centre 2D 3D TSV
10714509 4 Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor.EBI Bioorg Med Chem Lett 10: 399-402 (2000) Health Care Discovery& Preclinical Development, Novo Nordisk A/S, Mlv, Denmark. 2D 3D TSV
10714508 41 2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2.EBI Bioorg Med Chem Lett 10: 395-8 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10714507 1 Mechanism-based inactivation of thymidylate synthase by 5-(3-fluoropropyn-1-yl)-2'-deoxyuridine 5'-phosphate.EBI Bioorg Med Chem Lett 10: 391-4 (2000) State University of New York 2D 3D TSV
10714506 13 Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere.EBI Bioorg Med Chem Lett 10: 385-9 (2000) Eli Lilly and Company 2D 3D TSV
10714503 18 Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.EBI Bioorg Med Chem Lett 10: 373-5 (2000) Sankyo Co., Ltd. 2D 3D TSV
10714498 13 Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1.EBI Bioorg Med Chem Lett 10: 353-6 (2000) Università di Firenze 2D 3D TSV
10714496 4 Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA.EBI Bioorg Med Chem Lett 10: 345-7 (2000) Parke-Davis Neuroscience Research Centre 2D 3D TSV
10714492 21 2-Methyladenosine-Substituted 2',5'-oligoadenylates: conformations, 2-5A binding and catalytic activities with human ribonuclease L.EBI Bioorg Med Chem Lett 10: 329-31 (2000) Gifu University 2D 3D TSV
10708730 14 Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.BDB Eur J Pharmacol 390: 245-8 (2000) Lilly Research Laboratories 2D 3D TSV
10698459 41 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI Bioorg Med Chem Lett 10: 301-4 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10698458 26 Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.EBI Bioorg Med Chem Lett 10: 297-300 (2000) Georgetown University Medical Center 2D 3D TSV
10698455 13 Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2.EBI Bioorg Med Chem Lett 10: 285-8 (2000) Univ. de Valencia 2D 3D TSV
10698454 13 Probing the extended binding determinants of oligosaccharyl transferase with synthetic inhibitors of asparagine-linked glycosylation.EBI Bioorg Med Chem Lett 10: 281-4 (2000) Institute of Technology 2D 3D TSV
10698453 8 A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 2,3-disubstituted-4-phenylquinolines.EBI Bioorg Med Chem Lett 10: 277-9 (2000) Searle Discovery 2D 3D TSV
10698452 7 3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.EBI Bioorg Med Chem Lett 10: 273-5 (2000) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10698450 21 Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.BDB Bioorg Med Chem Lett 10: 265-8 (2000) Medivir AB 2D 3D TSV
10698448 24 N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.EBI Bioorg Med Chem Lett 10: 257-60 (2000) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10698447 6 1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.BDB Bioorg Med Chem Lett 10: 253-6 (2000) Universita degli Studi di Roma La Sapienza 2D 3D TSV
10698445 11 Exploring the chiral space within the active site of alpha-thrombin with a constrained mimic of D-Phe-Pro-Arg--design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex.EBI Bioorg Med Chem Lett 10: 243-7 (2000) Universit£ de Montr£al 2D 3D TSV
10698443 19 Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.EBI Bioorg Med Chem Lett 10: 235-8 (2000) Merck Research Laboratories 2D 3D TSV
10698440 12 The discovery of potent cRaf1 kinase inhibitors.EBI Bioorg Med Chem Lett 10: 223-6 (2000) Glaxo Wellcome 2D 3D TSV
10698439 68 Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI Bioorg Med Chem Lett 10: 217-21 (2000) Rhone-Poulenc Rorer 2D 3D TSV
10698438 12 N-(sulfonamido)alkyl[tetrahydro-1H-benzo[e]indol-2-yl]amines: potent antagonists of human neuropeptide Y Y5 receptor.EBI Bioorg Med Chem Lett 10: 213-6 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10698437 7 Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.EBI Bioorg Med Chem Lett 10: 209-11 (2000) Università di Ferrara 2D 3D TSV
10698436 1 Preparation of 5-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyloxy)-6-hydroxynap htho[2,3- f]quinoline-7,12-dione (FT-Alz), a new-type, potentially antitumor substance with various biological activities.EBI Bioorg Med Chem Lett 10: 203-7 (2000) Institute of Bioorganic Chemistry, Kawasaki, Japan. 2D 3D TSV
10698435 150 Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.EBI Bioorg Med Chem Lett 10: 199-201 (2000) Kyoto Pharmaceutical University 2D 3D TSV
10694412 15 Thermodynamics of substrate binding to the chaperone SecB.BDB Biochemistry 39: 2420-7 (2000) Indian Institute of Science 2D 3D TSV
10692507 41 5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.BDB Mol Pharmacol 57: 642-9 (2000) National Institute on Drug Abuse 2D 3D TSV
10691728 2 Cernuosides A and B, two sucrase inhibitors from Pulsatilla cernua.EBI J Nat Prod 63: 276-8 (2000) China Pharmaceutical University 2D 3D TSV
10691700 112 Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.EBI J Med Chem 43: 756-62 (2000) Friedrich-Alexander University 2D 3D TSV
10691697 133 Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.EBI J Med Chem 43: 721-35 (2000) Searle Research and Development 2D 3D TSV
10691696 14 A new class of conformationally rigid analogues of 4-amino-5-halopentanoic acids, potent inactivators of gamma-aminobutyric acid aminotransferase.EBI J Med Chem 43: 706-20 (2000) Northwestern University 2D 3D TSV
10691695 85 Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.EBI J Med Chem 43: 690-705 (2000) Abbott Laboratories 2D 3D TSV
10691694 9 Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: first phosphodiesterase 7 inhibitors.EBI J Med Chem 43: 683-9 (2000) Instituto de Química Médica 2D 3D TSV
10691693 64 Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.EBI J Med Chem 43: 675-82 (2000) Novartis Pharma AG 2D 3D TSV
10691692 60 Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors.EBI J Med Chem 43: 664-74 (2000) University College London 2D 3D TSV
10691690 6 Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography.EBI J Med Chem 43: 639-48 (2000) Emory University 2D 3D TSV
10691684 20 Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.BDB J Med Chem 43: 581-90 (2000) University of Tennessee at Memphis 2D 3D TSV
10691683 22 Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.EBI J Med Chem 43: 569-80 (2000) University of Arizona 2D 3D TSV
10691681 17 Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.EBI J Med Chem 43: 551-9 (2000) Clinical Research Institute of Montr£al 2D 3D TSV
10691680 72 The PPARs: from orphan receptors to drug discovery.EBI J Med Chem 43: 527-50 (2000) Glaxo Wellcome Research & Development 2D 3D TSV
10688634 12 Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).EBI J Pharmacol Exp Ther 292: 1146-52 (2000) University of California 2D 3D TSV
10688601 21 Cloning and pharmacological characterization of the rat CB(2) cannabinoid receptor.BDB J Pharmacol Exp Ther 292: 886-94 (2000) Virginia Commonwealth University 2D 3D TSV
10673109 9 Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.EBI Bioorg Med Chem Lett 10: 193-5 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10673107 63 8-Aminocyclazocine analogues: synthesis and structure-activity relationships.EBI Bioorg Med Chem Lett 10: 183-7 (2000) Institute 2D 3D TSV
10673106 28 RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.EBI Bioorg Med Chem Lett 10: 179-82 (2000) Hoechst Marion Roussel Deutschland GmhH 2D 3D TSV
10673105 38 Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.EBI Bioorg Med Chem Lett 10: 175-8 (2000) Synaptic Pharmaceutical Corporation 2D 3D TSV
10673103 55 Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.EBI Bioorg Med Chem Lett 10: 167-70 (2000) AstraZeneca R&D Montréal 2D 3D TSV
10673101 10 The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein.EBI Bioorg Med Chem Lett 10: 157-60 (2000) Universit£ Claude Bernard-Lyon 1 2D 3D TSV
10673099 34 Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.EBI Bioorg Med Chem Lett 10: 147-51 (2000) Wyeth-Ayerst Research 2D 3D TSV
10673095 2 First enantiospecific synthesis of a 3,4-dihydroxy-L-glutamic acid [(3S,4S)-DHGA], a new mGluR1 agonist.EBI Bioorg Med Chem Lett 10: 129-33 (2000) CNRS 2D 3D TSV
10669578 44 New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.EBI J Med Chem 43: 517-25 (2000) University of Groningen 2D 3D TSV
10669576 65 Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.EBI J Med Chem 43: 488-504 (2000) Novartis Institute for Biomedical Research 2D 3D TSV
10669572 14 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.EBI J Med Chem 43: 449-56 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10669571 24 Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.EBI J Med Chem 43: 440-8 (2000) University of Würzburg 2D 3D TSV
10669570 8 Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.EBI J Med Chem 43: 432-9 (2000) University of Groningen 2D 3D TSV
10669568 27 Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.EBI J Med Chem 43: 409-19 (2000) Eisai Co., Ltd. 2D 3D TSV
10669567 5 Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.EBI J Med Chem 43: 401-8 (2000) Mayo Medical School and Mayo Clinic 2D 3D TSV
10669566 53 Derivation of pharmacophore and CoMFA models for leukotriene D(4) receptor antagonists of the quinolinyl(bridged)aryl series.EBI J Med Chem 43: 392-400 (2000) Laboratorios Menarini 2D 3D TSV
10669565 20 Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.EBI J Med Chem 43: 381-91 (2000) University of Minnesota 2D 3D TSV
10669564 189 Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.EBI J Med Chem 43: 369-80 (2000) Procter and Gamble Pharmaceuticals 2D 3D TSV
10669563 7 Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.EBI J Med Chem 43: 361-8 (2000) Warner-Lambert Company 2D 3D TSV
10669562 29 Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.EBI J Med Chem 43: 351-60 (2000) Georgetown University Medical Center 2D 3D TSV
10669561 23 alpha-Substituted N-(sulfonamido)alkyl-beta-aminotetralins: potent and selective neuropeptide Y Y5 receptor antagonists.EBI J Med Chem 43: 346-50 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10669560 89 A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).BDB J Med Chem 43: 342-5 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10669559 180 Protease inhibitors: current status and future prospects.EBI J Med Chem 43: 305-41 (2000) University of Queensland 2D 3D TSV
10662686 6 Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.BDB Chem Biol 7: 27-38 (2000) University of California, San Francisco 2D 3D TSV
10658583 50 Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.BDB Bioorg Med Chem 7: 2775-800 (1999) Parke-Davis Pharmaceutical Research 2D 3D TSV
10654414 6 DNA polymerase beta inhibitors from Tetracera boiviniana.EBI J Nat Prod 62: 1660-3 (2000) University of Virginia 2D 3D TSV
10654412 8 DNA polymerase beta inhibitors from Baeckea gunniana.EBI J Nat Prod 62: 1624-6 (2000) University of Virginia 2D 3D TSV
10650073 2 Dimerization of resveratrol by the grapevine pathogen Botrytis cinerea.EBI J Nat Prod 63: 29-33 (2000) University of Louisiana at Monroe 2D 3D TSV
10649985 390 Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes.EBI J Med Chem 43: 292-300 (2000) Università degli Studi 2D 3D TSV
10649982 54 A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.EBI J Med Chem 43: 270-7 (2000) Universitá di Bari 2D 3D TSV
10649980 52 N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.EBI J Med Chem 43: 250-60 (2000) Universit£ di Camerino 2D 3D TSV
10649977 72 Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.EBI J Med Chem 43: 214-23 (2000) Rhône-Poulenc Rorer 2D 3D TSV
10649976 72 Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.EBI J Med Chem 43: 205-13 (2000) Massachusetts General Hospital 2D 3D TSV
10649973 30 3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.EBI J Med Chem 43: 177-89 (2000) Otsuka Pharmaceutical Company Ltd. 2D 3D TSV
10649972 104 Antitumor agents. 199. Three-dimensional quantitative structure-activity relationship study of the colchicine binding site ligands using comparative molecular field analysis.EBI J Med Chem 43: 167-76 (2000) University of North Carolina at Chapel Hill 2D 3D TSV
10649971 180 Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.EBI J Med Chem 43: 156-66 (2000) Parke-Davis Pharmaceutical Research 2D 3D TSV
10649968 28 Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.EBI J Med Chem 43: 139-41 (2000) University of Bristol 2D 3D TSV
10648470 4 Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.EBI Gastroenterology 118: 422-30 (2000) University Hospital 2D 3D TSV
10646498 23 Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.BDB J Neurochem 74: 478-89 (2000) Janssen Research Foundation 2D 3D TSV
10639289 1 Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.EBI J Med Chem 42: 5475-81 (2000) University of Antwerp 2D 3D TSV
10639288 55 Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.BDB J Med Chem 42: 5464-74 (1999) Parke-Davis Pharmaceutical Research 2D 3D TSV
10639287 62 Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.EBI J Med Chem 42: 5455-63 (2000) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10639286 14 Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships.EBI J Med Chem 42: 5448-54 (2000) Heidelberg University 2D 3D TSV
10639285 13 2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.EBI J Med Chem 42: 5437-47 (2000) University of Leipzig 2D 3D TSV
10639284 119 Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.EBI J Med Chem 42: 5426-36 (2000) University of Florida 2D 3D TSV
10639283 135 Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.EBI J Med Chem 42: 5415-25 (2000) Berlex Biosciences 2D 3D TSV
10639281 13 Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.EBI J Med Chem 42: 5390-401 (2000) Universit¿a di Perugia 2D 3D TSV
10639280 101 Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.BDB J Med Chem 42: 5369-89 (1999) AstraZeneca 2D 3D TSV
10639279 26 Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.EBI J Med Chem 42: 5359-68 (2000) The University of Arizona 2D 3D TSV
10639276 6 Molecular recognition of modified adenine nucleotides by the P2Y(1)-receptor. 1. A synthetic, biochemical, and NMR approach.EBI J Med Chem 42: 5325-37 (2000) Bar-Ilan University 2D 3D TSV
10639181 68 Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.BDB Proc Natl Acad Sci U S A 97: 925-30 (2000) Vanderbilt University School of Medicine 2D 3D TSV
10636251 14 Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.EBI Bioorg Med Chem Lett 10: 87-90 (2000) Institute 2D 3D TSV
10636250 20 Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.EBI Bioorg Med Chem Lett 10: 83-5 (2000) 3-Dimensional Pharmaceuticals 2D 3D TSV
10636249 21 Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.EBI Bioorg Med Chem Lett 10: 79-82 (2000) 3-Dimensional Pharmaceutical, Inc. 2D 3D TSV
10636248 7 Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.EBI Bioorg Med Chem Lett 10: 75-8 (2000) University Hospital Zurich 2D 3D TSV
10636247 83 New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.EBI Bioorg Med Chem Lett 10: 71-4 (2000) Janssen Research Foundation 2D 3D TSV
10636245 4 Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams.EBI Bioorg Med Chem Lett 10: 63-6 (2000) University of Tokyo 2D 3D TSV
10636243 6 Synthesis and binding studies of some epibatidine analogues.EBI Bioorg Med Chem Lett 10: 55-8 (2000) Institute of Pharmacy and Biochemistry 2D 3D TSV
10636238 71 Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.EBI Bioorg Med Chem Lett 10: 35-8 (2000) Institut de Recherche Jouveinal-Parke Davis, Fresnes, France. yves.pascal@wl.com 2D 3D TSV
10636237 10 The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.EBI Bioorg Med Chem Lett 10: 31-4 (2000) ChemBridge Corporation 2D 3D TSV
10636235 13 Binding dynamics of two water molecules constrained within the scytalone dehydratase binding pocket.EBI Bioorg Med Chem Lett 10: 23-6 (2000) Stine-Haskell Research Center 2D 3D TSV
10636233 3 A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.EBI Bioorg Med Chem Lett 10: 17-8 (2000) University of Maryland 2D 3D TSV
10636232 58 Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.EBI Bioorg Med Chem Lett 10: 13-6 (2000) COR Therapeutics, Inc. 2D 3D TSV
10636230 12 Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.EBI Bioorg Med Chem Lett 10: 5-8 (2000) Merck Research Laboratories 2D 3D TSV
10636229 27 Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.EBI Bioorg Med Chem Lett 10: 1-4 (2000) 3-Dimensional Pharmaceuticals 2D 3D TSV
10634944 215 The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.BDB Biochim Biophys Acta 1483: 285-93 (2000) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10633045 1 Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.EBI J Med Chem 43: 133-8 (2000) Glaxo Wellcome Inc. 2D 3D TSV
10633043 27 Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids and esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents.EBI J Med Chem 43: 123-7 (2000) Glaxo Wellcome Research and Development 2D 3D TSV
10633042 30 Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.EBI J Med Chem 43: 114-22 (2000) Harvard Medical School 2D 3D TSV
10633039 718 Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.EBI J Med Chem 43: 71-95 (2000) University of Wisconsin-Milwaukee 2D 3D TSV
10633038 36 QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency.EBI J Med Chem 43: 59-70 (2000) Research Triangle Institute 2D 3D TSV
10633037 88 Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).EBI J Med Chem 43: 41-58 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10633036 79 Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).EBI J Med Chem 43: 27-40 (2000) DuPont Pharmaceuticals Company 2D 3D TSV
10633035 20 Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.EBI J Med Chem 43: 22-6 (2000) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10633034 5 Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.EBI J Med Chem 43: 19-21 (2000) Glaxo Wellcome Research and Development 2D 3D TSV
10632067 50 Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities.BDB Bioorg Med Chem 7: 2569-75 (1999) Hong Kong University of Science and Technology 2D 3D TSV
10632058 16 Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.BDB Bioorg Med Chem 7: 2487-97 (1999) University of Alabama at Birmingham 2D 3D TSV
10617681 11 Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine.BDB Mol Pharmacol 57: 75-81 (2000) The DuPont Pharmaceuticals Research Laboratories 2D 3D TSV
10617091 73 Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.EBI Bioorg Med Chem Lett 9: 3459-64 (2000) Corvas International, Inc. 2D 3D TSV
10617088 15 Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.EBI Bioorg Med Chem Lett 9: 3441-6 (2000) University of Louisville 2D 3D TSV
10617086 21 Delta opioid binding selectivity of 3-ether analogs of naltrindole.EBI Bioorg Med Chem Lett 9: 3435-8 (2000) National Institute of Diabetes 2D 3D TSV
10617082 15 N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.EBI Bioorg Med Chem Lett 9: 3411-6 (2000) Institute 2D 3D TSV
10617079 3 Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.EBI Bioorg Med Chem Lett 9: 3397-402 (1999) Laboratory of Aquatic Natural Products Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Japan. 2D 3D TSV
10612603 1 Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146.EBI Bioorg Med Chem Lett 9: 3381-6 (2000) Lilly Research Laboratories 2D 3D TSV
10612602 29 Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.EBI Bioorg Med Chem Lett 9: 3375-80 (2000) University of Illinois at Chicago 2D 3D TSV
10612601 30 4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine.EBI Bioorg Med Chem Lett 9: 3369-74 (2000) Merck, Sharp & Dohme Research Laboratories 2D 3D TSV
10612600 14 First fatty acylated dipeptides to affect muscarinic receptor ligand binding.EBI Bioorg Med Chem Lett 9: 3363-8 (2000) University of Toledo 2D 3D TSV
10612598 29 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI Bioorg Med Chem Lett 9: 3351-6 (2000) Celltech Therapeutics Limited 2D 3D TSV
10612597 31 Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.EBI Bioorg Med Chem Lett 9: 3347-50 (2000) Research Triangle Institute 2D 3D TSV
10612594 32 Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.EBI Bioorg Med Chem Lett 9: 3329-34 (2000) Glaxo Wellcome Research and Development 2D 3D TSV
10612593 33 N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.EBI Bioorg Med Chem Lett 9: 3325-8 (2000) Georgetown University Medical Center 2D 3D TSV
10612590 56 Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.EBI Bioorg Med Chem Lett 9: 3307-12 (2000) Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories 2D 3D TSV
10612589 22 Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.EBI Bioorg Med Chem Lett 9: 3301-6 (2000) Merck Research Laboratories 2D 3D TSV
10612586 34 Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.EBI Bioorg Med Chem Lett 9: 3285-90 (2000) Yoshitomi Pharmaceutical Industries, LTD. 2D 3D TSV
10612585 4 Synthesis and acetylcholinesterase inhibitory activity of huperzine A-E2020 combined compound.EBI Bioorg Med Chem Lett 9: 3279-84 (2000) Institute of Materia Medica 2D 3D TSV
10612583 27 Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.EBI Bioorg Med Chem Lett 9: 3273-6 (2000) University of New Orleans 2D 3D TSV
10612582 13 Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry.EBI Bioorg Med Chem Lett 9: 3267-72 (2000) University of California 2D 3D TSV
10611640 49 Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.BDB Synapse 35: 144-50 (2000) Albany Medical College 2D 3D TSV
10611634 78 Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.BDB Synapse 35: 79-95 (2000) Institut de Recherches Servier, Centre de Recherches de Croissy 2D 3D TSV
10606521 13 Equilibrium thermodynamics of a physiologically-relevant heme-protein complex.BDB Biochemistry 38: 16876-81 (1999) University of North Carolina at Chapel Hill 2D 3D TSV
10604951 12 Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.BDB J Pharmacol Exp Ther 292: 215-27 (2000) University of Colorado 2D 3D TSV
10602710 51 Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.EBI J Med Chem 42: 5254-65 (2000) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10602709 43 Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.EBI J Med Chem 42: 5241-53 (2000) Bristol-Myers Squibb Pharmaceutical Research Institute 2D 3D TSV
10602705 82 Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.EBI J Med Chem 42: 5197-211 (2000) INSERM 2D 3D TSV
10602703 73 A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.EBI J Med Chem 42: 5181-7 (2000) Warner-Lambert Company 2D 3D TSV
10602702 22 Simple linear QSAR models based on quantum similarity measures.EBI J Med Chem 42: 5169-80 (2000) Czech Academy of Sciences 2D 3D TSV
10602699 15 Binding constants of neuraminidase inhibitors: An investigation of the linear interaction energy method.EBI J Med Chem 42: 5142-52 (2000) University of Southampton 2D 3D TSV
10602697 92 Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.BDB J Med Chem 42: 5120-30 (1999) SUGEN, Inc. 2D 3D TSV
10602693 64 Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.EBI J Med Chem 42: 5077-94 (2000) Wyeth-Ayerst Research 2D 3D TSV
10602690 36 Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).EBI J Med Chem 42: 5061-3 (2000) Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories 2D 3D TSV
10598788 305 Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.BDB Naunyn Schmiedebergs Arch Pharmacol 360: 488-99 (1999) Novartis Pharma AG 2D 3D TSV
10585536 23 Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.BDB Eur J Pharmacol 383: 209-14 (1999) Hungarian Academy of Sciences 2D 3D TSV
10585212 138 Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.EBI J Med Chem 42: 5029-42 (2000) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10585211 62 Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT(3) receptors.EBI J Med Chem 42: 5020-8 (2000) Universidad Complutense 2D 3D TSV
10585210 60 Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.EBI J Med Chem 42: 5010-9 (2000) University of Ferrara 2D 3D TSV
10585208 212 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.EBI J Med Chem 42: 4981-5001 (2000) Merck Sharp & Dohme Research Laboratories 2D 3D TSV
10585206 45 Structure-activity relationship studies of novel heteroretinoids: induction of apoptosis in the HL-60 cell line by a novel isoxazole-containing heteroretinoid.EBI J Med Chem 42: 4961-9 (2000) Università di Ferrara 2D 3D TSV
10585205 10 On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists.EBI J Med Chem 42: 4952-60 (2000) Polish Academy of Sciences 2D 3D TSV
10580501 2 Kainate receptors are involved in synaptic plasticity.BDB Nature 402: 297-301 (1999) University of Bristol 2D 3D TSV
10579852 8 Synthesis and biological evaluation of a potent E-selectin antagonist.EBI J Med Chem 42: 4909-13 (1999) Novartis Pharma AG 2D 3D TSV
10579851 151 New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.EBI J Med Chem 42: 4890-908 (1999) Centre de Recherches 2D 3D TSV
10579850 15 Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa.EBI J Med Chem 42: 4875-89 (1999) Eli Lilly and Company 2D 3D TSV
10579849 27 Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.BDB J Med Chem 42: 4861-74 (1999) Purdue University 2D 3D TSV
10579848 33 Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.EBI J Med Chem 42: 4853-60 (1999) Harvard Medical School 2D 3D TSV
10579847 27 Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.EBI J Med Chem 42: 4844-52 (1999) Abbott Laboratories 2D 3D TSV
10579846 68 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.EBI J Med Chem 42: 4836-43 (1999) School of Chemistry and Biochemistry 2D 3D TSV
10579845 6 Synthesis, acid-base behavior, and binding properties of 6-modified myo-inositol 1,4,5-tris(phosphate)s.EBI J Med Chem 42: 4824-35 (1999) Laboratoire de Pharmacochimie de la Communication Cellulaire UMR 7081 du CNRS 2D 3D TSV
10579843 81 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.EBI J Med Chem 42: 4804-13 (1999) Synaptic Pharmaceutical Corporation 2D 3D TSV
10579842 91 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.EBI J Med Chem 42: 4794-803 (1999) Synaptic Pharmaceutical Corporation 2D 3D TSV
10579841 113 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.EBI J Med Chem 42: 4778-93 (1999) Synaptic Pharmaceutical Corporation 2D 3D TSV
10579840 88 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.EBI J Med Chem 42: 4764-77 (1999) Synaptic Pharmaceutical Corporation 2D 3D TSV
10579836 7 Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors.EBI J Med Chem 42: 4729-32 (1999) Martin-Luther-University Halle-Wittenberg 2D 3D TSV
10579835 6 Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.EBI J Med Chem 42: 4725-8 (1999) Northwestern University 2D 3D TSV
10579830 98 Discovery of novel non-peptide CCR1 receptor antagonists.EBI J Med Chem 42: 4680-94 (1999) Berlex Biosciences 2D 3D TSV
10579829 11 Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.EBI J Med Chem 42: 4669-79 (1999) Westfälische Wilhelms-Universität Münster 2D 3D TSV
10579828 28 5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.EBI J Med Chem 42: 4659-68 (1999) Insituto de Qu�mica M�dica (CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain. 2D 3D TSV
10579825 14 Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth.EBI J Med Chem 42: 4630-9 (1999) University of Nebraska Medical Center 2D 3D TSV
10579824 36 Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.EBI J Med Chem 42: 4621-9 (1999) Research Triangle Institute 2D 3D TSV
10579821 51 Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.EBI J Med Chem 42: 4584-603 (1999) Novartis Horsham Research Centre 2D 3D TSV
10579820 4 Specific nonpeptide photoprobes as tools for the structural study of the angiotensin II AT(1) receptor.EBI J Med Chem 42: 4572-83 (1999) Laboratoires Fournier S.A. 2D 3D TSV
10579818 162 Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.EBI J Med Chem 42: 4547-62 (1999) Procter and Gamble Pharmaceuticals 2D 3D TSV
10579817 10 Molecular modeling studies on G-quadruplex complexes of telomerase inhibitors: structure-activity relationships.EBI J Med Chem 42: 4538-46 (1999) Institute of Cancer Research 2D 3D TSV
10579815 168 Affinity and selectivity of matrix metalloproteinase inhibitors: a chemometrical study from the perspective of ligands and proteins.EBI J Med Chem 42: 4506-23 (1999) Hoechst Marion Roussel 2D 3D TSV
10579811 70 Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.EBI J Med Chem 42: 4473-8 (1999) Università degli Studi di Ferrara 2D 3D TSV
10576696 32 Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.EBI Bioorg Med Chem Lett 9: 3243-8 (1999) Merck 2D 3D TSV
10576693 48 Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.EBI Bioorg Med Chem Lett 9: 3225-30 (1999) Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. 2D 3D TSV
10576692 17 Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).BDB Bioorg Med Chem Lett 9: 3221-4 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10576691 11 Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.EBI Bioorg Med Chem Lett 9: 3217-20 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10576690 13 Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.EBI Bioorg Med Chem Lett 9: 3211-6 (1999) Georgetown University Medical Center 2D 3D TSV
10576685 63 Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.EBI Bioorg Med Chem Lett 9: 3187-92 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10576684 67 A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.EBI Bioorg Med Chem Lett 9: 3181-6 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10571174 25 (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.EBI Bioorg Med Chem Lett 9: 3053-6 (1999) Research Triangle Institute 2D 3D TSV
10571170 27 Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.EBI Bioorg Med Chem Lett 9: 3031-4 (1999) Dipartimento di Scienze Farmaceutiche - Università di Genova 2D 3D TSV
10571165 30 Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.EBI Bioorg Med Chem Lett 9: 3009-14 (1999) ARIAD Pharmaceuticals, Inc. 2D 3D TSV
10571163 14 A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.EBI Bioorg Med Chem Lett 9: 2999-3002 (1999) Institute for Biomedical Research 2D 3D TSV
10571156 1 Synthesis and biological characterization of sqbazide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A2 receptor.EBI Bioorg Med Chem Lett 9: 2963-8 (1999) Ecole Nationale Supérieure de Chimie de Paris 2D 3D TSV
10571154 8 Guanidine-substituted imidazoles as inhibitors of nitric oxide synthase.EBI Bioorg Med Chem Lett 9: 2953-8 (1999) Wake Forest University Winston-Salem 2D 3D TSV
10571147 7 Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids.EBI Bioorg Med Chem Lett 9: 2915-20 (1999) Novartis Pharma Inc. 2D 3D TSV
10571146 19 3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.EBI Bioorg Med Chem Lett 9: 2909-14 (1999) Seoul National University 2D 3D TSV
10570049 4 Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter.EBI Mol Pharmacol 56: 1219-28 (1999) Kagoshima University 2D 3D TSV
10565848 33 Characterization and function of the bovine kidney epithelial angiotensin receptor subtype 4 using angiotensin IV and divalinal angiotensin IV as receptor ligands.BDB J Pharmacol Exp Ther 291: 1242-9 (1999) Washington State University 2D 3D TSV
10565843 8 Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.EBI J Pharmacol Exp Ther 291: 1204-9 (1999) Vanderbilt University School of Medicine 2D 3D TSV
10565829 17 Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.BDB J Pharmacol Exp Ther 291: 1093-9 (1999) Loughborough University 2D 3D TSV
10560746 10 Revised structure of a homonojirimycin isomer from Aglaonema treubii: first example of a naturally occurring alpha-homoallonojirimycin.EBI Bioorg Med Chem Lett 9: 3171-4 (1999) Institut de Chimie Organique et Analytique (I.C.O.A.) 2D 3D TSV
10560745 46 Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.EBI Bioorg Med Chem Lett 9: 3165-70 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10560742 85 3-Amidinophenylalanine-based inhibitors of urokinase.EBI Bioorg Med Chem Lett 9: 3147-52 (1999) Universität Jena 2D 3D TSV
10560741 60 Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.EBI Bioorg Med Chem Lett 9: 3143-6 (1999) Friedrich-Alexander University 2D 3D TSV
10560740 23 The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives.EBI Bioorg Med Chem Lett 9: 3137-42 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10560733 19 4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists.EBI Bioorg Med Chem Lett 9: 3103-8 (1999) The James Black Foundation, London, UK. matthew.tozer@kcl.ac.uk 2D 3D TSV
10560731 2 Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.EBI Bioorg Med Chem Lett 9: 3093-8 (1999) The University of Sydney 2D 3D TSV
10543913 1 Isolation of xestosterol esters of brominated acetylenic fatty acids from the marine sponge xestospongia testudinariaEBI J Nat Prod 62: 1439-42 (1999) Griffith University 2D 3D TSV
10543890 61 Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.EBI J Med Chem 42: 4462-70 (1999) Universita' degli Studi di Salerno 2D 3D TSV
10543889 4 Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.EBI J Med Chem 42: 4456-61 (1999) Abbott Laboratories 2D 3D TSV
10543888 60 Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.EBI J Med Chem 42: 4446-55 (1999) National Institute on Drug Abuse-Intramural Research Program 2D 3D TSV
10543887 12 Heteroarotinoids inhibit head and neck cancer cell lines in vitro and in vivo through both RAR and RXR retinoic acid receptors.EBI J Med Chem 42: 4434-45 (1999) University of Oklahoma Health Sciences Center 2D 3D TSV
10543886 1 Two-stage method for protein-ligand docking.EBI J Med Chem 42: 4422-33 (1999) German National Research Center for Information Technology 2D 3D TSV
10543883 25 Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.EBI J Med Chem 42: 4394-404 (1999) Université Louis Pasteur 2D 3D TSV
10543881 10 Compounds that activate the mouse melanocortin-1 receptor identified by screening a small molecule library based upon the beta-turn.EBI J Med Chem 42: 4380-7 (1999) Oregon Health Sciences University 2D 3D TSV
10543880 63 Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.EBI J Med Chem 42: 4362-79 (1999) Universita' degli Studi di Salerno 2D 3D TSV
10543879 37 Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI J Med Chem 42: 4351-61 (1999) University of Kansas 2D 3D TSV
10543877 25 Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.EBI J Med Chem 42: 4331-42 (1999) Uppsala University 2D 3D TSV
10543874 79 Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.EBI J Med Chem 42: 4300-12 (1999) Cardiff University 2D 3D TSV
10543872 31 Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.EBI J Med Chem 42: 4281-91 (1999) Novo Nordisk A/S 2D 3D TSV
10531324 22 Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor.BDB J Biol Chem 274: 31272-8 (1999) Indian Institute of Science 2D 3D TSV
10530956 45 Structure-activity relationship of HIV-1 protease inhibitors containing alpha-hydroxy-beta-amino acids. Detailed study of P1 site.BDB Bioorg Med Chem 7: 2063-72 (1999) Sankyo Co. Ltd. 2D 3D TSV
10522712 109 The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.EBI Bioorg Med Chem Lett 9: 2887-92 (1999) British Biotech Pharmaceuticals Limited 2D 3D TSV
10522707 16 2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.EBI Bioorg Med Chem Lett 9: 2863-6 (1999) GlaxoWellcome Medicines Research Centre 2D 3D TSV
10522706 8 Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex.EBI Bioorg Med Chem Lett 9: 2859-62 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10522703 103 Design and synthesis of novel dihydropyridine alpha-1a antagonists.EBI Bioorg Med Chem Lett 9: 2843-8 (1999) Synaptic Pharmaceutical Corporation 2D 3D TSV
10522702 52 Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.EBI Bioorg Med Chem Lett 9: 2837-42 (1999) NV Organon 2D 3D TSV
10522701 14 Synthesis and biological evaluation of 1,1-difluoro-2-(tetrahydro-3-furanyl)ethylphosphonic acids possessing a N9-purinylmethyl functional group at the ring. a new class of inhibitors for purine nucleoside phosphorylases.EBI Bioorg Med Chem Lett 9: 2833-6 (1999) Tokyo University of Pharmacy & Life Science 2D 3D TSV
10522699 37 Design, combinatorial chemical synthesis and in vitro characterization of novel urea based gelatinase inhibitors.EBI Bioorg Med Chem Lett 9: 2823-6 (1999) University of Wisconsin-Madison 2D 3D TSV
10522698 17 Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.EBI Bioorg Med Chem Lett 9: 2819-22 (1999) Korea Research Institute of Chemical Technology 2D 3D TSV
10522697 36 Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.EBI Bioorg Med Chem Lett 9: 2815-8 (1999) Warner-Lambert Company 2D 3D TSV
10522696 8 Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.BDB Bioorg Med Chem Lett 9: 1751-6 (1999) Gilead Sciences Inc. 2D 3D TSV
10522695 18 Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.BDB Bioorg Med Chem Lett 9: 2805-10 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10522694 4 The synthesis of a new class of oxytocin antagonists.EBI Bioorg Med Chem Lett 9: 2801-4 (1999) Ferring Research Institute 2D 3D TSV
10522693 14 Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.EBI Bioorg Med Chem Lett 9: 2795-800 (1999) Institute of Science and Technology 2D 3D TSV
10514305 4 Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.EBI J Nat Prod 62: 1241-5 (1999) Peking Union Medical College and Chinese Academy of Medical Sciences 2D 3D TSV
10514298 15 Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.EBI J Med Chem 42: 4269-74 (1999) Freie Universität Berlin 2D 3D TSV
10514296 8 Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.EBI J Med Chem 42: 4257-63 (1999) Purdue University 2D 3D TSV
10514295 7 3-Alkyl-6-chloro-2-pyrones: selective inhibitors of pancreatic cholesterol esterase.EBI J Med Chem 42: 4250-6 (1999) University of New Mexico 2D 3D TSV
10514294 15 Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties.EBI J Med Chem 42: 4239-49 (1999) Warner-Lambert Company 2D 3D TSV
10514293 31 Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.EBI J Med Chem 42: 4232-8 (1999) National Institute of Diabetes 2D 3D TSV
10514292 42 Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.BDB J Med Chem 42: 4225-31 (1999) Hong Kong University of Science and Technology 2D 3D TSV
10514289 18 Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.EBI J Med Chem 42: 4193-201 (1999) Universit£s Montpellier I et II 2D 3D TSV
10514288 12 Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.EBI J Med Chem 42: 4185-92 (1999) Universit£s Montpellier I et II 2D 3D TSV
10514285 66 Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.BDB J Med Chem 42: 4150-60 (1999) Medivir AB 2D 3D TSV
10514284 41 Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.EBI J Med Chem 42: 4140-9 (1999) Pharmacia & Upjohn 2D 3D TSV
10514283 8 Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores.EBI J Med Chem 42: 4129-39 (1999) Seoul National University 2D 3D TSV
10514281 16 Inhibition of neuronal nitric oxide synthase by 4-amino pteridine derivatives: structure-activity relationship of antagonists of (6R)-5,6,7,8-tetrahydrobiopterin cofactor.EBI J Med Chem 42: 4108-21 (1999) Julius-Maximilians University Würzburg 2D 3D TSV
10514279 145 Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70.BDB J Med Chem 42: 4088-98 (1999) ARIAD Pharmaceuticals, Inc. 2D 3D TSV
10514275 7 Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains.EBI J Med Chem 42: 4054-61 (1999) Uppsala University 2D 3D TSV
10514271 1 Diethylcarbamoylating/nitroxylating agents as dual action inhibitors of aldehyde dehydrogenase: a disulfiram-cyanamide merger.EBI J Med Chem 42: 4016-20 (1999) VA Medical Center 2D 3D TSV
10509933 4 Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.EBI Bioorg Med Chem Lett 9: 2773-8 (1999) Pfizer Inc. 2D 3D TSV
10509931 18 Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.EBI Bioorg Med Chem Lett 9: 2763-6 (1999) University of Arizona 2D 3D TSV
10509929 116 Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI Bioorg Med Chem Lett 9: 2753-8 (1999) Rhône-Poulenc Rorer 2D 3D TSV
10509928 31 Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.EBI Bioorg Med Chem Lett 9: 2747-52 (1999) Abbott Laboratories 2D 3D TSV
10509927 71 Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.EBI Bioorg Med Chem Lett 9: 2741-6 (1999) Merck Research Laboratories 2D 3D TSV
10509926 1 9-[(2'S,3'S)-3'-formyl-2',3'-dihydroxypropyl]adenine: a facile affinity-labeling probe of human S-adenosyl-L-homocysteine hydrolase.EBI Bioorg Med Chem Lett 9: 2737-40 (1999) Gifu University 2D 3D TSV
10509923 9 N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.EBI Bioorg Med Chem Lett 9: 2721-6 (1999) Institute 2D 3D TSV
10509922 27 Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.EBI Bioorg Med Chem Lett 9: 2715-20 (1999) SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. 2D 3D TSV
10509919 103 New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.EBI Bioorg Med Chem Lett 9: 2699-704 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10509910 10 Syntheses of novel antitumor dihydroxanthone derivatives with inhibitory activity against DNA topoisomerase II.EBI Bioorg Med Chem Lett 9: 2653-6 (1999) Ajinomoto Co., Inc. 2D 3D TSV
10508448 11 Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI J Med Chem 42: 4001-9 (1999) Brown University 2D 3D TSV
10508446 12 Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.EBI J Med Chem 42: 3982-93 (1999) Takeda Chemical Industries, Ltd. 2D 3D TSV
10508445 10 Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.EBI J Med Chem 42: 3971-81 (1999) AnorMED Inc. 2D 3D TSV
10508444 58 Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.EBI J Med Chem 42: 3965-70 (1999) Taisho Pharmaceutical Company Ltd. 2D 3D TSV
10508441 64 Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.EBI J Med Chem 42: 3934-41 (1999) Universit£ degli Studi di Bari 2D 3D TSV
10508439 4 Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI J Med Chem 42: 3910-8 (1999) Washington University 2D 3D TSV
10508435 61 Substituted isoquinolines and quinazolines as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha.EBI J Med Chem 42: 3860-73 (1999) University of California 2D 3D TSV
10508434 47 Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.EBI J Med Chem 42: 3852-9 (1999) Abbott Laboratories 2D 3D TSV
10508432 12 Design and fast synthesis of C-terminal duplicated potent C(2)-symmetric P1/P1'-modified HIV-1 protease inhibitors.BDB J Med Chem 42: 3835-44 (1999) Uppsala University 2D 3D TSV
10508430 38 Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.EBI J Med Chem 42: 3809-20 (1999) AstraZeneca 2D 3D TSV
10508429 14 Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation.EBI J Med Chem 42: 3800-8 (1999) Parke-Davis Pharmaceutical Research 2D 3D TSV
10508427 42 A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.EBI J Med Chem 42: 3785-8 (1999) Glaxo Wellcome Research & Development 2D 3D TSV
10508426 13 N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.EBI J Med Chem 42: 3779-84 (1999) Merck Research Laboratories 2D 3D TSV
10508425 68 Mixture-based synthetic combinatorial libraries.EBI J Med Chem 42: 3743-78 (1999) Torrey Pines Institute for Molecular Studies 2D 3D TSV
10499421 27 The cloned guinea pig neuropeptide Y receptor Y1 conforms to other mammalian Y1 receptors.BDB Peptides 20: 1043-53 (1999) Uppsala University 2D 3D TSV
10498829 62 Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.BDB Br J Pharmacol 128: 13-20 (1999) Cerebrus Ltd 2D 3D TSV
10498222 3 Asymmetric synthesis of novel quaternary alpha-hydroxy-delta-lactam dipeptide surrogates.EBI Bioorg Med Chem Lett 9: 2625-8 (1999) Corvas International, Inc. 2D 3D TSV
10498221 11 Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.EBI Bioorg Med Chem Lett 9: 2621-4 (1999) Merck Research Laboratories 2D 3D TSV
10498220 22 Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.EBI Bioorg Med Chem Lett 9: 2615-20 (1999) Merck Research Laboratories 2D 3D TSV
10498218 1 Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system.EBI Bioorg Med Chem Lett 9: 2607-12 (1999) The University of Montana 2D 3D TSV
10498215 60 New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.EBI Bioorg Med Chem Lett 9: 2593-8 (1999) Wyeth-Ayerst Research Laboratories 2D 3D TSV
10498212 3 Preparation and receptor binding affinities of cyclic C-terminal neurotensin (8-13) and (9-13) analogues.EBI Bioorg Med Chem Lett 9: 2579-82 (1999) Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston 29425, USA. 2D 3D TSV
10498211 42 Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI Bioorg Med Chem Lett 9: 2573-8 (1999) Corvas International, Inc. 2D 3D TSV
10498210 27 A new class of selective and potent inhibitors of neuronal nitric oxide synthase.EBI Bioorg Med Chem Lett 9: 2569-72 (1999) Pfizer Inc. Groton 2D 3D TSV
10498208 4 Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.EBI Bioorg Med Chem Lett 9: 2561-4 (1999) University of Tokyo 2D 3D TSV
10498206 25 Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.EBI Bioorg Med Chem Lett 9: 2549-54 (1999) Merck Research Laboratorie 2D 3D TSV
10498204 25 Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.EBI Bioorg Med Chem Lett 9: 2539-44 (1999) Rh£ne-Poulenc Rorer 2D 3D TSV
10498203 13 Dysidiolide and related gamma-hydroxy butenolide compounds as inhibitors of the protein tyrosine phosphatase, CDC25.EBI Bioorg Med Chem Lett 9: 2537-8 (1999) Mitotix, Inc. 2D 3D TSV
10498202 43 Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.EBI Bioorg Med Chem Lett 9: 2531-6 (1999) Bayer Corporation 2D 3D TSV
10498200 40 Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.EBI Bioorg Med Chem Lett 9: 2521-4 (1999) Pharmacia& Upjohn 2D 3D TSV
10498198 6 A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry.EBI Bioorg Med Chem Lett 9: 2509-14 (1999) Stine Haskell Research Center 2D 3D TSV
10498197 58 The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.EBI Bioorg Med Chem Lett 9: 2503-8 (1999) Warner-Lambert Company 2D 3D TSV
10498196 42 The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.EBI Bioorg Med Chem Lett 9: 2497-502 (1999) Warner-Lambert Company 2D 3D TSV
10498195 12 2,7-diazabicyclo[3.3.0]octanes as novel h5-HT receptor agonists.EBI Bioorg Med Chem Lett 9: 2491-6 (1999) Merck Sharp & Dohme Research Laboratories 2D 3D TSV
10498193 22 Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.EBI Bioorg Med Chem Lett 9: 2483-6 (1999) Biotech Research Institute 2D 3D TSV
10498189 16 Human telomerase inhibition by substituted acridine derivatives.EBI Bioorg Med Chem Lett 9: 2463-8 (1999) Institute of Cancer Research 2D 3D TSV
10496952 37 Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.BDB Mol Pharmacol 56: 705-13 (1999) University of Virginia 2D 3D TSV
10494877 50 2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.BDB Naunyn Schmiedebergs Arch Pharmacol 360: 103-8 (1999) Universität Wrzburg 2D 3D TSV
10484490 6 Cloning of mouse prostaglandin transporter PGT cDNA: species-specific substrate affinities.EBI Am J Physiol 277: 734-41 (1999) Albert Einstein College of Medicine 2D 3D TSV
10482466 32 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.BDB Bioorg Med Chem 7: 1743-54 Otsuka Pharmaceutical Co., Ltd 2D 3D TSV
10480891 6 Salt links dominate affinity of antibody HyHEL-5 for lysozyme through enthalpic contributions.BDB J Biol Chem 274: 26838-42 (1999) University of Houston 2D 3D TSV
10479314 6 DNA polymerase beta inhibitors from Sandoricum koetjape.EBI J Nat Prod 62: 1110-3 (1999) University of Virginia Charlottesville 2D 3D TSV
10479306 14 Small peptides containing phosphotyrosine and adjacent alphaMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain.EBI J Med Chem 42: 3737-41 (1999) INSERM 2D 3D TSV
10479303 36 Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.EBI J Med Chem 42: 3718-25 (1999) Warner-Lambert Company 2D 3D TSV
10479301 27 Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.EBI J Med Chem 42: 3701-10 (1999) Abbott Laboratories 2D 3D TSV
10479300 383 Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route.EBI J Med Chem 42: 3690-700 (1999) Universit£ degli Studi 2D 3D TSV
10479299 55 Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.EBI J Med Chem 42: 3679-89 (1999) Abbott Laboratories 2D 3D TSV
10479298 60 Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.EBI J Med Chem 42: 3668-78 (1999) Abbott Laboratories 2D 3D TSV
10479296 66 Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors.EBI J Med Chem 42: 3647-56 (1999) Massachusetts General Hospital 2D 3D TSV
10479295 12 2-thioether 5'-O-(1-thiotriphosphate)adenosine derivatives as new insulin secretagogues acting through P2Y-Receptors.EBI J Med Chem 42: 3636-46 (1999) Bar-Ilan University 2D 3D TSV
10479294 13 Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.EBI J Med Chem 42: 3629-35 (1999) Leiden/Amsterdam Center for Drug Research 2D 3D TSV
10479292 16 Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.EBI J Med Chem 42: 3615-22 (1999) Max-Planck Research Unit 2D 3D TSV
10479291 12 Synthesis, structure-activity relationships, and RARgamma-ligand interactions of nitrogen heteroarotinoids.EBI J Med Chem 42: 3602-14 (1999) University of Oklahoma Health Sciences Center 2D 3D TSV
10479290 25 Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI J Med Chem 42: 3588-601 (1999) University of Kansas 2D 3D TSV
10479289 55 Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.BDB J Med Chem 42: 3572-87 (1999) Rhone-Poulenc Rorer 2D 3D TSV
10479288 141 Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI J Med Chem 42: 3557-71 (1999) Rh£ne-Poulenc Rorer 2D 3D TSV
10479286 53 Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.EBI J Med Chem 42: 3527-38 (1999) Southern Research Institute 2D 3D TSV
10479285 17 The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.EBI J Med Chem 42: 3520-6 (1999) Clinical Research Institute of Montreal 2D 3D TSV
10479284 2 5-deazafolate analogues with a rotationally restricted glutamate or ornithine side chain: synthesis and binding interaction with folylpolyglutamate synthetase.EBI J Med Chem 42: 3510-9 (1999) Harvard Medical School 2D 3D TSV
10479283 74 CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.EBI J Med Chem 42: 3502-9 (1999) National Institute on Drug Abuse - Intramural Research Program 2D 3D TSV
10479279 20 N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.EBI J Med Chem 42: 3463-77 (1999) Novo Nordisk A/S 2D 3D TSV
10479278 70 Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.EBI J Med Chem 42: 3447-62 (1999) Novo Nordisk A/S 2D 3D TSV
10479277 15 Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.EBI J Med Chem 42: 3436-46 (1999) Georgetown University Medical Center 2D 3D TSV
10479275 5 A multisubstrate adduct inhibitor of AICAR transformylase.EBI J Med Chem 42: 3421-4 (1999) The Pennsylvania State University 2D 3D TSV
10476886 14 Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists.EBI Bioorg Med Chem Lett 9: 2453-8 (1999) Parke-Davis Pharmaceutical Research 2D 3D TSV
10476885 14 Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.EBI Bioorg Med Chem Lett 9: 2447-52 (1999) Warner-Lambert Company 2D 3D TSV
10476884 1 Synthesis of a phostone glycomimetic of the endothelin converting enzyme inhibitor phosphoramidon.EBI Bioorg Med Chem Lett 9: 2441-6 (1999) Université de Montréal 2D 3D TSV
10476879 52 Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.EBI Bioorg Med Chem Lett 9: 2413-8 (1999) Cadus Pharmaceutical Corporation 2D 3D TSV
10476878 8 Naphthazarin derivatives (II): formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity.EBI Bioorg Med Chem Lett 9: 2407-12 (1999) Chungnam National University 2D 3D TSV
10476877 15 NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.EBI Bioorg Med Chem Lett 9: 2403-6 (1999) Abbott Laboratories 2D 3D TSV
10476876 1 Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.EBI Bioorg Med Chem Lett 9: 2397-402 (1999) Fujisawa Pharmaceutical Co., Ltd. 2D 3D TSV
10476875 36 Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.EBI Bioorg Med Chem Lett 9: 2391-6 (1999) Merck Frosst Center for Therapeutic Research 2D 3D TSV
10476873 2 Synthesis and estrogen receptor binding affinity of a porphyrin-estradiol conjugate for targeted photodynamic therapy of cancer.EBI Bioorg Med Chem Lett 9: 2379-84 (1999) Department of Medicine, Boston University School of Medicine, MA 02118, USA. 2D 3D TSV
10476871 22 P2-achiral, P'-extended alpha-ketoamide inhibitors of calpain I.EBI Bioorg Med Chem Lett 9: 2371-4 (1999) Cephalon Inc. 2D 3D TSV
10476870 9 Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.EBI Bioorg Med Chem Lett 9: 2365-70 (1999) Hoechst Marion Roussel, Inc. 2D 3D TSV
10476869 35 Structure-activity relationships of a novel class of Src SH2 inhibitors.EBI Bioorg Med Chem Lett 9: 2359-64 (1999) ARIAD Pharmaceuticals, Inc. 2D 3D TSV
10476868 6 Structure-based design and synthesis of a novel class of Src SH2 inhibitors.EBI Bioorg Med Chem Lett 9: 2353-8 (1999) ARIAD Pharmaceuticals, Inc. 2D 3D TSV
10476866 3 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.EBI Bioorg Med Chem Lett 9: 2343-8 (1999) Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd, Basel. juergen.wichmann@roche.com 2D 3D TSV
10476865 2 Synthesis of new (benzimidazolyl)piperazines with affinity for the 5-HT1A receptor via Pd(0) amination of bromobenzimidazoles.EBI Bioorg Med Chem Lett 9: 2339-42 (1999) Universidad Complutense 2D 3D TSV
10476864 22 Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.EBI Bioorg Med Chem Lett 9: 2335-8 (1999) Hong Kong University of Science and Technology 2D 3D TSV
10476856 4 A rapid method to identify exo-protease inhibitors.EBI Bioorg Med Chem Lett 9: 2291-6 (1999) The Scripps Research Institute 2D 3D TSV
10471378 4 6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.BDB Biochem Biophys Res Commun 262: 643-6 (1999) Instituto de Biología Celular 2D 3D TSV
10467133 4 Structural basis for selective inhibition of Src family kinases by PP1.BDB Chem Biol 6: 671-8 (1999) Princeton University 2D 3D TSV
10465561 14 Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.EBI Bioorg Med Chem Lett 9: 2279-82 (1999) Department of Medicinal Chemistry, School of Pharmacy, Purdue University, West Lafayette, IN 47907-1333, USA. 2D 3D TSV
10465559 8 Significant compensatory role of position Y-2 conferring high affinity to non-phosphorylated inhibitors of Grb2-SH2 domain.EBI Bioorg Med Chem Lett 9: 2267-72 (1999) National Cancer Institute 2D 3D TSV
10465557 11 Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.EBI Bioorg Med Chem Lett 9: 2259-62 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10465552 10 3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.EBI Bioorg Med Chem Lett 9: 2233-6 (1999) Universit£ Catholiqu£ de Louvain 2D 3D TSV
10465550 11 Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).EBI Bioorg Med Chem Lett 9: 2223-8 (1999) Metabolic& Cardiovascular Diesases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA. 2D 3D TSV
10465549 21 Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.BDB Bioorg Med Chem Lett 9: 2217-22 (1999) Parke-Davis Pharmaceutical Research 2D 3D TSV
10465547 24 SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.EBI Bioorg Med Chem Lett 9: 2207-12 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10465539 14 Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.EBI Bioorg Med Chem Lett 9: 2173-6 (1999) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10465538 28 Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.EBI Bioorg Med Chem Lett 9: 2167-72 (1999) Uppsala University 2D 3D TSV
10465535 14 Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.EBI Bioorg Med Chem Lett 9: 2151-6 (1999) Warner-Lambert Company 2D 3D TSV
10465529 9 Novel conformationally restricted tetracyclic analogs of delta8-tetrahydrocannabinol.EBI Bioorg Med Chem Lett 9: 2119-24 (1999) University of Connecticut 2D 3D TSV
10465404 61 Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.BDB Bioorg Med Chem 7: 1281-93 (1999) Institut Curie 2D 3D TSV
10464027 118 Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.EBI J Med Chem 42: 3412-20 (1999) University of Oregon 2D 3D TSV
10464022 25 Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.EBI J Med Chem 42: 3356-68 (1999) Merck Research Laboratories 2D 3D TSV
10464021 59 N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.EBI J Med Chem 42: 3342-55 (1999) Knoll Pharmaceuticals 2D 3D TSV
10464020 62 Thiazolothiazepine inhibitors of HIV-1 integrase.EBI J Med Chem 42: 3334-41 (1999) National Cancer Institute 2D 3D TSV
10464018 16 Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI J Med Chem 42: 3315-23 (1999) University of Kansas 2D 3D TSV
10464016 1 Synthesis and properties of 3-(2-hydroxyethyl)-3-n-pentyldiazirine, a photoactivable general anesthetic.EBI J Med Chem 42: 3300-7 (1999) Massachusetts General Hospital 2D 3D TSV
10464012 5 New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.EBI J Med Chem 42: 3251-64 (1999) Rh£ne-Poulenc Rorer 2D 3D TSV
10464010 40 Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.EBI J Med Chem 42: 3227-42 (1999) Universitat de Barcelona 2D 3D TSV
10464008 3 Lead generation using pharmacophore mapping and three-dimensional database searching: application to muscarinic M(3) receptor antagonists.EBI J Med Chem 42: 3210-6 (1999) Astra Charnwood 2D 3D TSV
10464006 22 PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes.EBI J Med Chem 42: 3199-202 (1999) Wyeth-Ayerst Research 2D 3D TSV
10455277 9 Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists.BDB Br J Pharmacol 127: 1288-94 (1999) Universit&agrove; degli Studi di Milano 2D 3D TSV
10455251 10 RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.BDB Br J Pharmacol 127: 1075-82 (1999) Roche Bioscience 2D 3D TSV
10454469 6 Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties.BDB J Pharmacol Exp Ther 290: 989-97 (1999) Universidad de Sevilla, 2D 3D TSV
10450992 16 Tetrapeptide derived inhibitors of complexation of a class II MHC: fully unnatural ligands.EBI Bioorg Med Chem Lett 9: 2115-8 (1999) Merck Research Laboratories 2D 3D TSV
10450991 20 Tetrapeptide derived inhibitors of complexation of a class II MHC: the peptide backbone is not inviolate.EBI Bioorg Med Chem Lett 9: 2109-14 (1999) Merck Research Laboratories 2D 3D TSV
10450990 8 1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.EBI Bioorg Med Chem Lett 9: 2105-8 (1999) Cardiff University 2D 3D TSV
10450988 51 Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.EBI Bioorg Med Chem Lett 9: 2095-100 (1999) Eisai Research Institute 2D 3D TSV
10450987 22 Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.EBI Bioorg Med Chem Lett 9: 2089-94 (1999) Merck Research Laboratories 2D 3D TSV
10450986 7 C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.EBI Bioorg Med Chem Lett 9: 2085-8 (1999) Merck Research Laboratories 2D 3D TSV
10450984 16 Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.EBI Bioorg Med Chem Lett 9: 2073-8 (1999) Schering-Plough Research Institute 2D 3D TSV
10450981 58 Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.EBI Bioorg Med Chem Lett 9: 2059-64 (1999) Institut de Recherches Servier, Centre de Recherches de Croissy, Croissy sur Seine, France. 2D 3D TSV
10450980 55 Design and synthesis of beta-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase.EBI Bioorg Med Chem Lett 9: 2053-8 (1999) Monsanto Company 2D 3D TSV
10450979 4 Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.EBI Bioorg Med Chem Lett 9: 2049-52 (1999) University of Cambridge 2D 3D TSV
10450977 27 Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT).EBI Bioorg Med Chem Lett 9: 2039-42 (1999) Azwell Inc. 2D 3D TSV
10450976 1 Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.EBI Bioorg Med Chem Lett 9: 2037-8 (1999) Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories 2D 3D TSV
10450973 21 4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.EBI Bioorg Med Chem Lett 9: 2019-24 (1999) Warner-Lambert Company 2D 3D TSV
10450972 3 Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.EBI Bioorg Med Chem Lett 9: 2013-8 (1999) Institute of Chemistry 2D 3D TSV
10450969 48 The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.EBI Bioorg Med Chem Lett 9: 1997-2002 (1999) Southern Methodist University 2D 3D TSV
10450968 22 Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.EBI Bioorg Med Chem Lett 9: 1991-6 (1999) Merck Research Laboratories 2D 3D TSV
10450967 4 The design and synthesis of inhibitors of adenosine 5'-monophosphate deaminase.EBI Bioorg Med Chem Lett 9: 1985-90 (1999) AgrEvo UK Limited 2D 3D TSV
10450966 16 Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.EBI Bioorg Med Chem Lett 9: 1979-84 (1999) Fujisawa Pharmaceutical Co., Ltd. 2D 3D TSV
10450965 4 Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.EBI Bioorg Med Chem Lett 9: 1973-8 (1999) Novartis Pharmaceuticals 2D 3D TSV
10450964 35 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.EBI Bioorg Med Chem Lett 9: 1969-72 (1999) Universität Erlangen - Nürnberg 2D 3D TSV
10450962 4 Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.EBI Bioorg Med Chem Lett 9: 1957-62 (1999) University of Illinois at Chicago 2D 3D TSV
10450960 3 Isolation and structure of SCH 351633: a novel hepatitis C virus (HCV) NS3 protease inhibitor from the fungus Penicillium griseofulvum.EBI Bioorg Med Chem Lett 9: 1949-52 (1999) Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. 2D 3D TSV
10450955 19 The design and synthesis of ALS inhibitors from pharmacophore models.EBI Bioorg Med Chem Lett 9: 1927-32 (1999) Nankai University 2D 3D TSV
10450951 3 Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.EBI Bioorg Med Chem Lett 9: 1907-10 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10450950 16 Design of benzoic acid inhibitors of influenza neuraminidase containing a cyclic substitution for the N-acetyl grouping.BDB Bioorg Med Chem Lett 9: 1901-6 (1999) University of Alabama at Birmingham 2D 3D TSV
10450949 24 Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.EBI Bioorg Med Chem Lett 9: 1895-900 (1999) Wyeth-Ayerst Research 2D 3D TSV
10447965 2 Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene.EBI J Med Chem 42: 3188-92 (1999) University of Bath 2D 3D TSV
10447960 20 Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.EBI J Med Chem 42: 3154-62 (1999) Universidad de Valencia 2D 3D TSV
10447959 30 N(omega)-Nitroarginine-containing dipeptide amides. Potent and highly selective inhibitors of neuronal nitric oxide synthase.EBI J Med Chem 42: 3147-53 (1999) Northwestern University 2D 3D TSV
10447957 5 Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.EBI J Med Chem 42: 3126-33 (1999) University of Georgia 2D 3D TSV
10447955 16 Potent bivalent thrombin inhibitors: replacement of the scissile peptide bond at P(1)-P(1)' with arginyl ketomethylene isosteres.EBI J Med Chem 42: 3109-15 (1999) National Research Council Canada 2D 3D TSV
10447952 16 Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.EBI J Med Chem 42: 3087-93 (1999) State University of New York 2D 3D TSV
10447950 15 Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.EBI J Med Chem 42: 3066-74 (1999) Targacept Inc. 2D 3D TSV
10447949 27 Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.EBI J Med Chem 42: 3055-65 (1999) National Institute of Diabetes 2D 3D TSV
10447947 14 N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.EBI J Med Chem 42: 3033-40 (1999) Technische Universität München 2D 3D TSV
10447946 48 Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.EBI J Med Chem 42: 3026-32 (1999) BASF AG 2D 3D TSV
10447942 9 A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.EBI J Med Chem 42: 3011-3 (1999) TBA 2D 3D TSV
10445051 7 Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.BDB J Enzym Inhib 14: 307-21 (1999) University of Catania 2D 3D TSV
10433861 79 Somatostatin and its receptor family.BDB Front Neuroendocrinol 20: 157-98 (1999) Royal Victoria Hospital 2D 3D TSV
10425145 7 Activity-guided isolation of triterpenoid acyl CoA cholesteryl acyl transferase (ACAT) inhibitors from Ilex kudincha.EBI J Nat Prod 62: 1061-4 (1999) Kayaku Co. Ltd. 2D 3D TSV
10425142 3 New guaianolides and xanthine oxidase inhibitory flavonols from ajania fruticulosaEBI J Nat Prod 62: 1053-5 (1999) Nanjing University 2D 3D TSV
10425125 2 Harbinatic acid, a novel and potent DNA polymerase beta inhibitor from Hardwickia binata.EBI J Nat Prod 62: 1000-2 (1999) University of Virginia 2D 3D TSV
10425111 17 Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.EBI J Med Chem 42: 3004-7 (1999) Creighton University School of Medicine 2D 3D TSV
10425109 24 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.EBI J Med Chem 42: 2993-3000 (1999) CoCensys, Inc. 2D 3D TSV
10425106 12 4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.EBI J Med Chem 42: 2969-76 (1999) Brown University 2D 3D TSV
10425100 43 Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.EBI J Med Chem 42: 2909-19 (1999) Universität Hamburg 2D 3D TSV
10425096 80 2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.EBI J Med Chem 42: 2870-80 (1999) FAES, S.A. 2D 3D TSV
10425095 26 Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.EBI J Med Chem 42: 2862-9 (1999) University of Minnesota 2D 3D TSV
10425087 110 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.EBI J Med Chem 42: 2760-73 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10425086 83 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.EBI J Med Chem 42: 2752-9 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10425082 1 Pharmacotherapies for treatment of cocaine abuse: preclinical aspects.EBI J Med Chem 42: 2721-36 (1999) Research Triangle Institute 2D 3D TSV
10421757 5 Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.BDB Chem Biol 6: 519-29 (1999) Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC) 2D 3D TSV
10417407 14 Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.BDB Acta Crystallogr D Biol Crystallogr 55: 1395-404 (1999) Berlex 2D 3D TSV
10417314 13 Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes.EBI Biochem J 341: 529-35 (1999) Physiologisch-chemisches Institut der Eberhard-Karls-Universit£t T£bingen 2D 3D TSV
10411602 2 Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.EBI J Pharmacol Exp Ther 290: 854-62 (1999) Lilly Research Laboratories 2D 3D TSV
10411589 20 Comparison of the pharmacological properties of cloned rat, human, and bovine norepinephrine transporters.BDB J Pharmacol Exp Ther 290: 761-7 (1999) The University of Queensland 2D 3D TSV
10411588 4 Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.BDB J Pharmacol Exp Ther 290: 753-60 (1999) The University of Calgary 2D 3D TSV
10411577 6 The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.EBI J Pharmacol Exp Ther 290: 672-7 (1999) Kyorin University School of Medicine 2D 3D TSV
10411562 36 Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.BDB J Pharmacol Exp Ther 290: 551-60 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10411492 4 (2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.EBI J Med Chem 42: 2716-20 (1999) Università di Perugia 2D 3D TSV
10411491 96 1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.EBI J Med Chem 42: 2706-15 (1999) Merck Sharp and Dohme Research Laboratories 2D 3D TSV
10411488 34 2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase.EBI J Med Chem 42: 2679-84 (1999) Institute of Cancer Research 2D 3D TSV
10411485 46 Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.EBI J Med Chem 42: 2651-61 (1999) Schering-Plough Research Institute 2D 3D TSV
10411484 176 Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring?EBI J Med Chem 42: 2641-50 (1999) Universit£ degli Studi 2D 3D TSV
10411483 24 alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.EBI J Med Chem 42: 2633-40 (1999) Universit£tstrasse 16 2D 3D TSV
10411482 63 1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists.EBI J Med Chem 42: 2621-32 (1999) Shionogi & Company, Ltd. 2D 3D TSV
10411481 144 Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.EBI J Med Chem 42: 2610-20 (1999) CEA 2D 3D TSV
10411471 19 Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.EBI J Med Chem 42: 2498-503 (1999) Abbott Laboratories 2D 3D TSV
10406658 7 Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.EBI Bioorg Med Chem Lett 9: 1875-80 (1999) Schering-Plough Research Institute 2D 3D TSV
10406657 91 Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.EBI Bioorg Med Chem Lett 9: 1869-74 (1999) Merck Research Laboratories 2D 3D TSV
10406650 18 Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.EBI Bioorg Med Chem Lett 9: 1831-6 (1999) Georgetown University Medical Center 2D 3D TSV
10406649 31 From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.EBI Bioorg Med Chem Lett 9: 1825-30 (1999) The James Black Foundation, London, UK. matthew.tozer@kcl.ac.uk 2D 3D TSV
10406647 30 Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.EBI Bioorg Med Chem Lett 9: 1813-8 (1999) Warner-Lambert Company 2D 3D TSV
10406646 15 Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.EBI Bioorg Med Chem Lett 9: 1807-12 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10406645 36 Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.EBI Bioorg Med Chem Lett 9: 1801-6 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10406642 8 Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.EBI Bioorg Med Chem Lett 9: 1783-8 (1999) Pharmacia& Upjohn, Chem. Dept., Nerviano, Milan, Italy. paolo.pevarello@eu.pnu.com 2D 3D TSV
10406640 31 The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.EBI Bioorg Med Chem Lett 9: 1773-8 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10406637 20 Synthesis and identification of conformationally constrained selective MMP inhibitors.EBI Bioorg Med Chem Lett 9: 1757-60 (1999) Searle Discovery Research 2D 3D TSV
10406636 6 Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.BDB Bioorg Med Chem Lett 9: 1751-6 (1999) Gilead Sciences Inc. 2D 3D TSV
10406633 32 5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.EBI Bioorg Med Chem Lett 9: 1737-40 (1999) Wyeth-Ayerst Research 2D 3D TSV
10406632 11 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.EBI Bioorg Med Chem Lett 9: 1733-6 (1999) Wyeth-Ayerst Research 2D 3D TSV
10397508 8 1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.EBI Bioorg Med Chem Lett 9: 1721-6 (1999) Georgetown University Medical Center 2D 3D TSV
10397507 42 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.EBI Bioorg Med Chem Lett 9: 1715-20 (1999) Merck Frosst Centre For Therapeutic Research 2D 3D TSV
10397504 4 Synthesis and evaluation of 1-position-modified inositol 1,4,5-trisphosphate analogs.EBI Bioorg Med Chem Lett 9: 1697-702 (1999) The University of Tokyo 2D 3D TSV
10397503 40 Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.EBI Bioorg Med Chem Lett 9: 1691-6 (1999) Universit£ de Montr£al 2D 3D TSV
10397502 36 Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.EBI Bioorg Med Chem Lett 9: 1687-90 (1999) Stanford University 2D 3D TSV
10397500 3 Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties.EBI Bioorg Med Chem Lett 9: 1679-82 (1999) Universidad Complutense 2D 3D TSV
10397495 49 Thrombin inhibitors based on [5,5] trans-fused indane lactams.EBI Bioorg Med Chem Lett 9: 1657-62 (1999) Glaxo Wellcome Research and Development 2D 3D TSV
10397493 4 Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES).EBI Bioorg Med Chem Lett 9: 1645-50 (1999) Kingston University 2D 3D TSV
10395519 1 Interference of linoleic acid fraction in some receptor binding assays.EBI J Nat Prod 62: 912-4 (1999) Leiden University 2D 3D TSV
10395489 47 4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.EBI J Med Chem 42: 2478-84 (1999) Universita' di Firenze 2D 3D TSV
10395488 114 Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.EBI J Med Chem 42: 2469-77 (1999) CoCensys, Inc. 2D 3D TSV
10395486 75 Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.EBI J Med Chem 42: 2447-55 (1999) Duquesne University 2D 3D TSV
10395483 91 Structure-activity relationships for a class of inhibitors of purine nucleoside phosphorylase.EBI J Med Chem 42: 2422-31 (1999) University of Michigan 2D 3D TSV
10395482 40 Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.EBI J Med Chem 42: 2409-21 (1999) Merck Research Laboratories 2D 3D TSV
10395480 103 Apstatin analogue inhibitors of aminopeptidase P, a bradykinin-degrading enzyme.EBI J Med Chem 42: 2394-402 (1999) Pharmacia and Upjohn 2D 3D TSV
10395478 126 Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.BDB J Med Chem 42: 2373-82 (1999) University of Auckland 2D 3D TSV
10395476 3 Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.EBI J Med Chem 42: 2358-63 (1999) Novartis Pharma Inc. 2D 3D TSV
10395475 20 Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.EBI J Med Chem 42: 2351-7 (1999) The University of Wollongong 2D 3D TSV
10395474 14 Molecular modeling and synthesis of inhibitors of herpes simplex virus type 1 uracil-DNA glycosylase.EBI J Med Chem 42: 2344-50 (1999) University of Massachusetts Medical Center 2D 3D TSV
10395473 19 Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent.EBI J Med Chem 42: 2332-43 (1999) University of Alabama at Birmingham 2D 3D TSV
10387041 7 Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease.BDB Biochemistry 38: 7978-88 (1999) University of Queensland 2D 3D TSV
10386947 9 Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.EBI Bioorg Med Chem Lett 9: 1619-24 (1999) University of Oregon 2D 3D TSV
10386946 19 Design of scytalone dehydratase inhibitors as rice blast fungicides: derivatives of norephedrine.EBI Bioorg Med Chem Lett 9: 1613-8 (1999) Stine-Haskell Research Center 2D 3D TSV
10386945 30 Design of scytalone dehydratase inhibitors as rice blast fungicides: (N-phenoxypropyl)-carboxamides.EBI Bioorg Med Chem Lett 9: 1607-12 (1999) Stine-Haskell Research Center 2D 3D TSV
10386944 7 N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.EBI Bioorg Med Chem Lett 9: 1601-6 (1999) Universität des Saarlandes 2D 3D TSV
10386942 14 Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.EBI Bioorg Med Chem Lett 9: 1593-8 (1999) Institute 2D 3D TSV
10386940 31 Novel derivatives of 3-(dipropylamino)chroman. Interactions with 5-HT1A and D2A receptors.EBI Bioorg Med Chem Lett 9: 1583-6 (1999) Uppsala University 2D 3D TSV
10386938 16 Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.EBI Bioorg Med Chem Lett 9: 1573-6 (1999) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10386934 15 Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.EBI Bioorg Med Chem Lett 9: 1553-8 (1999) Central Research Laboratories, Zeria Pharmaceutical Co., Ltd., Saitama, Japan. 2D 3D TSV
10386932 56 Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.EBI Bioorg Med Chem Lett 9: 1541-6 (1999) Eisai Research Institute 2D 3D TSV
10386929 10 The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases.EBI Bioorg Med Chem Lett 9: 1527-32 (1999) The University of Kansas 2D 3D TSV
10386926 32 Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor.EBI Bioorg Med Chem Lett 9: 1511-6 (1999) INSERM 2D 3D TSV
10386923 3 Synthesis and evaluation of glucocerebrosidase inhibitory activity of anhydro deoxyinositols from (+)-epi- and (-)-vibo-quercitols.EBI Bioorg Med Chem Lett 9: 1493-8 (1999) Keio University 2D 3D TSV
10386921 33 Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.EBI Bioorg Med Chem Lett 9: 1481-6 (1999) Warner-Lambert Company 2D 3D TSV
10385678 4 Selective substrates for non-neuronal monoamine transporters.EBI Mol Pharmacol 56: 1-10 (1999) University of Heidelberg 2D 3D TSV
10379421 134 Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.BDB Cell Mol Neurobiol 19: 467-89 (1999) TBA 2D 3D TSV
10377455 121 Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.BDB Proc Natl Acad Sci U S A 96: 7563-8 (1999) St. Bartholomew's and the Royal London School of Medicine and Dentistry 2D 3D TSV
10377235 10 Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol.EBI J Med Chem 42: 2280-6 (1999) Laval University Medical Research Center 2D 3D TSV
10377234 12 Synthesis of classical and a nonclassical 2-amino-4-oxo-6-methyl-5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of thymidylate synthase.EBI J Med Chem 42: 2272-9 (1999) Duquesne University 2D 3D TSV
10377231 2 Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.EBI J Med Chem 42: 2251-9 (1999) CEA/DSV 2D 3D TSV
10377229 107 New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI J Med Chem 42: 2235-44 (1999) University of Göteborg 2D 3D TSV
10377223 57 Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.EBI J Med Chem 42: 2180-90 (1999) Merck Research Laboratories 2D 3D TSV
10377221 44 Butenolide endothelin antagonists with improved aqueous solubility.EBI J Med Chem 42: 2162-8 (1999) Warner-Lambert Company 2D 3D TSV
10377218 13 Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.EBI J Med Chem 42: 2125-35 (1999) Schering-Plough Research Institute 2D 3D TSV
10377217 20 Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition.EBI J Med Chem 42: 2112-24 (1999) Università di Modena e Reggio Emilia 2D 3D TSV
10377215 104 Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.EBI J Med Chem 42: 2087-104 (1999) Merck, Sharp & Dohme Research Laboratories 2D 3D TSV
10375538 86 Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors.BDB Chem Biol 6: 361-75 (1999) University of California, Berkeley 2D 3D TSV
10374926 2 Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.BDB Life Sci 64: 2011-20 (1999) Hungarian Academy of Sciences 2D 3D TSV
10360758 10 Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.EBI Bioorg Med Chem Lett 9: 1469-74 (1999) Palatin Technologies Inc. 2D 3D TSV
10360757 14 The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.EBI Bioorg Med Chem Lett 9: 1463-8 (1999) Cardiff University 2D 3D TSV
10360755 17 P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.EBI Bioorg Med Chem Lett 9: 1453-8 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10360754 26 Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.EBI Bioorg Med Chem Lett 9: 1447-52 (1999) Tartu University 2D 3D TSV
10360750 2 Uncarinic acids: phospholipase Cgamma1 inhibitors from hooks of Uncaria rhynchophylla.EBI Bioorg Med Chem Lett 9: 1429-32 (1999) Seoul National University 2D 3D TSV
10360749 97 Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).EBI Bioorg Med Chem Lett 9: 1423-8 (1999) The R. W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10360746 8 Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.EBI Bioorg Med Chem Lett 9: 1409-14 (1999) Institut de Recherches Servier 2D 3D TSV
10360745 40 Piperidine-renin inhibitors compounds with improved physicochemical properties.EBI Bioorg Med Chem Lett 9: 1403-8 (1999) F. Hoffmann-La Roche Ltd. 2D 3D TSV
10360744 26 Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.EBI Bioorg Med Chem Lett 9: 1397-402 (1999) F. Hoffmann-La Roche Ltd 2D 3D TSV
10360741 10 Efficient inhibition of muscle and liver glycogen phosphorylases by a new glucopyranosylidene-spiro-thiohydantoin.EBI Bioorg Med Chem Lett 9: 1385-90 (1999) Lajos Kossuth University 2D 3D TSV
10360740 35 N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.EBI Bioorg Med Chem Lett 9: 1379-84 (1999) POSTECH 2D 3D TSV
10360739 8 Acyl-CoA: cholesterol acyltransferase inhibitory activity of ginseng sapogenins, produced from the ginseng saponins.EBI Bioorg Med Chem Lett 9: 1375-8 (1999) Korea Research Institute of Bioscience and Biotechnology 2D 3D TSV
10360738 5 Synthesis and protein kinase C binding activity of benzolactam-V7.EBI Bioorg Med Chem Lett 9: 1371-4 (1999) Institute of Organic Chemistry 2D 3D TSV
10360736 2 S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp.EBI Bioorg Med Chem Lett 9: 1361-4 (1999) Kirin Brewery Co., Ltd. 2D 3D TSV
10360732 45 trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.EBI Bioorg Med Chem Lett 9: 1341-6 (1999) Abbott Laboratories 2D 3D TSV
10354414 5 Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.EBI J Med Chem 42: 2053-9 (1999) The Royal Danish School of Pharmacy 2D 3D TSV
10354412 8 Simplified pepstatins: synthesis and evaluation of N-terminally modified analogues.EBI J Med Chem 42: 2041-5 (1999) Institute of Pharmaceutical Chemistry and Institute of Pharmaceutical Technology 2D 3D TSV
10354409 131 New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.EBI J Med Chem 42: 2007-20 (1999) Wyeth-Ayerst Research Laboratories 2D 3D TSV
10354408 58 1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.EBI J Med Chem 42: 1999-2006 (1999) Novo Nordisk A/S 2D 3D TSV
10354406 23 3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.EBI J Med Chem 42: 1982-90 (1999) University of Kansas 2D 3D TSV
10354405 31 Unique analogues of anandamide: arachidonyl ethers and carbamates and norarachidonyl carbamates and ureas.EBI J Med Chem 42: 1975-81 (1999) Organix, Inc. 2D 3D TSV
10354404 60 Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a.EBI J Med Chem 42: 1965-74 (1999) University of Queensland 2D 3D TSV
10354399 90 Quantitative structure-activity relationship of human neutrophil collagenase (MMP-8) inhibitors using comparative molecular field analysis and X-ray structure analysis.EBI J Med Chem 42: 1908-20 (1999) Hoechst Marion Roussel 2D 3D TSV
10354398 12 Lamellarin alpha 20-sulfate, an inhibitor of HIV-1 integrase active against HIV-1 virus in cell culture.EBI J Med Chem 42: 1901-7 (1999) Institute of Chemical Technology 2D 3D TSV
10354397 28 Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors.EBI J Med Chem 42: 1894-900 (1999) Dipartimento di Scienze Farmaceutiche 2D 3D TSV
10354396 32 1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.EBI J Med Chem 42: 1881-93 (1999) Universit£ di Modena 2D 3D TSV
10354394 216 Highly potent cyclic disulfide antagonists of somatostatin.EBI J Med Chem 42: 1863-71 (1999) Tulane University School of Medicine 2D 3D TSV
10353842 147 Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R).BDB Biochemistry 38: 7307-20 (1999) National Institute of Diabetes and Digestive and Kidney Diseases 2D 3D TSV
10347254 11 Cloning and functional expression of the human histamine H3 receptor.BDB Mol Pharmacol 55: 1101-7 (1999) R.W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10346939 30 Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.EBI J Med Chem 42: 1855-61 (1999) National Institute on Aging Intramural Research Program 2D 3D TSV
10346937 15 Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase.EBI J Med Chem 42: 1842-8 (1999) Wake Forest University 2D 3D TSV
10346932 53 Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.EBI J Med Chem 42: 1803-15 (1999) University of Auckland 2D 3D TSV
10346931 18 Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.BDB J Med Chem 42: 1789-802 (1999) Japan Energy Corporation 2D 3D TSV
10346928 19 Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.EBI J Med Chem 42: 1757-66 (1999) Boehringer Ingelheim Pharmaceuticals Inc. 2D 3D TSV
10346927 114 Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI J Med Chem 42: 1749-56 (1999) Berlex Biosciences 2D 3D TSV
10346925 40 Homology modeling of gelatinase catalytic domains and docking simulations of novel sulfonamide inhibitors.EBI J Med Chem 42: 1723-38 (1999) Shionogi & Company, Ltd. 2D 3D TSV
10346920 2 4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors.EBI J Med Chem 42: 1684-6 (1999) SIBIA Neurosciences Inc. 2D 3D TSV
10340630 3 Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.BDB Synapse 32: 198-211 (1999) McGill University 2D 3D TSV
10340624 72 4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.EBI Bioorg Med Chem Lett 9: 1335-40 (1999) Ligand Pharmaceuticals, Inc. 2D 3D TSV
10340623 31 Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.EBI Bioorg Med Chem Lett 9: 1329-34 (1999) Organon Laboratories Ltd. 2D 3D TSV
10340622 47 Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.EBI Bioorg Med Chem Lett 9: 1323-8 (1999) Organon Laboratories Ltd. 2D 3D TSV
10340621 17 Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: ion-dipole interactions with lysine 60G.EBI Bioorg Med Chem Lett 9: 1317-22 (1999) Novartis Horsham Research Center 2D 3D TSV
10340620 30 Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.EBI Bioorg Med Chem Lett 9: 1311-6 (1999) Merck Research Laboratories 2D 3D TSV
10340616 6 Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.EBI Bioorg Med Chem Lett 9: 1291-4 (1999) Università degli Studi di L'Aquila 2D 3D TSV
10340615 51 4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.EBI Bioorg Med Chem Lett 9: 1285-90 (1999) Merck Sharp and Dohme Research Laboratories 2D 3D TSV
10340614 20 Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.EBI Bioorg Med Chem Lett 9: 1279-84 (1999) The DuPont Pharmaceutical Co. 2D 3D TSV
10340613 4 Inhibition of human telomerase by PNA-cationic peptide conjugates.EBI Bioorg Med Chem Lett 9: 1273-8 (1999) University of Cambridge 2D 3D TSV
10340610 2 Isotope edited NMR studies of glycosidases: design and synthesis of a novel glycosidase inhibitor.EBI Bioorg Med Chem Lett 9: 1255-60 (1999) Ohio State University 2D 3D TSV
10340609 15 L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.EBI Bioorg Med Chem Lett 9: 1251-4 (1999) Merck Research Laboratories 2D 3D TSV
10340605 5 Synthesis and evaluation of geldanamycin-estradiol hybrids.EBI Bioorg Med Chem Lett 9: 1233-8 (1999) Department of Medicine, Sloan-Kettering Institute for Cancer Research, New York, NY 10021, USA. 2D 3D TSV
10340604 22 Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.EBI Bioorg Med Chem Lett 9: 1227-32 (1999) Research and Development 2D 3D TSV
10340602 100 Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506.EBI Bioorg Med Chem Lett 9: 1219-24 (1999) Banyu Tsukuba Research Institute 2D 3D TSV
10336515 3 Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.BDB J Pharmacol Exp Ther 289: 1262-70 (1999) Banyu Pharmaceutical Co., Ltd. 2D 3D TSV
10336510 53 Pharmacological characterization of nicotine's interaction with cocaine and cocaine analogs.BDB J Pharmacol Exp Ther 289: 1229-36 (1999) Virginia Commonwealth University 2D 3D TSV
10329466 12 Synthesis of the quinoline-linked triazolopyrimidine analogues and their interactions with the recombinant tobacco acetolactate synthase.EBI Biochem Biophys Res Commun 258: 797-801 (1999) Seoul Women's University 2D 3D TSV
10328312 27 Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.EBI Bioorg Med Chem Lett 9: 1195-200 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10328310 15 Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.EBI Bioorg Med Chem Lett 9: 1185-8 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10328309 3 Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.EBI Bioorg Med Chem Lett 9: 1179-84 (1999) Biomolecular Engineering Research Institute 2D 3D TSV
10328307 24 Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.EBI Bioorg Med Chem Lett 9: 1171-4 (1999) G.D. Searle-Monsanto 2D 3D TSV
10328306 58 Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors.EBI Bioorg Med Chem Lett 9: 1167-70 (1999) G.D. Searle-Monsanto 2D 3D TSV
10328300 4 Synthesis and biological activity of trans-2,3-dihydroraloxifene.EBI Bioorg Med Chem Lett 9: 1137-40 (1999) Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285-4813, USA. 2D 3D TSV
10328297 13 Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.EBI Bioorg Med Chem Lett 9: 1121-6 (1999) Warner-Lambert Company 2D 3D TSV
10328293 23 The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.EBI Bioorg Med Chem Lett 9: 1103-8 (1999) Novartis Horsham Research Centre 2D 3D TSV
10328291 4 Synthesis of caged peptides using caged lysine: application to the synthesis of caged AIP, a highly specific inhibitor of calmodulin-dependent protein kinase II.EBI Bioorg Med Chem Lett 9: 1093-6 (1999) Osaka National Research Institute, AIST, Ikeda, Japan. 2D 3D TSV
10328287 46 Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.EBI Bioorg Med Chem Lett 9: 1069-74 (1999) Abbott Laboratories 2D 3D TSV
10327430 60 Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.BDB Neuropsychopharmacology 20: 612-27 (1999) University of North Carolina 2D 3D TSV
10322128 13 Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.BDB Chem Biol 6: 265-75 (1999) Ligand Pharmaceuticals, Inc 2D 3D TSV
10322126 60 Structure-based discovery and in-parallel optimization of novel competitive inhibitors of thymidylate synthase.BDB Chem Biol 6: 319-31 (1999) Northwestern University 2D 3D TSV
10230641 14 Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.EBI Bioorg Med Chem Lett 9: 1063-6 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10230640 33 4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.EBI Bioorg Med Chem Lett 9: 1057-62 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10230630 36 Thrombin inhibitors based on a propargylglycine template.EBI Bioorg Med Chem Lett 9: 1013-8 (1999) Biotech Research Institute 2D 3D TSV
10230629 69 Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.EBI Bioorg Med Chem Lett 9: 1009-12 (1999) Ligand Pharmaceuticals, Inc. 2D 3D TSV
10230628 95 Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.EBI Bioorg Med Chem Lett 9: 1003-8 (1999) Ligand Pharmaceuticals 2D 3D TSV
10230627 14 6-(1-Hydroxyalkyl))penam sulfone derivatives as inhibitors of class A and class C beta-lactamases II.EBI Bioorg Med Chem Lett 9: 997-1002 (1999) Wyeth-Ayerst Research 2D 3D TSV
10230626 22 6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C beta-lactamases I.EBI Bioorg Med Chem Lett 9: 991-6 (1999) Wyeth-Ayerst Research 2D 3D TSV
10230624 110 N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.EBI Bioorg Med Chem Lett 9: 979-84 (1999) The R.W. Johnson Pharmaceutical Research Institute 2D 3D TSV
10230623 10 Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin.EBI Bioorg Med Chem Lett 9: 973-8 (1999) University of Minnesota 2D 3D TSV
10230622 25 Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.EBI Bioorg Med Chem Lett 9: 967-72 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10230616 30 Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.EBI Bioorg Med Chem Lett 9: 943-8 (1999) Searle Discovery Research 2D 3D TSV
10230615 60 Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.EBI Bioorg Med Chem Lett 9: 937-42 (1999) Du Pont Pharmaceuticals Company 2D 3D TSV
10230614 7 Adenosine receptor ligands with oxygenated N6-substituents.EBI Bioorg Med Chem Lett 9: 933-6 (1999) Deakin University 2D 3D TSV
10230612 22 Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.EBI Bioorg Med Chem Lett 9: 925-30 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10230611 48 Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.EBI Bioorg Med Chem Lett 9: 919-24 (1999) The DuPont Pharmaceutical Company 2D 3D TSV
10230610 12 Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.EBI Bioorg Med Chem Lett 9: 913-8 (1999) BioChem Therapeutic Inc. 2D 3D TSV
10229636 30 delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.EBI J Med Chem 42: 1673-9 (1999) National Institute of Diabetes 2D 3D TSV
10229632 2 Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands.EBI J Med Chem 42: 1639-47 (1999) University of Minnesota 2D 3D TSV
10229631 36 Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.EBI J Med Chem 42: 1625-38 (1999) National Institute of Diabetes 2D 3D TSV
10229627 11 Development of fluorine-18-labeled 5-HT1A antagonists.EBI J Med Chem 42: 1576-86 (1999) National Institutes of Health 2D 3D TSV
10229626 66 Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.EBI J Med Chem 42: 1556-75 (1999) Universit£ di Siena 2D 3D TSV
10229625 16 Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.EBI J Med Chem 42: 1546-55 (1999) Parc Club Orsay Université 2D 3D TSV
10229623 82 Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors.EBI J Med Chem 42: 1525-36 (1999) Pharmacia and Upjohn 2D 3D TSV
10229620 3 Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore.EBI J Med Chem 42: 1501-4 (1999) University of Tokyo 2D 3D TSV
10229619 4 Emerging molecular approaches to pain therapy.EBI J Med Chem 42: 1481-500 (1999) Abbott Laboratories 2D 3D TSV
10227113 22 Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.BDB Schizophr Res 37: 107-22 (1999) Lilly Research Laboratories 2D 3D TSV
10224099 14 Structural elements of the gamma-aminobutyric acid type A receptor conferring subtype selectivity for benzodiazepine site ligands.BDB J Biol Chem 274: 13370-4 (1999) Synthélabo 2D 3D TSV
10220855 3 A transfected cell model for the renal toxin transporter, rOCT2.EBI Toxicol Sci 47: 181-6 (1999) University of Texas M. D. Anderson Cancer Center 2D 3D TSV
10220563 10 Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.EBI Mol Pharmacol 55: 847-54 (1999) Kyorin University School of Medicine 2D 3D TSV
10218828 16 Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis.BDB Bioorg Med Chem 7: 351-7 (1999) Hong Kong University of Science and Technology 2D 3D TSV
10215699 19 Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.BDB J Pharmacol Exp Ther 289: 1151-9 (1999) Gliatech Inc. 2D 3D TSV
10215672 11 Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001.BDB J Pharmacol Exp Ther 289: 926-35 (1999) Taisho Pharmaceutical Co., Ltd. 2D 3D TSV
10212133 93 5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.EBI J Med Chem 42: 1466-72 (1999) Ligand Pharmaceuticals, Inc. 2D 3D TSV
10212129 20 Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.EBI J Med Chem 42: 1428-40 (1999) University of California 2D 3D TSV
10212126 54 Chicoric acid analogues as HIV-1 integrase inhibitors.EBI J Med Chem 42: 1401-14 (1999) National Cancer Institute 2D 3D TSV
10212125 14 N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.EBI J Med Chem 42: 1393-400 (1999) Leiden/Amsterdam Center for Drug Research 2D 3D TSV
10212124 26 5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.EBI J Med Chem 42: 1384-92 (1999) Leiden University 2D 3D TSV
10212123 5 Bound structures of novel P3-P1' beta-strand mimetic inhibitors of thrombin.EBI J Med Chem 42: 1376-83 (1999) Michigan State University 2D 3D TSV
10212122 35 Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI J Med Chem 42: 1367-75 (1999) Molecumetics Ltd. 2D 3D TSV
10212120 34 Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines.EBI J Med Chem 42: 1348-57 (1999) Affymax Research Institute 2D 3D TSV
10212118 44 Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.EBI J Med Chem 42: 1333-40 (1999) Yale University 2D 3D TSV
10206559 18 N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.EBI Bioorg Med Chem Lett 9: 907-12 (1999) Warner-Lambert Company 2D 3D TSV
10206558 50 Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.EBI Bioorg Med Chem Lett 9: 901-6 (1999) Schering-Plough Research Institute 2D 3D TSV
10206557 36 Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.EBI Bioorg Med Chem Lett 9: 895-900 (1999) Corvas International, Inc. 2D 3D TSV
10206553 55 Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.EBI Bioorg Med Chem Lett 9: 875-80 (1999) Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. 2D 3D TSV
10206551 15 Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.EBI Bioorg Med Chem Lett 9: 863-8 (1999) Merck Research Laboratories 2D 3D TSV
10206550 28 Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters.EBI Bioorg Med Chem Lett 9: 857-62 (1999) Organix Inc 2D 3D TSV
10206549 2 Synthesis and activity of gamma-(L-gamma-azaglutamyl)-S-(p-bromobenzyl)-L-cysteinylglycine: a metabolically stable inhibitor of glyoxalase I.EBI Bioorg Med Chem Lett 9: 853-6 (1999) University of Minnesota 2D 3D TSV
10206548 6 Novel reverse-turn mimics inhibit farnesyl transferase.EBI Bioorg Med Chem Lett 9: 847-52 (1999) Cold Spring Harbor Laboratory 2D 3D TSV
10206547 95 Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.EBI Bioorg Med Chem Lett 9: 841-6 (1999) Universit£t Erlangen-N£rnberg 2D 3D TSV
10206546 27 Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.EBI Bioorg Med Chem Lett 9: 835-40 (1999) Warner-Lambert Company 2D 3D TSV
10206545 40 Ring constrained analogues of the orvinols: the furanomorphides.EBI Bioorg Med Chem Lett 9: 831-4 (1999) University of Bristol 2D 3D TSV
10206542 50 Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.EBI Bioorg Med Chem Lett 9: 815-20 (1999) Warner-Lambert Company 2D 3D TSV
10206539 1 A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.EBI Bioorg Med Chem Lett 9: 803-6 (1999) Kyoto Pharmaceutical University 2D 3D TSV
10201849 3 Synthesis of alpha-C(1-->3)-mannopyranoside of N-acetylgalactosamine, a new beta-galactosidase inhibitor.EBI Bioorg Med Chem Lett 9: 793-6 (1999) Institut de chimie organique de l'Université de Lausanne 2D 3D TSV
10201846 17 Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.EBI Bioorg Med Chem Lett 9: 775-80 (1999) Lilly Research Laboratories 2D 3D TSV
10201844 24 Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.EBI Bioorg Med Chem Lett 9: 765-70 (1999) A Subsidiary of Agouron Pharmaceuticals, Inc. 2D 3D TSV
10201842 69 Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.EBI Bioorg Med Chem Lett 9: 755-8 (1999) Merck Research Laboratories 2D 3D TSV
10201841 47 Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.EBI Bioorg Med Chem Lett 9: 749-54 (1999) Merck Research Laboratories 2D 3D TSV
10201840 33 A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.EBI Bioorg Med Chem Lett 9: 743-8 (1999) Allergan Pharmaceuticals 2D 3D TSV
10201839 22 Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.EBI Bioorg Med Chem Lett 9: 737-42 (1999) Novartis Horsham Research Center 2D 3D TSV
10201832 34 Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.EBI Bioorg Med Chem Lett 9: 703-8 (1999) Abbott Laboratories 2D 3D TSV
10201830 9 First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.EBI Bioorg Med Chem Lett 9: 691-6 (1999) Pohang University of Science and Technology 2D 3D TSV
10201829 9 1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.EBI Bioorg Med Chem Lett 9: 685-90 (1999) NV Organon 2D 3D TSV
10201827 7 Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.EBI Bioorg Med Chem Lett 9: 673-8 (1999) Department of Medicinal Chemistry, Merck Research Laboratories, Merck& Co., Inc., Rahway, New Jersey 07065-0900, USA. 2D 3D TSV
10201826 24 Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.EBI Bioorg Med Chem Lett 9: 667-72 (1999) Albert Szent-Gy£rgyi Medical University 2D 3D TSV
10201825 2 Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.EBI Bioorg Med Chem Lett 9: 663-6 (1999) Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA. 2D 3D TSV
10201822 20 Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.EBI Bioorg Med Chem Lett 9: 647-52 (1999) Eli Lilly and Company 2D 3D TSV
10201821 166 Potent, orally absorbed glucagon receptor antagonists.EBI Bioorg Med Chem Lett 9: 641-6 (1999) Merck Research Laboratories 2D 3D TSV
10198227 3 PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.EBI Biochem Biophys Res Commun 257: 410-3 (1999) University of Tennessee Medical Center 2D 3D TSV
10197974 22 Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.EBI J Med Chem 42: 1312-9 (1999) INSERM 2D 3D TSV
10197973 4 Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: optimization from lipid profiles.EBI J Med Chem 42: 1306-11 (1999) Zeneca Pharmaceuticals 2D 3D TSV
10197972 133 1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.EBI J Med Chem 42: 1293-305 (1999) Tanabe Seiyaku Company, Ltd. 2D 3D TSV
10197970 88 2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.EBI J Med Chem 42: 1274-81 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10197969 5 Enzyme-assisted total synthesis of the optical antipodes D-myo-inositol 3,4,5-trisphosphate and D-myo-inositol 1,5, 6-trisphosphate: aspects of their structure-activity relationship to biologically active inositol phosphates.EBI J Med Chem 42: 1262-73 (1999) Bergische Universität Wuppertal 2D 3D TSV
10197967 70 Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.EBI J Med Chem 42: 1235-49 (1999) Boehringer Ingelheim Pharma KG 2D 3D TSV
10197965 13 Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.EBI J Med Chem 42: 1213-24 (1999) Agouron Pharmaceuticals, Inc. 2D 3D TSV
10197964 32 Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics.EBI J Med Chem 42: 1203-12 (1999) Agouron Pharmaceuticals, Inc. 2D 3D TSV
10197962 13 Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.EBI J Med Chem 42: 1178-92 (1999) The DuPont Merck Pharmaceutical Company 2D 3D TSV
10197960 171 Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.EBI J Med Chem 42: 1161-9 (1999) Warner-Lambert Company 2D 3D TSV
10197959 92 Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.EBI J Med Chem 42: 1151-60 (1999) Warner-Lambert Company 2D 3D TSV
10196521 2 Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter.EBI Nat Neurosci 1: 349-51 (1999) University of Heidelberg 2D 3D TSV
10098677 14 Solid-phase synthesis of novel inhibitors of farnesyl transferase.EBI Bioorg Med Chem Lett 9: 623-6 (1999) Institute of Cancer Research 2D 3D TSV
10098676 52 Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.EBI Bioorg Med Chem Lett 9: 619-22 (1999) Merck KGaA 2D 3D TSV
10098675 6 Homoisofagomines: chemical-enzymatic synthesis and evaluation as alpha- and beta-glucosidase inhibitors.EBI Bioorg Med Chem Lett 9: 615-8 (1999) Technische Universit£t Berlin 2D 3D TSV
10098670 24 Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.EBI Bioorg Med Chem Lett 9: 589-94 (1999) Allergan Inc. 2D 3D TSV
10098669 33 Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.EBI Bioorg Med Chem Lett 9: 585-8 (1999) Merck Sharp & Dohme Research Laboratories 2D 3D TSV
10098666 48 High affinity retinoic acid receptor antagonists: analogs of AGN 193109.EBI Bioorg Med Chem Lett 9: 573-6 (1999) Allergan Inc. 2D 3D TSV
10098663 81 Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs.EBI Bioorg Med Chem Lett 9: 559-62 (1999) University of Tokyo 2D 3D TSV
10098661 3 Inhibition of 4-hydroxyphenylpyruvate dioxygenase by sethoxydim, a potent inhibitor of acetyl-coenzyme A carboxylase.EBI Bioorg Med Chem Lett 9: 551-4 (1999) Tunghai Christian University 2D 3D TSV
10098659 1 Synthesis of 5,8-dimethoxy-3-hydroxy-4-quinolone, a reported inhibitor of HIV RT, and evidence the original proposed structure was incorrect.EBI Bioorg Med Chem Lett 9: 543-6 (1999) MediChem Research, Inc. 2D 3D TSV
10098657 2 (3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.EBI Bioorg Med Chem Lett 9: 533-8 (1999) Kyorin Pharmaceutical Co., Ltd. 2D 3D TSV
10098656 13 Synthesis and biological evaluation of alpha,alpha-difluorobenzylphosphonic acid derivatives as small molecular inhibitors of protein-tyrosine phosphatase 1B.EBI Bioorg Med Chem Lett 9: 529-32 (1999) Tokyo University of Pharmacy & Life Science 2D 3D TSV
10098655 9 Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene.EBI Bioorg Med Chem Lett 9: 523-8 (1999) Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. 2D 3D TSV
10096862 3 bis-5-Alkylresorcinols from Panopsis rubescens that inhibit DNA polymerase beta.EBI J Nat Prod 62: 477-80 (1999) University of Virginia 2D 3D TSV
10091708 32 Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.EBI Bioorg Med Chem Lett 9: 491-6 (1999) Merck Research Laboratories 2D 3D TSV
10091706 176 Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.EBI Bioorg Med Chem Lett 9: 481-6 (1999) Department of Medicinal Chemistry, University of Kansas, Lawrence 66045, USA. 2D 3D TSV
10091705 51 Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2 side chain.EBI Bioorg Med Chem Lett 9: 475-80 (1999) Lilly Research Laboratories 2D 3D TSV
10091703 8 The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold.EBI Bioorg Med Chem Lett 9: 463-8 (1999) Novartis Institute for Medical Sciences 2D 3D TSV
10091702 2 Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity.EBI Bioorg Med Chem Lett 9: 459-62 (1999) Novartis Pharma AG 2D 3D TSV
10091700 36 Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism.EBI Bioorg Med Chem Lett 9: 449-52 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10091699 97 Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones.EBI Bioorg Med Chem Lett 9: 443-8 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10091698 12 Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.EBI Bioorg Med Chem Lett 9: 437-42 (1999) Université de Lille II 2D 3D TSV
10091697 6 Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin.EBI Bioorg Med Chem Lett 9: 431-6 (1999) Glaxo Wellcome Research and Development 2D 3D TSV
10091694 90 Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.EBI Bioorg Med Chem Lett 9: 413-8 (1999) Nippon Steel Corporation 2D 3D TSV
10091693 23 The synthesis and evaluation of temperature sensitive tubulin toxins.EBI Bioorg Med Chem Lett 9: 407-12 (1999) Department of Chemistry, University of Virginia, Charlottesville 22901, USA. 2D 3D TSV
10091692 44 Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.EBI Bioorg Med Chem Lett 9: 401-6 (1999) Zeria Pharmaceutical Co., Ltd. 2D 3D TSV
10091687 52 Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.EBI Bioorg Med Chem Lett 9: 375-80 (1999) Cubist Pharmaceuticals, Inc. 2D 3D TSV
10091684 10 The LMC delta opioid recognition pharmacophore: comparison of SNC80 and oxymorphindole.EBI Bioorg Med Chem Lett 9: 357-62 (1999) National Institute of Diabetes 2D 3D TSV
10091683 12 Periodinates: a new class of protein tyrosine phosphatase inhibitors.EBI Bioorg Med Chem Lett 9: 353-6 (1999) McGill University 2D 3D TSV
10091682 10 Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.EBI Bioorg Med Chem Lett 9: 347-52 (1999) National Cancer Institute 2D 3D TSV
10091679 9 New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.EBI Bioorg Med Chem Lett 9: 333-6 (1999) Nantes 2D 3D TSV
10091678 65 Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors.EBI Bioorg Med Chem Lett 9: 327-32 (1999) Hoechst Marion Roussel GmbH 2D 3D TSV
10091677 15 Substituted furans as inhibitors of the PDE4 enzyme.EBI Bioorg Med Chem Lett 9: 323-6 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10091675 31 Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis.EBI Bioorg Med Chem Lett 9: 313-8 (1999) Merck Research Laboratories 2D 3D TSV
10091674 36 Structure-based design of COX-2 selectivity into flurbiprofen.EBI Bioorg Med Chem Lett 9: 307-12 (1999) Merck Frosst Canada Inc. 2D 3D TSV
10091673 21 Synthesis of potent and selective inhibitors of human plasma kallikrein.EBI Bioorg Med Chem Lett 9: 301-6 (1999) The Procter& Gamble Company 2D 3D TSV
10090793 12 Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine.EBI J Med Chem 42: 1106-11 (1999) Purdue University 2D 3D TSV
10090791 77 Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.EBI J Med Chem 42: 1088-99 (1999) Tanabe Seiyaku Company, Ltd. 2D 3D TSV
10090790 131 Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.EBI J Med Chem 42: 1076-87 (1999) Taisho Pharmaceutical Company, Ltd. 2D 3D TSV
10090788 75 Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).EBI J Med Chem 42: 1053-65 (1999) SmithKline Beecham S.p.A. 2D 3D TSV
10090787 25 Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors.EBI J Med Chem 42: 1041-52 (1999) University of Antwerp (UIA) 2D 3D TSV
10090786 33 Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptorsEBI J Med Chem 42: 1027-40 (1999) Eli Lilly and Company 2D 3D TSV
10090785 63 Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.EBI J Med Chem 42: 1018-26 (1999) NOVARTIS Limited 2D 3D TSV
10090784 76 Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.EBI J Med Chem 42: 1007-17 (1999) Harvard Medical School 2D 3D TSV
10090780 28 Structural and conformational requirements for high-affinity binding to the SH2 domain of Grb2(1).EBI J Med Chem 42: 971-80 (1999) Novartis Forschungsinstitut 2D 3D TSV
10090778 9 Design, synthesis, and evaluation of conformationally constrained tongs, new inhibitors of HIV-1 protease dimerization.EBI J Med Chem 42: 957-62 (1999) Université de Paris-sud 2D 3D TSV
10090777 6 Novel inhibitors of carboxypeptidase G2 (CPG2): potential use in antibody-directed enzyme prodrug therapy.EBI J Med Chem 42: 951-6 (1999) Imperial College of Science 2D 3D TSV
10087037 2 Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.EBI J Pharmacol Exp Ther 289: 448-54 (1999) Rutgers University 2D 3D TSV
10087018 11 Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.BDB J Pharmacol Exp Ther 289: 304-11 (1999) University of Rochester 2D 3D TSV
10087012 8 Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line.BDB J Pharmacol Exp Ther 289: 251-60 (1999) Medical College of Georgia 2D 3D TSV
10082798 6 Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes.EBI Biochim Biophys Acta 1417: 224-31 (1999) Kyoto University Hospital 2D 3D TSV
10081621 4 Erythromycin derivatives ABT 229 and GM 611 act on motilin receptors in the rabbit duodenum.BDB Clin Exp Pharmacol Physiol 26: 242-5 (1999) University of Melbourne 2D 3D TSV
10075775 6 Sideroxylonal C, a new inhibitor of human plasminogen activator inhibitor type-1, from the flowers of Eucalyptus albens.EBI J Nat Prod 62: 324-6 (1999) Griffith University 2D 3D TSV
10075763 6 Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.EBI J Nat Prod 62: 294-6 (1999) Department of Horticulture and National Food Safety and Toxicology Center 2D 3D TSV
10075742 13 New bioactive flavonoids and stilbenes in cubé resin insecticide.EBI J Nat Prod 62: 205-10 (1999) University of California 2D 3D TSV
10072689 39 Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.EBI J Med Chem 42: 920-34 (1999) Biogen Inc. 2D 3D TSV
10072688 25 Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge.EBI J Med Chem 42: 910-9 (1999) Northwestern University 2D 3D TSV
10072687 18 Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists.EBI J Med Chem 42: 903-9 (1999) Gliatech Inc. 2D 3D TSV
10072686 25 Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase.EBI J Med Chem 42: 896-902 (1999) University of Connecticut 2D 3D TSV
10072685 82 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors.EBI J Med Chem 42: 882-95 (1999) School of Chemistry and Biochemistry 2D 3D TSV
10072684 8 Prediction of the binding free energies of new TIBO-like HIV-1 reverse transcriptase inhibitors using a combination of PROFEC, PB/SA, CMC/MD, and free energy calculations.EBI J Med Chem 42: 868-81 (1999) University of California at San Francisco 2D 3D TSV
10072683 4 Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase.EBI J Med Chem 42: 859-67 (1999) Emory University 2D 3D TSV
10072682 22 Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements.EBI J Med Chem 42: 849-58 (1999) University of Bonn 2D 3D TSV
10072681 113 Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.EBI J Med Chem 42: 833-48 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10072680 32 Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies.EBI J Med Chem 42: 819-32 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10072679 86 Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.EBI J Med Chem 42: 805-18 (1999) DuPont Pharmaceuticals Company 2D 3D TSV
10052994 6 CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs.EBI J Pharm Sci 88: 347-50 (1999) The University of Michigan 2D 3D TSV
10052983 40 Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.EBI J Med Chem 42: 769-76 (1999) University of Connecticut 2D 3D TSV
10052980 138 Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.EBI J Med Chem 42: 742-50 (1999) Ligand Pharmaceuticals, Inc 2D 3D TSV
10052979 45 Aminopyridazines as acetylcholinesterase inhibitors.EBI J Med Chem 42: 730-41 (1999) Universit£ Louis Pasteur 2D 3D TSV
10052978 22 Phosphotyrosine-containing dipeptides as high-affinity ligands for the p56lck SH2 domain.EBI J Med Chem 42: 722-9 (1999) Boehringer Ingelheim Pharmaceuticals Inc. 2D 3D TSV
10052977 82 Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.EBI J Med Chem 42: 706-21 (1999) National Institute of Diabetes 2D 3D TSV
10052976 126 3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.EBI J Med Chem 42: 691-705 (1999) Merck, Sharp and Dohme Research Laboratories 2D 3D TSV
10052975 129 Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.EBI J Med Chem 42: 677-90 (1999) Merck, Sharp and Dohme Research Laboratories 2D 3D TSV
10052973 36 Cycloalkanecarboxylic esters derived from lysergol, dihydrolysergol-I, and elymoclavine as partial agonists and antagonists at rat 5-HT2A receptors: pharmacological evidence that the indolo[4,3-fg]quinoline system of the ergolines is responsible for high 5-HT2A receptor affinity.EBI J Med Chem 42: 659-68 (1999) Freie Universit£t Berlin 2D 3D TSV
10052970 24 Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.EBI J Med Chem 42: 628-37 (1999) University of Minnesota 2D 3D TSV
10052969 50 5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.BDB J Med Chem 42: 619-27 (1999) Universita degli Studi di Roma La Sapienza 2D 3D TSV
10052968 3 Design and synthesis of novel amphiphilic dendritic galactosides for selective targeting of liposomes to the hepatic asialoglycoprotein receptor.EBI J Med Chem 42: 609-18 (1999) Leiden University 2D 3D TSV
10052966 30 Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.EBI J Med Chem 42: 593-600 (1999) Freie Universität Berlin 2D 3D TSV
10052963 7 New peptidic cysteine protease inhibitors derived from the electrophilic alpha-amino acid aziridine-2,3-dicarboxylic acid.EBI J Med Chem 42: 560-72 (1999) Albert-Ludwigs-University of Freiburg 2D 3D TSV
10052962 21 Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.EBI J Med Chem 42: 545-59 (1999) SmithKline Beecham Pharmaceuticals 2D 3D TSV
10052961 24 Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.EBI J Med Chem 42: 541-4 (1999) Rhône-Poulenc Rorer 2D 3D TSV
10051134 18 [3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum.BDB Br J Pharmacol 126: 179-88 (1999) Monash University 2D 3D TSV
10048786 2 Effects of the indolocarbazole 3744W on the tyrosine kinase activity of the cytoplasmic domain of the platelet-derived growth factor beta-receptor.EBI Cell Signal 11: 95-100 (1999) Wellcome Research Laboratories 2D 3D TSV
10021947 44 4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.EBI Bioorg Med Chem Lett 9: 291-4 (1999) Merck & Co. 2D 3D TSV
10021946 17 Identification of (-)-cis-6-acetyl-4S-(3-chloro-4-fluoro-benzoylamino)- 3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3S-ol as a potential antimigraine agent.EBI Bioorg Med Chem Lett 9: 285-90 (1999) SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK. 2D 3D TSV
10021945 8 Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1).EBI Bioorg Med Chem Lett 9: 279-84 (1999) University at Stony Brook 2D 3D TSV
10021944 8 Specific, uncompetitive inhibition of beta-galactosidases by a 5,6-isopropylidenedioxyfuro[2,3-d]isoxazole-3-methanol derivative.EBI Bioorg Med Chem Lett 9: 277-8 (1999) Institut de chimie organique de l'Université de Lausanne 2D 3D TSV
10021942 46 Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.EBI Bioorg Med Chem Lett 9: 265-70 (1999) Scripps Research Institute 2D 3D TSV
10021941 6 Synthesis and PLA2-inhibitory properties of 2(R)-acetamido-alkylphosphomethanols with a variable aggregate anchor.EBI Bioorg Med Chem Lett 9: 261-4 (1999) Tumor Biology Center 2D 3D TSV
10021933 11 Highly potent inhibitors of the Grb2-SH2 domain.EBI Bioorg Med Chem Lett 9: 221-6 (1999) Novartis Pharma Inc. 2D 3D TSV
10021927 80 Design and synthesis of thiol containing inhibitors of matrix metalloproteinases.EBI Bioorg Med Chem Lett 9: 195-200 (1999) Novartis Biomedical Research Institute 2D 3D TSV
10021923 54 Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor.EBI Bioorg Med Chem Lett 9: 179-84 (1999) SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK. 2D 3D TSV
10021922 10 Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety.EBI Bioorg Med Chem Lett 9: 173-8 (1999) University of Tokyo 2D 3D TSV
10021918 59 Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class.EBI Bioorg Med Chem Lett 9: 151-6 (1999) Merck Frosst Centre for Therapeutic Research 2D 3D TSV
10021917 4 Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110.EBI Bioorg Med Chem Lett 9: 145-50 (1999) MediChem Research, Inc. 2D 3D TSV
10021916 2 Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates.EBI Bioorg Med Chem Lett 9: 141-4 (1999) Duquesne University 2D 3D TSV
10021915 3 The synthesis of ketomethylene pseudopeptide analogues of dipeptide aldehyde inhibitors of calpain.EBI Bioorg Med Chem Lett 9: 139-40 (1999) Hoechst Marion Roussel, Inc. 2D 3D TSV
10021913 42 Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.EBI Bioorg Med Chem Lett 9: 127-32 (1999) Pfizer Inc 2D 3D TSV
10021912 32 Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate.EBI Bioorg Med Chem Lett 9: 123-6 (1999) DuPont Pharmaceuticals Company 2D 3D TSV

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