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Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 97-102 (1999)
Universit£T Erlangen-N£Rnberg
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 91-6 (1999)
Novartis Pharmaceuticals
The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 75-8 (1999)
Eli Lilly
Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 43-8 (1999)
Instituto De QuíMica MéDica (Csic)
A study of novel antiallergic agents with eosinophilic infiltration inhibiting action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 19-24 (1999)
Tokushima Bunri University
Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 9: 7-12 (1999)
Schering-Plough Research Institute
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 526-31 (1999)
Eli Lilly
Metallopeptidase inhibitors of tetanus toxin: A combinatorial approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 515-25 (1999)
University of Paris
Structure-activity relationships: analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 497-509 (1999)
University of California
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 490-6 (1999)
Università
Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 458-77 (1999)
University of Marburg
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 427-37 (1999)
Recordati
A new class of pseudopeptide antagonists of the kinin B1 receptor containing alkyl spacers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 409-14 (1999)
Institute of Mutagenesis and Differentiation
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 400-4 (1999)
Sapienza University of Rome
Identification and characterization of m1 selective muscarinic receptor antagonists1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 356-63 (1999)
Warner-Lambert
Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 336-45 (1999)
Angelini Ricerche
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 333-5 (1999)
University of Pennsylvania
Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3689-92 (1999)
Research Triangle Institute
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3683-8 (1999)
Corvas International
Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3677-82 (1999)
Smithkline Beecham Pharmaceuticals
Differential activity of rosiglitazone enantiomers at PPAR gamma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3657-8 (1999)
Glaxo Wellcome Research and Development
Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3649-52 (1999)
University of Maryland
Design and synthesis of novel conformationally restricted HIV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3637-42 (1999)
Vertex Pharmaceuticals
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3631-6 (1999)
Vertex Pharmaceuticals
(2Z,4E)-5-(5,6-dichloro-2-indolyl)-2-methoxy-N-(1,2,2,6,6- pentamethylpiperidin-4-yl)-2,4-pentadienamide, a novel, potent and selective inhibitor of the osteoclast V-ATPase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3621-6 (1999)
Smithkline Beecham Research Unit
Tricyclic ureas: a new class of HIV-1 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3615-20 (1999)
Dupont Pharmaceuticals
The solid phase synthesis of a series of tri-substituted hydantoin ligands for the somatostatin SST5 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3609-14 (1999)
Glaxo Wellcome Cambridge Chemistry Laboratory
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3603-8 (1999)
Nv Organon Scientific Development Group
The discovery of orally available thrombin inhibitors: studies towards the optimisation of CGH1668.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3583-8 (1999)
Novartis Horsham Research Center
Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3577-82 (1999)
Pfizer
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3571-6 (1999)
Universidad De Santiago De Compostela
Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3567-70 (1999)
University of Vigo
Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3537-42 (1999)
Aids Drug Screening and Development Laboratory
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3531-6 (1999)
Abbott Laboratories
Inhibition stereochemistry of hydroxamate inhibitors for thermolysin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3515-8 (1999)
Pohang University of Science and Technology
Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5' and 8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3505-10 (1999)
University of Washington
Design and synthesis of new secretory phospholipase A2 inhibitor of a phospholipid analog.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3495-8 (1999)
Kwansei Gakuin University
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3469-74 (1999)
Schering-Plough Research Institute
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 359: 7-10 (1999)
Schering-Plough Research Institute
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 359: 1-6 (1999)
Eli Lilly
Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Ann N Y Acad Sci 861: 140-5 (1998)
Albany Medical College
2,6-Difluorophenol as a bioisostere of a carboxylic acid: bioisosteric analogues of gamma-aminobutyric acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 329-32 (1999)
Northwestern University
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 312-23 (1999)
Nippon Steel
Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 305-11 (1999)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 260-6 (1999)
University College London
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 249-59 (1999)
Lindsley F. Kimball Research Institute
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 210-2 (1999)
Ligand Pharmaceuticals
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 202-5 (1999)
Smithkline Beecham Pharmaceuticals
Pharmacological treatment of obesity: therapeutic strategies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 181-201 (1999)
The R. W. Johnson Pharmaceutical Research Institute
Potent 3-spiropiperidine growth hormone secretagogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 107-12 (1999)
Merck Research Laboratories
Primary active transport of peptidic endothelin antagonists by rat hepatic canalicular membrane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 288: 575-81 (1999)
University of Tokyo
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 62: 173-5 (1999)
Harbor Branch Oceanographic Institution
Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jpn J Cancer Res 89: 1220-8 (1999)
Kobe University
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 173-7 (1999)
Università
Carboxy-substituted cinnamides: a novel series of potent, orally active LTB4 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 164-72 (1999)
Novartis Pharmaceuticals
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 42: 135-52 (1999)
Dupont Pharmaceuticals
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the alpha2-adrenoceptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 118-34 (1999)
University of Kansas
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 87-94 (1999)
Procter and Gamble Pharmaceuticals
Synthesis and structure-activity relationships of a new model of arylpiperazines. 4. 1-[omega-(4-Arylpiperazin-1-yl)alkyl]-3-(diphenylmethylene) - 2, 5-pyrrolidinediones and -3-(9H-fluoren-9-ylidene)-2, 5-pyrrolidinediones: study of the steric requirements of the terminal amide fragment on 5-HT1A a![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 36-49 (1999)
Universidad Complutense
Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 42: 25-35 (1999)
National Cancer Institute-Bethesda
Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 125: 1413-20 (1998)
Smithkline Beecham Pharmaceuticals
Cloning and characterization of the human galanin GALR2 receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Peptides 19: 1771-81 (1998)
Synaptic Pharmaceutical
Trypanocidal bisbenzylisoquinoline alkaloids are inhibitors of trypanothione reductase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzym Inhib 13: 1-9 (1998)
Orstom
Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 5457-65 (1998)
University of Auckland
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5445-56 (1999)
Institut FüR Biochemie
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5402-9 (1999)
Centro De InvestigacióN Grupo Ferrer
New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5393-401 (1999)
Universit£
The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5375-81 (1999)
Institute of Cancer Research
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5362-74 (1999)
Eli Lilly
Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5353-61 (1999)
University of Connecticut
Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3423-8 (1999)
Centre De Recherche Pierre Fabre
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3409-14 (1999)
Warner-Lambert
Conformationally constrained analogues of diacylglycerol (DAG). 15. The indispensable role of the sn-1 and sn-2 carbonyls in the binding of DAG-lactones to protein kinase C (PK-C).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3403-8 (1999)
National Institutes of Health
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3365-70 (1999)
Ligand Pharmaceuticals
Acceptor substrate-based selective inhibition of galactosyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3359-64 (1999)
Scripps Research Institute
Chemoenzymatic synthesis of iminocyclitol derivatives: a useful library strategy for the development of selective fucosyltransfer enzymes inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3353-8 (1999)
Scripps Research Institute
Potent inhibitors of the MAP kinase p38.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3335-40 (1998)
R. W. Johnson Pharmaceutical Research Institute
Synthesis of benzocycloalkane derivatives as new conformationally restricted ligands for melatonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3325-30 (1999)
Paris-Sud University
A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 8: 3321-4 (1998)
Gilead Sciences
Potent, non-thiol inhibitors of farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3311-6 (1999)
Merck Research Laboratories
Aryl C-glycosides: physiologically stable glycomimetics of sialyl Lewis X.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3307-10 (1999)
Sankyo
Restricting the flexibility of crosslinked, interfacial peptide inhibitors of HIV-1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3281-6 (1999)
Purdue University
Novel phosphate mimetics for the design of non-peptidyl inhibitors of protein tyrosine phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3275-80 (1999)
University of Toronto
Thio-sugars. IV: Design and synthesis of S-linked fucoside analogs as a new class of alpha-L-fucosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3265-8 (1999)
University of Connecticut
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3251-6 (1999)
Abbott Laboratories
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3229-34 (1999)
Novartis Horsham Research Center
Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3223-8 (1999)
Glaxowellcome Medicines Research Center
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3203-6 (1999)
Pharmacopeia
Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3193-8 (1999)
Biochem Therapeutic
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3171-6 (1999)
Smithkline Beecham Pharmaceuticals
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3165-70 (1999)
Smithkline Beecham Pharmaceuticals
Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3153-8 (1998)
Ajinomoto
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3149-52 (1999)
Research Triangle Institute
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3143-8 (1999)
Dupont Pharmaceuticals
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3127-32 (1999)
Neurogen
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3111-6 (1998)
Smithkline Beecham Pharmaceuticals
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3093-6 (1999)
Washington University
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3087-92 (1999)
Merck Research Laboratories
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3081-6 (1999)
Merck Research Laboratories
Orally active indole N-oxide PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3053-8 (1998)
Rh£Ne-Poulenc Rorer Central Research
Design, synthesis and biological activity of a pyrrolo [2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 3019-24 (1999)
Universit£
Preparation of biotinylated allosamidins with strong chitinase inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2987-90 (1998)
University of Tokyo
Synthesis of benzanilide derivatives as dual acting agents with alpha 1-adrenoceptor antagonistic action and steroid 5-alpha reductase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2967-72 (1998)
Zeria Pharmaceutical
Conformationally constrained NO synthase inhibitors: rigid analogs of L-N-iminoethylornithine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2961-6 (1999)
Université
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2955-60 (1999)
Glaxo Wellcome Research and Development
PDE4 inhibitors: new xanthine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2925-30 (1998)
Chiroscience
4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2907-12 (1999)
Pharmacia & Upjohn
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2897-902 (1999)
Novo Nordisk
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2891-6 (1999)
Novartis Pharma
Synthesis of benzo[c]quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5 alpha-reductase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2871-6 (1999)
Universit£
Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2865-70 (1999)
Novartis Pharma
Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2859-64 (1998)
Smithkline Beecham Pharmaceuticals
Synthesis and antiproliferative activity of a cyclic analog of dolastatin 10.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2855-8 (1999)
Laboratoire Des M£Canismes Mol£Culaires Des Communications Cellulaires (Cnrs Upr 9023)
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2849-54 (1999)
Eli Lilly
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2839-44 (1999)
Dupont Pharmaceuticals
Design and synthesis of a pyridone-based phosphotyrosine mimetic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2813-6 (1999)
Cadus Pharmaceutical
Design and synthesis of dipeptidyl alpha',beta'-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2809-12 (1999)
University of Michigan
Exploration of beta-turn scaffolding motifs as components of sialyl Le(X) mimetics and their relevance to P-selectin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2803-8 (1999)
Universit£
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2797-802 (1999)
Abbott Laboratories
Sialyl Lewis X-polysaccharide conjugates: targeting inflammatory lesions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2783-6 (1999)
Drug Delivery System Institute
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2777-82 (1999)
Merck Frosst Centre For Therapeutic Research
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2757-62 (1999)
Idun Pharmaceuticals
Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2747-50 (1999)
National Chung-Hsing University
2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2737-42 (1998)
Rh£Ne-Poulenc Rorer
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2731-6 (1999)
Ligand Pharmaceuticals
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2719-24 (1999)
Boehringer Ingelheim (Canada)
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2715-8 (1999)
Neurogen
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2705-10 (1999)
Dupont Pharmaceuticals
Pyrroles and other heterocycles as inhibitors of p38 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2689-94 (1999)
Merck Research Laboratory
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2685-8 (1999)
University of Michigan
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2681-4 (1999)
University of Michigan
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2675-80 (1999)
Wyeth-Ayerst Research Laboratory
Thalidomide analogs and PDE4 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2669-74 (1998)
Celgene
The synthesis and biological activity of a novel series of diazepine MMP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2657-62 (1999)
Wyeth-Ayerst Research
P2-proline-derived inhibitors of calpain I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2647-52 (1999)
Cephalon
Aryl sulfonamides as selective PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2635-40 (1999)
Chiroscience
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2629-34 (1998)
Chiroscience
Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2623-8 (1999)
Glaxowellcome Medicines Research Center
Synthesis and binding of stable bisubstrate ligands for phosphoglycerate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2603-8 (1998)
University of Sheffield
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2589-94 (1999)
Cambridge University Forvie Site
Synthesis of boronic acid analogs of L-arginine as alternate substrates or inhibitors of nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2573-6 (1999)
Université
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2563-8 (1999)
Biotech Research Institute
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2521-6 (1999)
Schering-Plough Research Institute
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2501-6 (1999)
Corvas International
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2495-500 (1999)
Merck
The development of novel and selective p56lck tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2489-94 (1999)
R. W. Johnson Pharmaceutical Research Institute
H-phosphonate derivatives as novel peptide deformylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2479-82 (1999)
Ohio State University
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2467-72 (1999)
Merck
Templates for design of inhibitors for serine proteases: application of the program DOCK to the discovery of novel inhibitors for thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2463-6 (1999)
Wayne State University
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2457-62 (1999)
Solvay Pharma
N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2451-6 (1999)
Pfizer
NMR and topochemical studies of peptidomimetic HIV-I protease inhibitors containing a cis-epoxide amide isostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2423-6 (1999)
Biotech Research Institute
Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2415-8 (1999)
Warner-Lambert
Synthesis of sialyl Lewis X mimetics using the Ugi four-component reaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2333-8 (1999)
Scripps Research Institute
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2321-6 (1999)
Molecumetics
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2315-20 (1999)
Pharmacopeia
Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2309-14 (1999)
Warner-Lambert
Exploring structure-activity relationships around the phosphomannose isomerase inhibitor AF14049 via combinatorial synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2303-8 (1999)
Affymax Research Institute
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2297-302 (1999)
University of California
Combinatorial chemistry: from peptides and peptidomimetics to small organic and heterocyclic compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2273-8 (1999)
Institute For Molecular Studies
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2263-8 (1999)
Schering-Plough Research Institute
L-tryptophan urea amides as NK1/NK2 dual antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2259-62 (1999)
Merck Research Laboratories
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2253-8 (1999)
Merck Research Laboratories
Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2247-52 (1999)
Takarazuka Research Institute
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2241-6 (1999)
Takarazuka Research Institute
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2235-40 (1999)
Berlex Biosciences
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2223-6 (1999)
Clemson University
Isoxazolylthioamides as potential immunosuppressants a combinatorial chemistry approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2203-8 (1999)
Novartis Pharma
Conformationally restricted analogues of nicotine and anabasine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2173-8 (1999)
Sibia Neurosciences
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2169-72 (1999)
Boehringer Ingelheim Pharmaceuticals
Novel H3 receptor antagonists. Sulfonamide homologs of histamine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2157-62 (1999)
Schering-Plough Research Institute
Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2149-50 (1999)
National Cancer Institute-Bethesda
Probing the importance of spacial and conformational domains in captopril analogs for angiotensin converting enzyme activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2123-8 (1999)
Universit£
Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2117-22 (1999)
Warner-Lambert
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2111-6 (1999)
Merck Research Laboratories
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2087-92 (1999)
Abbott Laboratories
Design and synthesis of conformationally-constrained MMP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2077-80 (1999)
Procter and Gamble Pharmaceuticals
Kampanols: novel Ras farnesyl-protein transferase inhibitors from Stachybotrys kampalensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2071-6 (1999)
Merck Research Laboratories
Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2067-70 (1999)
Warner-Lambert
Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[[(4-chlorophenyl)sulfonyl]-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2061-6 (1999)
Pfizer
SAR of novel biarylmethylamine dopamine D4 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2033-8 (1999)
Darmstadt
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2027-32 (1999)
Institute For Bioorganic Research
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2011-6 (1999)
Freie UniversitäT Berlin
Actinomycin D, C2 and VII, inhibitors of Grb2-SHC interaction produced by Streptomyces.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 2001-2 (1999)
Korea Research Institute of Bioscience and Biotechnology
Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1997-2000 (1998)
University of Tokyo
Identification and characterization of m4 selective muscarinic antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1991-6 (1999)
Parke-Davis Pharmaceutical Research
Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1985-90 (1999)
Eli Lilly
A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1949-52 (1998)
Chinese Academy of Science
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1943-8 (1999)
Eli Lilly
4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1935-40 (1999)
Zeneca Pharmaceuticals
SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1929-34 (1998)
R. W. Johnson Pharmaceutical Research Institute
Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1923-8 (1998)
R. W. Johnson Pharmaceutical Research Institute
Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K(+)-ATPase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1909-12 (1999)
Ajou University
17 alpha-alkyl- or 17 alpha-substituted benzyl-17 beta-estradiols: a new family of estrone-sulfatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1891-6 (1999)
Laval University
Inhibition of HIV integrase by novel nucleotides bearing tricyclic bases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1887-90 (1999)
University of Iowa
Novel cytokine release inhibitors. Part I: Triterpenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1883-6 (1999)
RhóNe-Poulenc Rorer Central Research
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1877-82 (1999)
Berlex Biosciences
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1867-72 (1998)
Rh£Ne-Poulenc Rorer Central Research
Synthesis and anti-HIV activities of symmetrical N1,N3-dibenzyl-2-hydroxy-propane derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1861-6 (1999)
Université
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1851-6 (1999)
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1845-50 (1999)
Merck Sharp and Dohme Research Laboratories
Modeling, synthesis and biological activity of novel antifungal agents (1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1819-24 (1998)
Nippon Roche Research Center
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1813-8 (1999)
National Taiwan University
Development of new chromanol antagonists of leukotriene D4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1791-6 (1998)
Pfizer
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1781-6 (1998)
Pfizer
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1771-6 (1999)
Merck
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1767-70 (1999)
Novo Nordisk
Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1757-62 (1999)
National Cancer Institute-Bethesda
Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1745-50 (1999)
Dupont Pharmaceuticals
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1719-24 (1999)
Merck Research Laboratories
Peptide-based inhibitors of the hepatitis C virus serine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1713-8 (1999)
Boehringer Ingelheim (Canada)
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1697-702 (1999)
Merck Research Laboratories
Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1689-92 (1998)
Glaxowellcome
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1683-6 (1999)
Biotech Research Institute
Identification of a potent analogue of Nazumamide A through iteration of combinatorial tetrapeptide libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1669-72 (1999)
Central Drug Research Institute
Synthesis and acetylcholinesterase inhibitory activity of (+/-)-14-fluorohuperzine A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1661-4 (1999)
Chinese Academy of Sciences
Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1649-54 (1999)
R. W. Johnson Pharmaceutical Research Institute
Adenosine deaminase inhibitors. Synthesis and biological evaluation of aralkyladenines (ARADS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1639-42 (1999)
University of Rhode Island
A new series of cyclic amino acids as inhibitors of S-adenosyl L-methionine synthetase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1629-34 (1999)
Umr 6519
Diarylsulfonamides as selective, non-peptidic thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1613-8 (1999)
Pharmazeutisch-Chemisches Institut Der UniversitäT
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1595-600 (1999)
3-Dimensional Pharmaceuticals
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1569-74 (1999)
Università
Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1563-8 (1999)
Royal Danish School of Pharmacy
Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1551-4 (1999)
Dainippon Pharmaceutical
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1541-6 (1999)
Yamanouchi Pharmaceutical
A potent dipeptide inhibitor of dipeptidyl peptidase IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1537-40 (1999)
Tanabe Seiyaku
Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1531-6 (1998)
Solvay Pharma
Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1521-4 (1999)
San Francisco State University
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1511-6 (1999)
Medivir
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1499-502 (1999)
Parke-Davis Pharmaceutical Research
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1477-82 (1999)
Institute For Drug Research
Inhibition of electric eel acetylcholinesterase by porphin compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1467-70 (1999)
Taejon National University of Technology
5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1461-6 (1999)
Institute
Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1449-54 (1999)
Fujisawa Pharmaceutical
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1443-8 (1999)
Abbott Laboratories
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1437-42 (1999)
Boehringer Ingelheim (Canada)
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1419-24 (1999)
University of Paris
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1407-12 (1999)
Centre De Recherche Pierre Fabre
New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1381-6 (1999)
Centre De Recherches De Croissy
Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1369-74 (1999)
Universit£
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1353-8 (1999)
University of Bologna
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1343-8 (1999)
Merck Sharp Laboratory
Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1337-42 (1999)
Centre De Recherche Pierre Fabre
A 3D-QSAR study on ginkgolides and their analogues with comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1291-6 (1999)
Chinese Academy of Sciences
A depsipeptide fungal metabolite inhibitor of cholesteryl ester transfer protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1277-80 (1999)
Schering-Plough Research Institute
Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1255-60 (1999)
Merck Frosst Centre For Therapeutic Research
1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1249-54 (1999)
Menarini Ricerche
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1237-42 (1999)
Pharmacia & Upjohn
Design and synthesis of bio-isosteres of thymidine triphosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1211-4 (1999)
University of Wales Cardiff
Direct synthesis of [DOTA-DPhe1]-octreotide and [DOTA-DPhe1,Tyr3]-octreotide (SMT487): two conjugates for systemic delivery of radiotherapeutical nuclides to somatostatin receptor positive tumors in man.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1207-10 (1999)
Novartis Pharma
Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: novel inhibitors of COX-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1181-6 (1999)
Boehringer Ingelheim Pharmaceuticals
Structure-activity relationships in 2-aminodiphenylsulfides against trypanothione reductase from Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1175-80 (1999)
Ura Cnrs 1309
Synthesis and anti-inflammatory activity of chalcone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1169-74 (1999)
Universidad De Valencia
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1163-8 (1999)
Wyeth-Ayerst Research
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1157-62 (1999)
Affymax Research Institute
Substrate specificity of human prolyl-4-hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1139-44 (1999)
Cornell University
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1133-8 (1999)
Gliatech
Serotonergic ergoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1117-22 (1999)
Pharmacia & Upjohn
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1107-12 (1999)
Merck Research Laboratories
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1101-6 (1999)
Merck Research Laboratories
The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 8: 1077-82 (1998)
Dupont Pharmaceuticals
Potent antimitotic and cell growth inhibitory properties of substituted chalcones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1051-6 (1999)
University of Manchester Institute of Science and Technology
Design and synthesis of a new type of non steroidal human aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1041-4 (1999)
Centre D'Etudes Et De Recherche Sur Le MéDicament De Normandie
Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 1019-22 (1999)
Kyushu University
Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 399-404 (1998)
Rh£Ne-Poulenc Rorer Central Research
Synthesis and 5 alpha-reductase inhibitory activity of 8-substituted benzo[f]quinolinones derived from palladium mediated coupling reactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 395-8 (1999)
Eli Lilly
A new strong inhibitor of beta-mannosidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 371-2 (1999)
S.E.S.N.A.B., Pole Sciences Et Technologie, Universit�
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 365-70 (1999)
Glaxo Wellcome Research and Development
Synthesis of novel cyclic protease inhibitors using Grubbs olefin metathesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 357-60 (1999)
University of Wisconsin-Madison
Naphthalenebis[alpha,alpha-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 345-50 (1999)
University of Toronto
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 333-8 (1999)
Proscript
Inhibition of thermolysin with nitrone-bearing substrate analogs: a new type of thermolysin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 323-6 (1999)
Pohang University of Science and Technology
Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 307-12 (1999)
Dupont Pharmaceuticals
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 301-6 (1999)
Dupont Pharmaceuticals
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 295-300 (1999)
Wyeth-Ayerst Research Laboratories
Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 289-94 (1999)
Warner-Lambert
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 281-4 (1999)
Pfizer
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 261-6 (1999)
Novartis Pharma
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 249-54 (1999)
Abbott Laboratories
Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 243-8 (1999)
Schering-Plough Research Institute
Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 209-14 (1999)
Cv Therapeutics
Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 195-8 (1999)
Purdue University
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 175-8 (1998)
Rh£Ne-Poulenc Rorer Central Research
S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 133-8 (1999)
Glaxo Wellcome Research and Development
Investigations of azapeptides as mimetics of Leu-enkephalin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 117-20 (1999)
Scripps Research Institute
DNA gyrase inhibitory activity of ellagic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 97-100 (1998)
R. W. Johnson Pharmaceutical Research Institute
Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) bearing a pyrazole ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 81-6 (1999)
Fujisawa Pharmaceutical
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 65-70 (1999)
Novartis Pharma
Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 63-4 (1999)
Cinc
High affinity phenylglycinol-based NK1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 51-6 (1999)
Merck Sharp and Dohme Research Laboratories
Selective inhibition of low affinity IgE receptor (CD23) processing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 29-34 (1999)
Smithkline Beecham Pharmaceuticals
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 23-8 (1999)
Smithkline Beecham Pharmaceuticals
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 17-22 (1999)
Merck
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 555-60 (1999)
University of Arizona
Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 529-34 (1999)
Abbott Laboratories
Novel bisphosphonate inhibitors of phosphoglycerate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 515-20 (1998)
Sheffield University
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 505-10 (1998)
RhôNe-Poulenc Rorer
5-Aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 493-8 (1999)
Novartis Pharma
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 487-92 (1999)
Hong Kong University of Science and Technology
Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 473-6 (1999)
Eli Lilly
A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 453-8 (1999)
Merck Frosst Center For Therapeutic Research
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 447-52 (1999)
Georgetown University Medical Center
Structure activity relationship study of known inhibitors of the enzyme 5 alpha-reductase (5AR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 409-14 (1999)
Kingston University
Solid phase synthesis of a biased mini tetrapeptoid-library for the discovery of monodentate ITAM mimics as ZAP-70 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 405-8 (1999)
Preclinical Research Novartis
Endothiopeptide inhibitors of HIV-1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 699-704 (1999)
Purdue University
Diimidazo[1,2-c:4',5'-e]pyrimidines: N6-N1 conformationally restricted adenosines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 695-8 (1999)
Griffith University
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 691-4 (1999)
Griffith University
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 8: 687-90 (1998)
University of Illinois At Chicago
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 675-80 (1999)
Centre De Recherche Pierre Fabre
Syntheses of D- and L-myo-inositol 1,2,4,5-tetrakisphosphate and stereoselectivity of the I(1,4,5)P3 receptor binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 659-62 (1999)
Pohang University of Science & Technology
Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 635-40 (1998)
Universite De Rennes
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 631-4 (1999)
Biotech Research Institute
A novel series of N-(hexahydro-1,4-diazepin-6-yl) and N-(hexahydroazepin- 3-yl)benzamides with high affinity for 5-HT3 and dopamine D2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 619-24 (1999)
Dainippon Pharmaceutical
An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 613-8 (1999)
Institute For Chemical Biology
1-[omega-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5- pyrrolidinediones as 5-HT1A receptor ligands: study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 581-6 (1999)
Universidad Complutense
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 575-80 (1999)
Istituto Di Strutturistica Chimica G. Giacomello
1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 569-74 (1999)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 567-8 (1999)
University of Pennsylvania
Synthesis and 5 alpha-reductase inhibitory activities of benzofuran derivatives with a carbamoyl group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 561-6 (1999)
Sankyo
Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 837-42 (1999)
Dupont Pharmaceuticals
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 823-8 (1999)
Dupont Pharmaceuticals
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 817-22 (1999)
Merck Research Laboratories
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 799-804 (1999)
National Institute of Diabetes
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 8: 793-8 (1998)
Institut Curie
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 775-80 (1999)
Dupont Pharmaceuticals
(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 765-70 (1999)
Eli Lilly
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 745-50 (1999)
Ligand Pharmaceuticals
Epoxide derivatives of pipecolic acid and proline are inhibitors of pipecolate oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 739-44 (1999)
Oregon State University
Solid phase synthesis of benzylamine-derived sulfonamide library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 735-8 (1999)
Biotech Research Institute
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 725-30 (1999)
Pfizer
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 715-20 (1999)
Dupont Pharmaceuticals
Syntheses and kinetic evaluation of hydroxamate-based peptide inhibitors of glyoxalase I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 705-10 (1999)
University of Waterloo
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 983-8 (1999)
R. W. Johnson Pharmaceutical Research Institute
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 979-82 (1999)
University of Illinois At Chicago
A 2-methyleneoxetane analog of orlistat demonstrating inhibition of porcine pancreatic lipase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 977-8 (1998)
University of Connecticut
Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 965-70 (1999)
Novartis Pharma
Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 959-64 (1999)
Ferring Research Institute
Peptide inhibitors of N-succinyl diaminopimelic acid aminotransferase (DAP-AT): a novel class of antimicrobial compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 945-50 (1999)
University of Bristol
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 931-4 (1999)
Schering-Plough Research Institute
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 925-30 (1999)
Georgetown University Medical Center
Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 919-24 (1999)
Green Cross Research Laboratories
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 913-8 (1999)
Green Cross Research Laboratories
Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 897-902 (1999)
Novartis Pharmaceuticals
Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 8: 891-6 (1999)
Abbott Laboratories
Structural analysis of inhibitor binding to human carbonic anhydrase II.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Protein Sci 7: 2483-9 (1998)
University of Pennsylvania
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 287: 860-7 (1998)
Second Tokushima Institute of New Drug Research
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5320-33 (1999)
Synaptic Pharmaceutical
Synthesis and potent antifolate activity and cytotoxicity of B-ring deaza analogues of the nonpolyglutamatable dihydrofolate reductase inhibitor Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl- L-ornithine (PT523).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5310-9 (1999)
Harvard Medical School
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5272-86 (1999)
Western Maryland College
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5265-71 (1999)
Trinity College
Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5247-56 (1999)
Newcastle University
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5198-218 (1999)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5188-97 (1999)
Research Triangle Institute
The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5177-87 (1999)
Kennesaw State University
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5167-76 (1999)
Vrije Universiteit Brussel
Enantiospecific semisynthesis of (+)-almuheptolide-A, a novel natural heptolide inhibitor of the mammalian mitochondrial respiratory chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5158-66 (1999)
Universidad De Valencia
Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5150-7 (1999)
Novo Nordisk
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5148-9 (1999)
Purdue University
Immunophilins: beyond immunosuppression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5119-43 (1999)
Guilford Pharmaceuticals
Role of the cofactor calcium in the activation of outer membrane phospholipase A.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 37: 16011-8 (1998)
Utrecht University
Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 358: 522-8 (1998)
King'S College London
Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 6: 1835-50 (1998)
Cnrs
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 5113-7 (1998)
Dupont Pharmaceuticals
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5084-93 (1999)
Virginia Commonwealth University
Design and synthesis of a series of 6-substituted-2-pyridinylmethylamine derivatives as novel, high-affinity, selective agonists at 5-HT1A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5070-83 (1998)
Pierre Fabre Research Center
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5055-69 (1998)
Glaxo Wellcome Research and Development
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5037-54 (1998)
Glaxo Wellcome Research and Development
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 5020-36 (1999)
Glaxo Wellcome Research and Development
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4995-5001 (1999)
Purdue University
Tetrahydro-isoquinoline-based factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4983-94 (1999)
Boehringer Mannheim
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4973-82 (1999)
Georgetown University Medical Center
Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4965-72 (1998)
Universit£T Regensburg
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4950-7 (1999)
National Institute of Diabetes and Digestive and Kidney Diseases
N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4933-8 (1999)
Universit£
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4911-4 (1999)
University of Minnesota
Muscarinic receptor binding sites of the M4 subtype in porcine lung parenchyma.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Pharmacol Toxicol 83: 200-7 (1998)
Case Western Reserve University
Baicalein, an alpha-glucosidase inhibitor from Scutellaria baicalensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1413-5 (1999)
Hokkaido University
Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1410-2 (1999)
Virginia Polytechnic Institute and State University
Isolation and structure elucidation of new PKCalpha inhibitors from Pinus flexilis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1407-9 (1998)
Virginia Polytechnic and State University
Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1356-60 (1999)
National University of Singapore
Inhibitory activity of unsaturated fatty acids and anacardic acids toward soluble tissue factor-factor VIIa complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1352-5 (1999)
Searle Discovery Research
Isolation of translactone-containing triterpenes with thrombin inhibitory activities from the leaves of Lantana camara.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1328-31 (1999)
Glaxo Wellcome Research and Development
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 71: 2558-64 (1998)
F. Hoffmann-La Roche
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 273: 32776-86 (1998)
Medical College of Georgia
Inhibition of human caspases by peptide-based and macromolecular inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 273: 32608-13 (1998)
Merck Research Laboratories
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4903-9 (1998)
Universitá
(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 4890-902 (1998)
Schering-Plough Research Institute
Human telomerase inhibition by regioisomeric disubstituted amidoanthracene-9,10-diones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4873-84 (1998)
The Institute of Cancer Research
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4854-60 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4833-43 (1998)
Institut Jacques Monod (Umr Cnrs 7592/UniversitéS Paris Vi and Vii)
Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4800-18 (1998)
Center In Molecular Toxicology and The Vanderbilt Cancer Center
Selective tight binding inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4790-9 (1998)
University of Washington
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4767-76 (1998)
The University of Arizona
Synthesis of 7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and novel derivatives free of positional isomers. Potent inhibitors of cAMP-specific phosphodiesterase and of malignant tumor cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4733-43 (1998)
University of Kaiserslautern
Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4706-15 (1998)
Ep811-Cnrs
Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4693-705 (1998)
Northeast Louisiana University
Novel CDC25A phosphatase inhibitors from pyrolysis of 3-alpha-azido-B-homo-6-oxa-4-cholesten-7-one on silica gel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4677-80 (1998)
University of Arizona
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 5: 597-608 (1998)
Dupont Pharmaceuticals
Transport of monoamine transmitters by the organic cation transporter type 2, OCT2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 273: 30915-20 (1998)
University of Heidelberg
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 287: 800-5 (1998)
Kyoto University Hospital
Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 287: 448-56 (1998)
Dupont Pharmaceuticals
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4623-35 (1998)
Merck Sharp and Dohme Research Laboratories
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4607-14 (1998)
Merck Research Laboratories
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4587-98 (1998)
Fujisawa Pharmaceutical
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4577-86 (1998)
Northwestern University Medical School
Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4567-76 (1998)
Smithkline Beecham Pharmaceuticals
Synthesis and enzymic evaluation of 4-mercapto-6-oxo-1, 4-azaphosphinane-2-carboxylic acid 4-oxide as an inhibitor of mammalian dihydroorotase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4550-5 (1998)
University of Sydney
Alkoxypsoralens, novel nonpeptide blockers of Shaker-type K+ channels: synthesis and photoreactivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4542-9 (1998)
University of Kiel
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4533-41 (1998)
Duquesne University
Three-dimensional quantitative structure-activity relationship study of the cannabimimetic (aminoalkyl)indoles using comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4521-32 (1998)
Sanofi Research Division
Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4492-501 (1998)
Merck Research Laboratories
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4486-91 (1998)
University of Minnesota
Synthesis and antitumor activity of new glycosides of epipodophyllotoxin, analogues of etoposide, and NK 611.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4475-85 (1998)
Umr 176 Cnrs/Institut Curie
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4466-74 (1998)
Merck Research Laboratories
Pharmacophoric search and 3D-QSAR comparative molecular field analysis studies on agonists of melatonin sheep receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4453-65 (1998)
Universit£
Highly potent bisphosphonate ligands for phosphoglycerate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4439-52 (1998)
University of Sheffield
TROTEC-1: a new high-affinity ligand for labeling of the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4429-32 (1998)
Institut F£R Bioanorganische Und Radiopharmazeutische Chemie
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Regul Pept 29-37 (1998)
Uppsala University
Cloning and functional expression of the guinea pig neuropeptide Y Y2 receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Regul Pept 23-8 (1998)
Uppsala University
The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hepatology 28: 1341-6 (1998)
University of Toronto
A new series of S-adenosyl-L-methionine synthetase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzym Inhib 13: 361-7 (1998)
Laboratoire De Chimie Bioorganique
New alkaloids from the papua new guinean sponge agelas nakamurai ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1310-2 (1998)
Kagoshima University
Activity-guided isolation of steroidal alkaloid antiestrogen-binding site inhibitors from Pachysandra procumbens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1257-62 (1998)
University of Illinois At Chicago
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1212-5 (1998)
Uppsala University
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 3. Discovery of a novel series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with weak toxicological effects on adrenal glands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4408-20 (1998)
Fujisawa Pharmaceutical
Potent cyano and carboxamido side-chain analogues of 1', 1'-dimethyl-delta8-tetrahydrocannabinol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4400-7 (1998)
Organix
CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4385-99 (1998)
University of Texas At Austin
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 4365-77 (1998)
Parke-Davis Pharmaceutical Research
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4354-9 (1998)
Ligand Pharmaceuticals
Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4329-42 (1998)
Warner-Lambert
Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4309-16 (1998)
Chugai Pharmaceutical
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4301-8 (1998)
Takeda Chemical Industries
Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4288-300 (1998)
Abbott Laboratories
Studies on selectin blockers. 7. Structure-activity relationships of sialyl Lewis X mimetics based on modified Ser-Glu dipeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4279-87 (1998)
Kanebo
Design of new topoisomerase II inhibitors based upon a quinobenzoxazine self-assembly model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4273-8 (1998)
The University of Texas At Austin
Quantitative structure-activity relationships of 2, 4-diamino-5-(2-X-benzyl)pyrimidines versus bacterial and avian dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4261-72 (1998)
University of California
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4251-60 (1998)
Wyeth-Ayerst Research
Design of benzamidine-type inhibitors of factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4240-50 (1998)
Institut FüR Biochemie
Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4232-9 (1998)
Takeda Chemical Industries
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4216-23 (1998)
Sw 8 Rh£Ne-Poulenc Rorer Central Research
Derivation of a pharmacophore model for anandamide using constrained conformational searching and comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4207-15 (1998)
Saint Louis University School of Medicine
Synthesis and evaluation of N-[11C]methylated analogues of epibatidine as tracers for positron emission tomographic studies of nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4199-206 (1998)
National Institute On Drug Abuse
6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4196-8 (1998)
The R. W. Johnson Pharmaceutical Research Institute
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4190-5 (1998)
Takeda Chemical Industries
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4186-9 (1998)
University of Bologna
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4181-5 (1998)
Astra Arcus Usa
SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 125: 202-8 (1998)
Smithkline Beecham Pharmaceuticals
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4171-6 (1998)
Freie UniversitäT Berlin
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4165-70 (1998)
University of Crete
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4150-60 (1998)
University of Bologna
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4143-9 (1998)
Research Triangle Institute
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4130-42 (1998)
University of Wisconsin-Milwaukee
Novel, highly potent aldose reductase inhibitors: (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine -4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4118-29 (1998)
Dainippon Pharmaceutical
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4062-79 (1998)
Fujisawa Pharmaceutical
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4053-61 (1998)
Fujisawa Pharmaceutical
New platelet fibrinogen receptor glycoprotein IIb-IIIa antagonists: orally active series of N-alkylated amidines with a 6,6-bicyclic template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4036-52 (1998)
Mitsui Pharmaceuticals
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4021-35 (1998)
RhôNe-Poulenc Rorer
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 4001-11 (1998)
University of Vienna
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3994-4000 (1998)
Vrije Universiteit
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3987-93 (1998)
Vrije Universiteit
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 3976-86 (1998)
University of Bologna
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3972-5 (1998)
F. Hoffmann-La Roche
Structure-based design of beta-lactamase inhibitors. 1. Synthesis and evaluation of bridged monobactams.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3961-71 (1998)
F. Hoffmann-La Roche
Geometrically and conformationally restrained cinnamoyl compounds as inhibitors of HIV-1 integrase: synthesis, biological evaluation, and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3948-60 (1998)
Sapienza University of Rome
N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3940-7 (1998)
Università
Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3928-39 (1998)
Yale University
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3923-7 (1998)
Smithkline Beecham Pharmaceuticals
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3919-22 (1998)
Glaxowellcome Medicines Research Centre
Reduced folate derivatives are endogenous substrates for cMOAT in rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Am J Physiol 275: 789-96 (1998)
University of Tokyo
Electrophysiological characteristics of the proton-coupled peptide transporter PEPT2 cloned from rat brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Am J Physiol 275: 967-75 (1998)
Medical College of Georgia
Structural basis of inhibitor selectivity in MAP kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Structure 6: 1117-28 (1998)
University of Texas At Dallas
Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Biophys Res Commun 250: 246-51 (1998)
State University of New Jersey
Thermodynamic analysis of the binding of the polyglutamate chain of 5-formyltetrahydropteroylpolyglutamates to serine hydroxymethyltransferase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 37: 13536-42 (1998)
Virginia Commonwealth University
Effect of modulators on the ATPase activity and vanadate nucleotide trapping of human P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Pharmacol 56: 719-27 (1998)
Eli Lilly
Novel peptidyl phosphorus derivatives as inhibitors of human calpain I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3912-6 (1998)
Cephalon
Naamidine A is an antagonist of the epidermal growth factor receptor and an in vivo active antitumor agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3909-11 (1998)
University of Utah
Selective inhibitors of human lactate dehydrogenases and lactate dehydrogenase from the malarial parasite Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3879-87 (1998)
University of New Mexico School of Medicine
Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3857-64 (1998)
Brigham Young University
Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3831-44 (1998)
Universit£
Inhibition of monoamine oxidase-B by condensed pyridazines and pyrimidines: effects of lipophilicity and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3812-20 (1998)
Université
Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3793-803 (1998)
Pharmacia & Upjohn
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3782-92 (1998)
LinköPing University
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3763-72 (1998)
Universita' Di Siena
Proton-coupled oligopeptide transport by rat renal cortical brush border membrane vesicles: a functional analysis using ACE inhibitors to determine the isoform of the transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochim Biophys Acta 1373: 277-81 (1998)
University of Oxford
Synthesis and characterization of heteroarotinoids demonstrate structure specificity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3753-7 (1998)
University of Oklahoma Health Sciences Center
Bicyclic acylguanidine Na+/H+ antiporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3736-47 (1998)
Merck
Novel orally active growth hormone secretagogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3705-14 (1998)
Novo Nordisk
2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3690-8 (1998)
National Institute On Drug Abuse
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3675-83 (1998)
Pfizer
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3664-74 (1998)
Novartis Pharma
Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3645-54 (1998)
Sanofi Winthrop
2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 3624-34 (1998)
Universita Degli Studi Di Milano
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3609-23 (1998)
Washington University
Classical/nonclassical hybrid cannabinoids: southern aliphatic chain-functionalized C-6beta methyl, ethyl, and propyl analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3596-608 (1998)
University of Hawaii
ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3582-95 (1998)
Smithkline Beecham Pharmaceuticals
Discovery of potent, achiral matrix metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3568-71 (1998)
Procter and Gamble Pharmaceuticals
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3563-7 (1998)
Smithkline Beecham Pharmaceuticals
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3557-62 (1998)
Berlex Biosciences
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3551-6 (1998)
Berlex Biosciences
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 95: 10836-41 (1998)
Merck Research Laboratories
Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 273: 23321-6 (1998)
Synaptic Pharmaceutical
Recent natural products based drug development: a pharmaceutical industry perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1053-71 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 1046-8 (1998)
The University of Tokyo
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 124: 1300-6 (1998)
Smithkline Beecham Pharmaceuticals
Pyrazole bioisosteres of leflunomide as B-cell immunosuppressants for xenotransplantation and chronic rejection: scope and limitations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3530-8 (1998)
Novartis Pharma
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3515-29 (1998)
Procter & Gamble Pharmaceuticals
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3507-14 (1998)
Hokkaido University
Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3499-506 (1998)
University of Oregon
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3493-8 (1998)
University of Bristol
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 3467-76 (1998)
Upjohn
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3461-6 (1998)
Ligand Pharmaceuticals
Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3442-9 (1998)
Novartis Pharma
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3426-34 (1998)
Duquesne University
Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3417-25 (1998)
University of Queensland
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3387-401 (1998)
Ciba-Geigy
4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3367-72 (1998)
Eisai
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3303-6 (1998)
Georgetown University Medical Center
5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 15: 1154-9 (1998)
University of Michigan
Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3298-302 (1998)
Cambridge Neuroscience
Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3293-7 (1998)
Organix
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 3276-92 (1998)
Parke-Davis Pharmaceutical Research
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3261-75 (1998)
Abbott Laboratories
1,4- and 2,6-disubstituted amidoanthracene-9,10-dione derivatives as inhibitors of human telomerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3253-60 (1998)
The Institute of Cancer Research
Synthesis and comparison of the antiinflammatory activity of manoalide and cacospongionolide B analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3232-8 (1998)
Universit£
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3220-31 (1998)
National University of Singapore
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3210-9 (1998)
Merck Research Laboratories
Salicylhydrazine-containing inhibitors of HIV-1 integrase: implication for a selective chelation in the integrase active site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3202-9 (1998)
National Cancer Institute-Bethesda
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3186-201 (1998)
National Institute of Diabetes
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3174-85 (1998)
Universit£
2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3159-73 (1998)
Novartis Institute For Medical Sciences
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3128-41 (1998)
National Taiwan University
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3103-27 (1998)
Merck Research Laboratories
Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Peptides 19: 1091-8 (1998)
Hungarian Academy of Sciences
Molecular pharmacology of homologues of ibotenic acid at cloned metabotropic glutamic acid receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 350: 311-6 (1998)
The Royal Danish School of Pharmacy
Pharmacology of [3H]prostaglandin E1/[3H]prostaglandin E2 and [3H]prostaglandin F2alpha binding to EP3 and FP prostaglandin receptor binding sites in bovine corpus luteum: characterization and correlation with functional data.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 286: 1094-102 (1998)
Alcon Laboratories
Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 286: 1007-13 (1998)
Memorial Sloan-Kettering Cancer Center
Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 286: 650-6 (1998)
Smithkline Beecham Pharmaceuticals
Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Pharmacol 54: 342-52 (1998)
Institut F£R Physiologie
Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 54: 322-33 (1998)
Georgetown University
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
NIDA Res Monogr 178: 440-66 (1998)
Sri International
Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its"hydrolytic activity": synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3078-83 (1998)
Brigham Young University
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3048-61 (1998)
Cambridge Neuroscience
Bis-substituted malonic acid hydroxamate derivatives as inhibitors of human neutrophil collagenase (MMP8).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3041-7 (1998)
Boehringer Mannheim
A new approach to the design of novel inhibitors of Na+,K+-ATPase: 17alpha-substituted seco-D 5beta-androstane as cassaine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3033-40 (1998)
Prassis Istituto Di Ricerche Sigma-Tau
Novel combretastatin analogues effective against murine solid tumors: design and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3022-32 (1998)
Ajinomoto
Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 3015-21 (1998)
Pharmaceutical Research Center
Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2972-84 (1998)
Boehringer Ingelheim Pharmaceuticals
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2960-71 (1998)
Boehringer Ingelheim Pharmaceuticals
Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2939-45 (1998)
The R. W. Johnson Pharmaceutical Research Institute
Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2934-8 (1998)
Pfizer
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2928-31 (1998)
Pfizer
Thermodynamics of binding of calcium, magnesium, and zinc to the N-methyl-D-aspartate receptor ion channel peptidic inhibitors, conantokin-G and conantokin-T.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 273: 19573-8 (1998)
University of Notre Dame
A new cacospongionolide inhibitor of human secretory phospholipase A2 from the Tyrrhenian sponge Fasciospongia cavernosa and absolute configuration of cacospongionolides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 931-5 (1998)
Istituto Per La Chimica Di Molecole Di Interesse Biologico Cnr
The inhibition of the reverse transcriptase of HIV-1 by the natural sulfoglycolipids from cyanobacteria: contribution of different moieties to their high potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 891-5 (1998)
Tel-Aviv University
Phospholipase Cgamma1 inhibitory principles from the sarcotestas of Ginkgo biloba.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 867-71 (1998)
Seoul National University
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 281: 533-538 (1998)
University of California
Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 349: 129-32 (1998)
Mcgill University
Prodrugs of nitroxyl and nitrosobenzene as cascade latentiated inhibitors of aldehyde dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2903-9 (1998)
St. Cloud State University
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2882-91 (1998)
Boehringer Ingelheim (Canada)
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2872-81 (1998)
Southern Research Institute
N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2858-71 (1998)
Glaxo Wellcome Research and Development
Styrylquinoline derivatives: a new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2846-57 (1998)
Paris-Sud University
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2835-45 (1998)
National Institute of Diabetes
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 1. Michael acceptor structure-activity studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2806-18 (1998)
Agouron Pharmaceuticals
Tripeptide aldehyde inhibitors of human rhinovirus 3C protease: design, synthesis, biological evaluation, and cocrystal structure solution of P1 glutamine isosteric replacements.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2786-805 (1998)
Agouron Pharmaceuticals
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2779-85 (1998)
Ligand Pharmaceuticals
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2765-78 (1998)
Yamanouchi Pharmaceutical
Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2745-53 (1998)
RhôNe-Poulenc Rorer
Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2732-44 (1998)
Rh£Ne-Poulenc Rorer
Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2709-19 (1998)
Eli Lilly
Design, synthesis, and biological activities of potent and selective somatostatin analogues incorporating novel peptoid residues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2679-85 (1998)
University of California San Diego
Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2676-8 (1998)
Hokkaido University
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2667-70 (1998)
Merck Sharp and Dohme Research Laboratories
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2663-6 (1998)
Cephalon
In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 286: 569-77 (1998)
Parke-Davis Pharmaceutical Research
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 286: 354-61 (1998)
University of California
Characterization of alpha1-adrenoceptor subtypes in the pig.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 347: 301-9 (1998)
Uppsala University
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 5: 299-306 (1998)
University of California San Francisco
[125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 348: 311-20 (1998)
Novartis Pharma
N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2651-6 (1998)
Merck Research Laboratories
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2643-50 (1998)
New York University Medical Center
Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2636-42 (1998)
Abbott Laboratories
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2631-5 (1998)
University of California San Diego
In vitro platelet-activating factor receptor binding inhibitory activity of pinusolide derivatives: a structure-activity study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2626-30 (1998)
Seoul National University
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2588-603 (1998)
Sugen
Carbocyclic analogues of the potent cytidine deaminase inhibitor 1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2572-8 (1998)
National Cancer Institute-Bethesda
Homonojirimycin isomers and N-alkylated homonojirimycins: structural and conformational basis of inhibition of glycosidases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2565-71 (1998)
Hokuriku University
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2537-52 (1998)
University of Wisconsin-Milwaukee
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2524-36 (1998)
Warner-Lambert
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2503-12 (1998)
Karo Bio
Design of a new class of orally active fibrinogen receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2492-502 (1998)
RhôNe-Poulenc Rorer
Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2461-80 (1998)
Hoechst Marion Roussel
Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2451-60 (1998)
Gilead Sciences
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2445-50 (1998)
The George Washington University Medical Center
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2442-4 (1998)
Wyeth-Ayerst Research
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 357: 483-9 (1998)
Novartis Pharma
Doxorubicin- and daunorubicin-glutathione conjugates, but not unconjugated drugs, competitively inhibit leukotriene C4 transport mediated by MRP/GS-X pump.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Biophys Res Commun 247: 859-63 (1998)
University of Texas M. D. Anderson Cancer Center
Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 124: 485-92 (1998)
Universit&Aagrove
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 854-6 (1998)
The University of Tokyo
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 709-12 (1998)
Universidad De Valencia
Calorimetric investigation of ethidium and netropsin binding to chicken erythrocyte chromatin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 37: 9119-26 (1998)
Universite De Liege
Synthesis and dopamine transporter affinity of the four stereoisomers of (+/-)-2-(methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2430-5 (1998)
University of New Orleans
Optimizing the binding of fullerene inhibitors of the HIV-1 protease through predicted increases in hydrophobic desolvation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2424-9 (1998)
University of California
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2411-23 (1998)
Dupont Pharmaceuticals
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2390-410 (1998)
Fujisawa Pharmaceutical
2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2380-9 (1998)
University of Oklahoma Health Sciences Center
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2371-9 (1998)
University of North Carolina At Chapel Hill
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2361-70 (1998)
Wake Forest University School of Medicine
GPIIb/IIIa integrin antagonists with the new conformational restriction unit, trisubstituted beta-amino acid derivatives, and a substituted benzamidine structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2345-60 (1998)
Nippon Steel
Auxiliary agents for the peroral administration of peptide and protein drugs: synthesis and evaluation of novel pepstatin analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2339-44 (1998)
Institute of Pharmaceutical Chemistry
Studies on selectin blockers. 6. Discovery of homologous fucose sugar unit necessary for E-selectin binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2302-7 (1998)
Kanebo
Synthesis and glutathione S-transferase structure-affinity relationships of nonpeptide and peptidase-stable glutathione analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2278-88 (1998)
Université
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2268-77 (1998)
Pfizer
Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2252-60 (1998)
University of Arizona
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2243-51 (1998)
Virginia Commonwealth University
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2201-6 (1998)
National Institute of Diabetes and Digestive and Kidney Diseases
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2194-200 (1998)
Affymax Research Institute
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2180-3 (1998)
Pharmacia & Upjohn
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2175-9 (1998)
Merck Research Laboratories
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 6: 595-604 (1998)
Sankyo
Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Am J Med 104: 413-21 (1998)
Dallas Department of Veterans Affairs Medical Center
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2146-63 (1998)
Merck Research Laboratories
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2134-45 (1998)
Purdue University
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2126-33 (1998)
Università
Selective inhibitors of monoamine oxidase (MAO). 5. 1-Substituted phenoxathiin inhibitors containing no nitrogen that inhibit MAO A by binding it to a hydrophobic site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2118-25 (1998)
The Wellcome Research Laboratories
Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2100-10 (1998)
Universit£
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 2076-89 (1998)
Purdue University
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2068-75 (1998)
3-Dimensional Pharmaceuticals
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2047-55 (1998)
National Institute of Diabetes and Digestive and Kidney Diseases
Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'-deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta, and epsilon nor HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2040-6 (1998)
Max-Delbr�Ck-Centrum F�R Molekulare Medizin
Arylpiperazines with serotonin-3 antagonist activity: a comparative molecular field analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2029-39 (1998)
Purdue University
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2019-28 (1998)
Dupont Pharmaceuticals
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 2010-8 (1998)
Institut De Chimie Pharmaceutique Albert Lespagnol
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1997-2009 (1998)
R. W. Johnson Pharmaceutical Research Institute
Melatonin receptor pharmacology: toward subtype specificity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biol Cell 89: 531-7 (1997)
King'S College London
GR196429: a nonindolic agonist at high-affinity melatonin receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 285: 1239-45 (1998)
Glaxo Wellcome Research and Development
Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Biophys Res Commun 246: 470-5 (1998)
Medical College of Georgia
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Pharmacol 55: 1035-43 (1998)
Roche Bioscience
Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 70: 2252-61 (1998)
Paris-Sud University
Energetic roles of hydrogen bonds at the ureido oxygen binding pocket in the streptavidin-biotin complex.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 37: 7657-63 (1998)
University of Washington
Calorimetric studies of E. coli SSB protein-single-stranded DNA interactions. Effects of monovalent salts on binding enthalpy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 278: 999-1014 (1998)
Washington University
The elucidation of somatostatin receptor functions: a current view.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Rev Physiol Biochem Pharmacol 133: 55-108 (1998)
German Institute of Human Nutrition
Spongiacidins A-D, new bromopyrrole alkaloids from hymeniacidon sponge ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 693-5 (1998)
Hokkaido University
Isolation of 1-carboxymethylnicotinic acid from the marine sponge anthosigmella cf. raromicrosclera As a cysteine protease inhibitor1 ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 671-2 (1998)
The University of Tokyo
Cyclotheonamides E2 and E3, new potent serine protease inhibitors from the marine sponge of the genus Theonella.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 667-70 (1998)
The University of Tokyo
Nitrogen-containing furanose and pyranose analogues from Hyacinthus orientalis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 625-8 (1998)
Hokuriku University
Petrosaspongiolides M-R: new potent and selective phospholipase A2 inhibitors from the New Caledonian marine sponge Petrosaspongia nigra.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 571-5 (1998)
Universit£
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1980-90 (1998)
Research Triangle Institute
(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1970-9 (1998)
University of Virginia
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1962-9 (1998)
Georgetown University Medical Center
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1956-61 (1998)
University of North Carolina At Chapel Hill
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 1943-55 (1998)
Eli Lilly
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1934-42 (1998)
Astra Arcus
Synthesis and structure-activity relationships of bafilomycin A1 derivatives as inhibitors of vacuolar H+-ATPase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1883-93 (1998)
Smithkline Beecham
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1846-54 (1998)
Università
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1764-76 (1998)
Abbott Laboratories
Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1752-63 (1998)
Warner-Lambert
Macrocyclic amino carboxylates as selective MMP-8 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1749-51 (1998)
Dupont Pharmaceuticals
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1745-8 (1998)
Dupont Pharmaceuticals
Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1741-4 (1998)
Novartis Pharma
Agonist-induced up-regulation of alpha4beta2 nicotinic acetylcholine receptors in M10 cells: pharmacological and spatial definition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 53: 950-62 (1998)
University of Bath
Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Psychiatry 3: 123-34 (1998)
University of Toronto
Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1729-40 (1998)
University of Leipzig
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1708-15 (1998)
Universit£
Isosteric analogues of nicotinamide adenine dinucleotide derived from furanfurin, thiophenfurin, and selenophenfurin as mammalian inosine monophosphate dehydrogenase (type I and II) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1702-7 (1998)
Universit£
Inhibition of human alcohol dehydrogenases by formamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1696-701 (1998)
The University of Iowa
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1688-95 (1998)
Arizona State University
Conformationally defined retinoic acid analogues. 4. Potential new agents for acute promyelocytic and juvenile myelomonocytic leukemias.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1679-87 (1998)
University of Alabama At Birmingham
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1641-50 (1998)
Georgetown University Medical Center
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1631-40 (1998)
Universit£
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1613-8 (1998)
University of Grenoble
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1598-612 (1998)
Smithkline Beecham Pharmaceuticals
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1581-97 (1998)
National Cancer Institute-Frederick
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1574-80 (1998)
University of Catania
5-(5,6-Dichloro-2-indolyl)-2-methoxy-2,4-pentadienamides: novel and selective inhibitors of the vacuolar H+-ATPase of osteoclasts with bone antiresorptive activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1568-73 (1998)
Smithkline Beecham
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1561-7 (1998)
Schering-Plough Research Institute
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1557-60 (1998)
University of Camerino
In vitro binding properties in rat brain of [3H]Ro 25-6981, a potent and selective antagonist of NMDA receptors containing NR2B subunits.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 70: 2147-55 (1998)
F. Hoffmann-La Roche
Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1524-30 (1998)
Upr 9023 Cnrs
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1513-23 (1998)
Novartis Pharmaceuticals
Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1476-96 (1998)
University of Tokyo
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1456-66 (1998)
National Institute of Diabetes
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 1446-55 (1998)
Dupont Pharmaceuticals
Development of a three-dimensional CysLT1 (LTD4) antagonist model with an incorporated amino acid residue from the receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1439-45 (1998)
Vrije Universiteit
Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1428-38 (1998)
Vrije Universiteit
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1409-16 (1998)
Duquesne University
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1382-91 (1998)
University of Pennsylvania
Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1367-70 (1998)
University of Manchester
2-Iminohomopiperidinium salts as selective inhibitors of inducible nitric oxide synthase (iNOS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1361-6 (1998)
Pfizer
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1357-60 (1998)
Pharmacia & Upjohn
Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 343: 67-77 (1998)
Hospital Saint-Antoine
Isolation of 1-Methylherbipoline Salts of Halisulfate-1 and of Suvanine as Serine Protease Inhibitors from a Marine Sponge, Coscinoderma mathewsi![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 248-50 (1998)
Aoyama Gakuin University
Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo[2,3-d]pyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1263-71 (1998)
Duquesne University
Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1252-62 (1998)
University of Michigan
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1218-35 (1998)
Smithkline Beecham Pharmaceuticals
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1209-17 (1998)
Kanebo
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1205-8 (1998)
Merck
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 5: 185-96 (1998)
Merck Research Laboratories
DNA polymerase and topoisomerase II inhibitors from Psoralea corylifolia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 362-6 (1998)
Ohio State University
5-Lipoxygenase and cyclooxygenase-1 inhibitory active compounds from Atractylodes lancea.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 347-50 (1998)
Heinrich-Heine-UniversitäT DüSseldorf
Pharmacophoric requirements for cannabinoid side chains: multiple bond and C1'-substituted delta 8-tetrahydrocannabinols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1195-200 (1998)
National Hellenic Research Foundation
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1172-84 (1998)
Pfizer
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1155-62 (1998)
University of North Carolina At Chapel Hill
Potent antagonists of somatostatin: synthesis and biology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1146-54 (1998)
Tulane University School of Medicine
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1138-45 (1998)
University of Louvain
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1124-37 (1998)
Procter & Gamble Pharmaceuticals
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1112-23 (1998)
Procter & Gamble Pharmaceuticals
Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D- mannopyranosyloxy)phenyl]hexane (TBC1269).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1099-111 (1998)
Texas Biotechnology
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1060-7 (1998)
Warner-Lambert
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1042-9 (1998)
Parke-Davis Pharmaceutical Research
Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1011-3 (1998)
Merck Research Laboratories
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 340: 249-58 (1997)
Mayo Clinic
Differential agonist inhibition identifies multiple epibatidine binding sites in mouse brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 285: 377-86 (1998)
University of Colorado
Pharmacological characterization of the human ionotropic glutamate receptor subtype GluR3 stably expressed in mammalian cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 285: 358-70 (1998)
Sibia Neurosciences
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 285: 170-7 (1998)
University of Bonn
Synthesis and pharmacological evaluation of ring-methylated derivatives of 3,4-(methylenedioxy)amphetamine (MDA).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 1001-5 (1998)
Purdue University
Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 996-1000 (1998)
G.D. Searle And
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 913-8 (1998)
Harvard Medical School
Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 902-12 (1998)
University of Maryland
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 877-93 (1998)
Schering-Plough Research Institute
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 864-76 (1998)
University of Maryland
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 836-52 (1998)
Universidad De Alcal£
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 821-35 (1998)
Smithkline Beecham Pharmaceuticals
(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 808-20 (1998)
Università
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 798-807 (1998)
Glaxo Wellcome Research and Development
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 787-97 (1998)
Glaxo Wellcome Research and Development
Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 775-7 (1998)
Searle
A novel kainate receptor ligand [3H]-(2S,4R)-4-methylglutamate: pharmacological characterization in rabbit brain membranes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 1483-8 (1997)
University of Bristol
Discovery of nonsteroidal androgens.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Biophys Res Commun 244: 1-4 (1998)
University of Tennessee At Memphis
Glyphosate is an inhibitor of plant cytochrome P450: functional expression of Thlaspi arvensae cytochrome P45071B1/reductase fusion protein in Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Biophys Res Commun 244: 110-4 (1998)
University of Wales Aberystwyth
Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 301-5 (1998)
Institut FüR Biowissenschaften
Aminopyrimidines with high affinity for both serotonin and dopamine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 760-71 (1998)
Warner-Lambert
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 742-51 (1998)
University of Auckland
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 728-41 (1998)
Universit£
Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-[2-(diphenylmethoxy)ethyl]-1-(3-phenylpropyl)piperidine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 699-705 (1998)
Organix
alpha-Substituted malonester amides: tools to define the relationship between ACAT inhibition and adrenal toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 682-90 (1998)
Warner-Lambert
Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 674-81 (1998)
Universit£
Novel 3-aralkyl-7-(amino-substituted)-1,2,3-triazolo[4,5-d]pyrimidines with high affinity toward A1 adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 668-73 (1998)
Università
(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 41: 655-7 (1998)
Smithkline Beecham Pharmaceuticals
Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 284: 1033-9 (1998)
University of Tokyo
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 640-9 (1998)
Shionogi
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 623-39 (1998)
Ligand Pharmaceuticals
Synthesis of a methylenebis(phosphonate) analogue of mycophenolic adenine dinucleotide: a glucuronidation-resistant MAD analogue of NAD.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 618-22 (1998)
Codon Pharmaceuticals
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 602-17 (1998)
Abbott Laboratories
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 1. Construction of the basic framework.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 564-78 (1998)
Fujisawa Pharmaceutical
A1 adenosine receptor antagonists as ligands for positron emission tomography (PET) and single-photon emission tomography (SPET).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 555-63 (1998)
Forschungszentrum JüLich
29-Methylidene-2,3-oxidosqualene derivatives as stereospecific mechanism-based inhibitors of liver and yeast oxidosqualene cyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 540-54 (1998)
Università
Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitro or nitroso)pyrimidine derivatives and analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 503-8 (1998)
Nagoya City University
Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 489-502 (1998)
Takeda Chemical Industries
Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 468-77 (1998)
University of Illinois At Chicago
Mapping the melatonin receptor. 5. Melatonin agonists and antagonists derived from tetrahydrocyclopent[b]indoles, tetrahydrocarbazoles and hexahydrocyclohept[b]indoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 451-67 (1998)
University College London
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 437-50 (1998)
Collegeville
Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 428-36 (1998)
University of Pennsylvania
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 420-7 (1998)
Oxis International
2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 413-9 (1998)
Signal Pharmaceuticals
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 407-12 (1998)
Abbott Laboratories
Ethylene biosynthesis: processing of a substrate analog supports a radical mechanism for the ethylene-forming enzyme.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 5: 49-57 (1998)
Duke University
Engineering novel specificities for ligand-activated transcription in the nuclear hormone receptor RXR.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 5: 13-21 (1998)
University of Texas Southwestern Medical Center
Design of potent selective zinc-mediated serine protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nature 391: 608-12 (1998)
Arris
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 401-6 (1998)
Merck Research Laboratories
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 379-92 (1998)
Eli Lilly
2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 358-78 (1998)
Eli Lilly
2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 346-57 (1998)
Eli Lilly
Design and synthesis of malonic acid-based inhibitors of human neutrophil collagenase (MMP8).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 339-45 (1998)
Institut FüR Biochemie
5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 311-7 (1998)
Universit£
5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 303-10 (1998)
Ligand Pharmaceuticals
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 291-302 (1998)
Ligand Pharmaceuticals
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 271-5 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 266-70 (1998)
Pfizer
Novel potent nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 263-5 (1998)
University of Tokyo
In vitro binding characteristics of a new selective group II metabotropic glutamate receptor radioligand, [3H]LY354740, in rat brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 53: 228-33 (1998)
F. Hoffmann-La Roche
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 53: 195-201 (1998)
Suntory Institute For Bioorganic Research
A new flavonol glycoside gallate ester from Acer okamotoanum and its inhibitory activity against human immunodeficiency virus-1 (HIV-1) integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 145-8 (1998)
Korea Institute of Science & Technology
Lignans interfering with 5 alpha-dihydrotestosterone binding to human sex hormone-binding globulin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 119-21 (1998)
Universit£T Bayreuth
Friedelane triterpenoids from Maytenus macrocarpa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 82-5 (1998)
Universidad De Laguna
Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 71-6 (1998)
University of Antwerp
Litebamine N-homologues: preparation and anti-acetylcholinesterase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 46-50 (1998)
National Taiwan University
Two new isoflavones from Ceiba pentandra and their effect on cyclooxygenase-catalyzed prostaglandin biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 8-12 (1998)
Uppsala University
Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 61: 2-7 (1998)
Uppsala University
Evidence for the absolute conformational specificity of the intestinal H+/peptide symporter, PEPT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 273: 3861-4 (1998)
Martin-Luther-University Halle-Wittenberg
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 357: 17-24 (1998)
Eli Lilly
Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 357: 1-9 (1998)
UniversitÄT WÜRzburg
Adenosine receptor agonists: synthesis and biological evaluation of the diastereoisomers of 2-(3-hydroxy-3-phenyl-1-propyn-1-yl)NECA.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 5: 2267-75 (1997)
UniversitÀ
Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Am J Physiol 274: 157-69 (1998)
Wake Forest University
Synthesis and ligand binding of tropane ring analogues of paroxetine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 247-57 (1998)
Research Triangle Institute
Matrix metalloproteinase inhibitors: a structure-activity study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 199-223 (1998)
Glycomed
Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 183-90 (1998)
National Institute of Diabetes
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 157-66 (1998)
University of Pennsylvania
Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 148-56 (1998)
University of Manchester
A new class of highly potent farnesyl diphosphate-competitive inhibitors of farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 143-7 (1998)
Tsukuba Research Institute
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 284: 777-89 (1998)
Sibia Neurosciences
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 284: 644-50 (1998)
Sanofi Recherche
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 284: 500-7 (1998)
University of Arizona
Characterization of central- and peripheral-type benzodiazepine receptors in rat salivary glands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Pharmacol 55: 209-14 (1998)
Tokyo Dental College
From micromolar to nanomolar affinity: a systematic approach to identify the binding site of CGRP at the human calcitonin gene-related peptide 1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 117-23 (1998)
Eth ZüRich
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 109-16 (1998)
Novo Nordisk
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 102-8 (1998)
Leiden/Amsterdam Center For Drug Research
Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 96-101 (1998)
G. D. Searle Research and Development
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 74-95 (1998)
Abbott Laboratories
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 53-62 (1998)
Dupont Pharmaceuticals
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 46-52 (1998)
National Institute of Diabetes
Second generation"peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 38-45 (1998)
Warner-Lambert
(Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 41: 10-23 (1998)
Wayne State University School of Medicine
2-(1-Naphthyloxy)ethylamines with enhanced affinity for human 5-HT1D beta (h5-HT1B) serotonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4415-9 (1998)
Medical College of Virginia/Virginia Commonwealth University
Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4406-14 (1998)
University of New Orleans
Synthesis and structure-activity relationships of 3,7-dimethyl-1-propargylxanthine derivatives, A2A-selective adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4396-405 (1998)
Julius-Maximilians-UniversitäT WüRzburg
Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4378-85 (1998)
F. Hoffmann-La Roche
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4372-7 (1998)
Schering-Plough Research Institute
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4360-71 (1998)
Harvard University
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4340-46 (1998)
National Institute On Drug Abuse-Intramural Research Program
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4329-39 (1998)
National Institute On Drug Abuse
Fibrinogen receptor (GPIIb-IIIa) antagonists derived from 5,6-bicyclic templates. Amidinoindoles, amidinoindazoles, and amidinobenzofurans containing the N-alpha-sulfonamide carboxylic acid function as potent platelet aggregation inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4308-18 (1998)
Cor Therapeutics
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4302-7 (1998)
Rochester
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4290-301 (1998)
Schering-Plough Research Institute
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4281-9 (1998)
Cambridge Neuroscience
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4265-80 (1998)
Smithkline Beecham Pharmaceuticals
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4257-64 (1998)
Université
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4235-56 (1998)
Wyeth-Ayerst Research Laboratories
Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4222-34 (1998)
University of Tokyo
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4199-207 (1998)
National Cancer Institute-Frederick
Development of a high-affinity ligand that binds irreversibly to Mel1b melatonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4195-8 (1998)
Duquesne University
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4169-94 (1998)
Abbott Laboratories
Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropsychopharmacology 18: 63-101 (1998)
H. Lundbeck
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Science 279: 77-81 (1998)
Abbott Laboratories
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4146-53 (1998)
University of Groningen
Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4136-45 (1998)
Universidad De Alcalá
Peptidomimetic inhibitors of the human cytomegalovirus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4113-35 (1998)
Boehringer Ingelheim
Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4103-12 (1998)
Schering-Plough Research Institute
A strategy for the incorporation of water molecules present in a ligand binding site into a three-dimensional quantitative structure--activity relationship analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4089-102 (1998)
University of Alcala
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4079-88 (1998)
Dupont Pharmaceuticals
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 4030-52 (1997)
Biocryst Pharmaceuticals
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4026-9 (1998)
Warner-Lambert
1-[1-2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) yields two active primary metabolites in vitro: synthesis, identification from rat liver microsome extracts, and affinity for the neuronal dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4019-25 (1998)
University of Montpellier
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3997-4005 (1998)
University of Kansas
Cloning and expressional characterization of a novel galanin receptor. Identification of different pharmacophores within galanin for the three galanin receptor subtypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 272: 31949-52 (1997)
Schering-Plough Research Institute
Energetics of heme binding to native and denatured states of cytochrome b562.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 36: 16141-6 (1997)
University of Illinois
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 283: 1305-22 (1997)
Emory University
Interactions of nonsteroidal anti-inflammatory drugs with rat renal organic anion transporter, OAT-K1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 283: 1039-42 (1998)
Kyoto University Hospital
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3979-85 (1998)
Agouron Pharmaceuticals
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3974-8 (1998)
Centre De Recherche Pierre Fabre
Enzymatic properties of the unnatural beta-L-enantiomers of 2',3'-dideoxyadenosine and 2',3'-didehydro-2',3'-dideoxyadenosine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3969-73 (1998)
University of Montpellier
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3957-62 (1998)
University of Arizona
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3947-56 (1998)
University of Paris
Tyrosine kinase inhibitors. 13. Structure-activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 3915-25 (1997)
University of Auckland
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3905-14 (1998)
University of Minnesota
Potent and selective inhibition of neuronal nitric oxide synthase by N omega-propyl-L-arginine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3869-70 (1998)
Northwestern University
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3865-8 (1998)
Merck Research Laboratories
3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3861-4 (1998)
Research Triangle Institute
Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 52: 1150-6 (1997)
Merck Sharp and Dohme Research Laboratories
Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Life Sci 61: 2117-26 (1997)
Eli Lilly
Zanhasaponins A and B, antiphospholipase A2 saponins from an antiinflammatory extract of Zanha africana root bark.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 1158-60 (1998)
Universitat De Val£Ncia
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 2: 601-8 (1995)
University of California San Diego
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 2: 471-81 (1995)
Smithkline Beecham Pharmaceuticals
Importance of the C-1 substituent in classical cannabinoids to CB2 receptor selectivity: synthesis and characterization of a series of O,2-propano-delta 8-tetrahydrocannabinol analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3312-8 (1997)
Kennesaw State University
17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3297-304 (1997)
University of Maryland
DNA gyrase inhibitory and antimicrobial activities of some diphenic acid monohydroxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3292-6 (1997)
R.W. Johnson Pharmaceutical Research Institute
Angiotensin analogues palmitoylated in positions 1 and 4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3271-9 (1997)
Universit£
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3263-70 (1997)
University of Minnesota
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3248-53 (1997)
Hokuriku University
Sulfated galactocerebrosides as potential antiinflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3234-47 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3228-33 (1997)
Institute of Science
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3217-27 (1997)
Abbott Laboratories
A model for binding of structurally diverse natural product inhibitors of protein phosphatases PP1 and PP2A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3199-206 (1997)
University of California
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3192-8 (1997)
Smithkline Beecham
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3173-81 (1997)
Zeneca Pharmaceuticals
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3161-72 (1997)
University of Michigan
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3144-50 (1997)
Abbott Laboratories
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3141-3 (1997)
Abbott Laboratories
Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Am J Physiol 273: 706-11 (1997)
Kyoto University Hospital
Design, synthesis, and biochemical evaluation of phosphonate and phosphonamidate analogs of glutathionylspermidine as inhibitors of glutathionylspermidine synthetase/amidase from Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3842-50 (1997)
University of Michigan
Synthesis and structure-activity profiles of A-homoestranes, the estratropones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3836-41 (1997)
University of Virginia
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3804-19 (1997)
Uppsala University
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 3781-92 (1997)
Parke-Davis Pharmaceutical Research
Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3773-80 (1997)
WestfäLische Wilhelms-UniversitäT MüNster
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3765-72 (1997)
University of Ghent
Synthesis and biological evaluation of 4-(hydroxyalkyl)estradiols and related compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3756-64 (1997)
Ohio State University
Betidamino acid scan of the GnRH antagonist acyline.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3739-48 (1997)
Salk Institute
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3726-33 (1997)
Merck Research Laboratories
Design, synthesis, and cocrystal structure of a nonpeptide Src SH2 domain ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3719-25 (1997)
Warner-Lambert
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3712-4 (1997)
Eli Lilly
Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 3707-11 (1997)
Parke-Davis Pharmaceutical Research
(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3700-5 (1997)
Royal Danish School of Pharmacy
2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3694-9 (1997)
Harvard Medical School
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3687-93 (1997)
Merck Research Laboratories
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3679-86 (1997)
Cocensys
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3670-8 (1997)
Universit£
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3645-50 (1997)
University of Bristol
Synthesis and pharmacological comparison of dimethylheptyl and pentyl analogs of anandamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3626-34 (1997)
Research Triangle Institute
Potent anandamide analogs: the effect of changing the length and branching of the end pentyl chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3617-25 (1997)
Organix
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 3601-16 (1997)
Novartis Pharmaceuticals
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3594-600 (1997)
University of Minnesota
Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3551-6 (1997)
Novartis Pharma
Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3542-50 (1997)
Centre De Recherche Pierre Fabre
Studies on selection blockers. 5. Design, synthesis, and biological profile of sialyl Lewis x mimetics based on modified serine-glutamic acid dipeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3534-41 (1997)
Kanebo
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3524-33 (1997)
Universit£T Regensburg
Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3516-23 (1997)
University of Strathclyde
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3504-7 (1997)
Shionogi
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3501-3 (1997)
Merck Sharp and Dohme Research Laboratories
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3497-500 (1997)
Merck Sharp and Dohme Research Laboratories
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3494-6 (1997)
Smithkline Beecham Pharmaceuticals
ATP-dependent transport of bilirubin glucuronides by the multidrug resistance protein MRP1 and its hepatocyte canalicular isoform MRP2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem J 327: 305-10 (1997)
Deutsches Krebsforschungszentrum
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 283: 735-41 (1997)
Torrey Pines Institute For Molecular Studies
[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 283: 488-93 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuroreport 8: 3189-96 (1997)
Cnrs Upr 9023
Cloning and expression of a human serotonin 5-HT4 receptor cDNA.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 69: 1810-9 (1997)
Janssen Research Foundation
Synthesis, cardiotonic activity, and structure-activity relationships of 17 beta-guanylhydrazone derivatives of 5 beta-androstane-3 beta, 14 beta-diol acting on the Na+,K(+)-ATPase receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3484-8 (1997)
Prassis Istituto Di Ricerche Sigma-Tau
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3456-65 (1997)
Université
Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3442-52 (1997)
Pfizer
7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3423-33 (1997)
Southern Methodist University
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3408-22 (1997)
RhôNe-Poulenc Rorer
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3402-7 (1997)
Instituto De QuíMica MéDica (Csic)
New orally active non-peptide fibrinogen receptor (GpIIb-IIIa) antagonists: identification of ethyl 3-[N-[4-[4-[amino[(ethoxycarbonyl) imino]methyl]phenyl]-1,3-thiazol-2-yl]-N-[1-[(ethoxycarbonyl)methyl]pip erid -4-yl]amino]propionate (SR 121787) as a potent and long-acting antithrombotic agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3393-401 (1997)
Sanofi Recherche
Structure-activity relationships of (4-acylpyrrol-2-yl)alkanoic acids as inhibitors of the cytosolic phospholipase A2: variation of the substituents in positions 1, 3, and 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3381-92 (1997)
Ludwig-Maximilians University
Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3369-80 (1997)
Pharmacia & Upjohn
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3359-68 (1997)
Genentech
Effect of a chemical modification on the hydrated adenosine intermediate produced by adenosine deaminase and a model reaction for a potential mechanism of action of 5-aminoimidazole ribonucleotide carboxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3336-45 (1997)
Southern Illinois University
C-terminal modifications of histidyl-N-benzylglycinamides to give improved inhibition of Ras farnesyltransferase, cellular activity, and anticancer activity in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3319-22 (1997)
Warner-Lambert
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 283: 216-25 (1997)
Preclinical R & D, Astra Arcus
Four new clerodane diterpenes from the leaves of Casearia guianensis which inhibit the interaction of leukocyte function antigen 1 with intercellular adhesion molecule 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 894-9 (1997)
Searle Research and Development
In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 884-8 (1997)
Medichem Research
Biliary excretion of pravastatin in rats: contribution of the excretion pathway mediated by canalicular multispecific organic anion transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Drug Metab Dispos 25: 1123-9 (1997)
Toho University School of Pharmaceutical Sciences
Interaction of cyclosporin derivatives with the ATPase activity of human P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Br J Pharmacol 122: 241-8 (1997)
Novartis Takarazuka Research Institute
Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 122: 217-24 (1997)
Kyoto University
Expression cloning of a rat hypothalamic galanin receptor coupled to phosphoinositide turnover.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 272: 24612-6 (1997)
Synaptic Pharmaceutical
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 356: 328-34 (1997)
RhôNe-Poulenc Rorer
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 356: 312-20 (1997)
Smithkline Beecham Pharmaceuticals
Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
FEBS Lett 413: 489-94 (1997)
Organon
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3119-29 (1997)
Université
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3109-18 (1997)
Universit£
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3100-8 (1997)
University of Ferrara
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3091-9 (1997)
Klinikum Der Friedrich-Schiller-Universit£T Jena
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3085-90 (1997)
Chinese Academy of Sciences
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3064-70 (1997)
University of Minnesota
Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3057-63 (1997)
National Cancer Institute-Bethesda
Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3049-56 (1997)
University of North Carolina
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3040-8 (1997)
University
Conformationally restricted analogues of trimethoprim: 2,6-diamino-8-substituted purines as potential dihydrofolate reductase inhibitors from Pneumocystis carinii and Toxoplasma gondii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3032-9 (1997)
Duquesne University
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3014-24 (1997)
University of Tennessee
Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 3009-13 (1997)
University of North Texas
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2997-3008 (1997)
Purdue University
Fused pyrrolo[2,3-c]carbazol-6-ones: novel immunostimulants that enhance human interferon-gamma activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2994-6 (1997)
Cephalon
Ras farnesyltransferase: a new therapeutic target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2971-90 (1997)
Warner-Lambert
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Br J Pharmacol 122: 126-32 (1997)
Roche Bioscience
The somatostatin analog octreotide as potential treatment for re-stenosis and chronic rejection.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Transplant Proc 29: 2599-600 (1997)
Novartis Pharma Research
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2948-52 (1997)
University of Ferrara
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2936-47 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2922-30 (1997)
Boehringer Ingelheim Pharmaceuticals
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2910-21 (1997)
Universit£
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2895-901 (1997)
National Institute On Aging
Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2866-75 (1997)
Merck Frosst Centre For Therapeutic Research
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2843-57 (1997)
Eli Lilly
Selective inhibition of neuronal nitric oxide synthase by N omega-nitroarginine-and phenylalanine-containing dipeptides and dipeptide esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2813-7 (1997)
Northwestern University
Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 842-3 (1997)
National Taiwan University
Molecular cloning and pharmacological characterization of a new galanin receptor subtype.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 52: 337-43 (1997)
The Schering Plough Research Institute
Antipsoriatic anthrones with modulated redox properties. 4. Synthesis and biological activity of novel 9,10-dihydro-1,8-dihydroxy-9-oxo-2-anthracenecarboxylic and -hydroxamic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2780-7 (1997)
WestfäLische Wilhelms-UniversitäT MüNster
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2762-9 (1997)
F. Hoffmann-La Roche
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2740-9 (1997)
University of Arizona
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2733-9 (1997)
Oregon State University
Synthesis and antimalarial effects of phenothiazine inhibitors of a Plasmodium falciparum cysteine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2726-32 (1997)
Universidad Central De Venezuela
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 2706-25 (1997)
Glaxo Wellcome Research and Development
Synthesis, biological evaluation, and structure-activity relationships of 3-acylindole-2-carboxylic acids as inhibitors of the cytosolic phospholipase A2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2694-705 (1997)
Ludwig-Maximilians University
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2688-93 (1997)
Warner-Lambert
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2674-87 (1997)
Roche Bioscience
2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2661-73 (1997)
Organix
Methotrexate is excreted into the bile by canalicular multispecific organic anion transporter in rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cancer Res 57: 3506-10 (1997)
Toho University School of Pharmaceutical Sciences
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 282: 1011-9 (1997)
Neurogen
Kinetic analysis of the primary active transport of conjugated metabolites across the bile canalicular membrane: comparative study of S-(2,4-dinitrophenyl)-glutathione and 6-hydroxy-5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)benzothiazole glucuronide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 282: 866-72 (1997)
University of Tokyo
Cloning and characterization of two human polyspecific organic cation transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
DNA Cell Biol 16: 871-81 (1997)
Anatomisches Institut Der Bayerischen Julius-Maximilians-Universit£T
Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2653-6 (1997)
Universidad Complutense
Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2609-25 (1997)
G.D. Searle
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2596-608 (1997)
National Institute of Diabetes
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2588-95 (1997)
Niddk
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2579-87 (1997)
National Institute of Environmental Health Sciences
The chemistry of pseudomonic acid. 18. Heterocyclic replacement of the alpha,beta-unsaturated ester: synthesis, molecular modeling, and antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2563-70 (1997)
Smithkline Beecham Pharmaceuticals
The role of phenylalanine at position 6 in glucagon's mechanism of biological action: multiple replacement analogues of glucagon.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2555-62 (1997)
University of Arizona
Synthesis of nonhydrolyzable analogues of thiazole-4-carboxamide and benzamide adenine dinucleotide containing fluorine atom at the C2' of adenine nucleoside: induction of K562 differentiation and inosine monophosphate dehydrogenase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2533-8 (1997)
Codon Pharmaceuticals
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 2525-32 (1997)
Novartis Pharmaceuticals
Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2502-24 (1997)
Agouron Pharmaceuticals
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2491-501 (1997)
Merck Sharp & Dohme Research Laboratories
Synthesis and ligand binding studies of 4'-iodobenzoyl esters of tropanes and piperidines at the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2474-81 (1997)
University of Oklahoma
Selective inhibitors of monoamine oxidase. 4. SAR of tricyclic N-methylcarboxamides and congeners binding at the tricyclics' hydrophilic binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2466-73 (1997)
Wellcome Research Laboratories
Identification of highly potent retinoic acid receptor alpha-selective antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2445-51 (1997)
Allergan
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2440-4 (1997)
University of Pennsylvania
Thermodynamic and structural analysis of phosphotyrosine polypeptide binding to Grb2-SH2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 36: 10006-14 (1997)
Schering-Plough Research Institute
Novel selective thiol inhibitors of neutral endopeptidase containing heterocycles at P'2 position.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzym Inhib 12: 155-60 (1997)
R & D, Zambon Group
Yeast hexokinase inhibitors designed from the 3-D enzyme structure rebuilding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzym Inhib 12: 101-21 (1997)
Universite Paul Sabatier
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl-dipyridodiazepinones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 2430-3 (1997)
Boehringer Ingelheim Pharmaceuticals
Synthesis of racemic 6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones as antagonists of N-methyl-d-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2424-9 (1997)
Cocensys
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2374-85 (1997)
Merck Sharp and Dohme Research Laboratories
Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2363-73 (1997)
Life Science Research Center
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2347-62 (1997)
Monash University
Synthesis of analogs of 2-methoxyestradiol with enhanced inhibitory effects on tubulin polymerization and cancer cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2323-34 (1997)
Purdue University
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2296-303 (1997)
Parke-Davis Pharmaceutical Research
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2289-92 (1997)
Smithkline Beecham Pharmaceuticals
Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABA(C) receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 329: 223-9 (1997)
University of Sydney
Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 713-20 (1997)
F. Hoffmann-La Roche
[3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 671-9 (1997)
Roche Bioscience
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 621-9 (1997)
Roche Bioscience
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 609-20 (1997)
Smithkline Beecham Pharmaceuticals
Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 4: 461-71 (1997)
Massachusetts Institute of Technology
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 4: 423-31 (1997)
Vertex Pharmaceuticals
N-(3-lodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(3',4'-dichloro phenyl)nortropane (beta-CDIT), a tropane derivative: pharmacological characterization as a specific ligand for the dopamine transporter in the rodent brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 282: 467-74 (1997)
University of Tours
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 282: 445-51 (1997)
Georgetown University
Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 282: 301-8 (1997)
Yamanouchi Pharmaceutical
[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 282: 181-91 (1997)
Institut De Recherches Servier
Antitumor agents. 174. 2',3',4',5,6,7-Substituted 2-phenyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2266-75 (1997)
University of North Carolina At Chapel Hill
A refined model for the somatostatin pharmacophore: conformational analysis of lanthionine-sandostatin analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2252-8 (1997)
University of California San Diego
Lanthionine-somatostatin analogs: synthesis, characterization, biological activity, and enzymatic stability studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2241-51 (1997)
University of California San Diego
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2228-40 (1997)
Warner-Lambert
Steroidal affinity labels of the estrogen receptor. 3. Estradiol 11 beta-n-alkyl derivatives bearing a terminal electrophilic group: antiestrogenic and cytotoxic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2217-27 (1997)
Inserm Unit�
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2196-210 (1997)
Schering-Plough Research Institute
Phosphodiester amidates of unsaturated nucleoside analogues: synthesis and anti-HIV activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2191-5 (1997)
Wayne State University School of Medicine
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 2164-76 (1997)
Boehringer Ingelheim (Canada)
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2156-63 (1997)
Suntory
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2133-9 (1997)
University of Michigan Medical Center
(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2123-5 (1997)
Abbott Laboratories
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2117-22 (1997)
Le Centre Hospitalier Universitaire De Qu£Bec
Inhibition of human telomerase by a G-quadruplex-interactive compound.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2113-6 (1997)
Institute For Drug Development
Activity of Parthenolide at 5HT2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 651-3 (1997)
University of Montana
Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 638-41 (1997)
University of Antwerp
Effects of flavonoids isolated from scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 598-601 (1997)
Ehime University
Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2085-101 (1997)
Eli Lilly
Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2064-84 (1997)
Dupont Pharmaceuticals
Synthesis and in vitro evaluation of two progressive series of bifunctional polyhydroxybenzamide catechol-O-methyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2035-9 (1997)
University of Otago
(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2017-34 (1997)
Merck
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 2003-10 (1997)
Universit£
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1990-2002 (1997)
Universit£
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1982-9 (1997)
Virginia Polytechnic Institute and State University
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1977-81 (1997)
University of Minnesota
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1955-68 (1997)
Abbott Laboratories
Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 beta-converting enzyme inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1941-6 (1997)
Sanofi Winthrop
Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 51: 350-6 (1997)
Schering-Plough Research Institute
Molecular recognition at the thrombin active site: structure-based design and synthesis of potent and selective thrombin inhibitors and the X-ray crystal structures of two thrombin-inhibitor complexes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 4: 287-95 (1997)
Laboratorium FÜR Organische Chemie
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 4: 297-307 (1997)
University of California Berkeley
Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1930-6 (1997)
Duquesne University
Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1906-18 (1997)
Institut De Recherche Servier
Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1901-5 (1997)
Glaxo Wellcome Research and Development
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1886-93 (1997)
University of Nottingham
Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1876-85 (1997)
Zeneca Pharmaceuticals
Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1863-9 (1997)
Kyowa Hakko Kogyo
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1835-44 (1997)
Organix
Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1820-6 (1997)
University of Auckland
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1808-19 (1997)
Universit£
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1794-807 (1997)
Smithkline Beecham S.P.A. Milano
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1779-88 (1997)
Merck Research Laboratories
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1773-8 (1997)
Cv Therapeutics
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1771-2 (1997)
Warner-Lambert
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1768-70 (1997)
Upr 421 Du Cnrs
Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1763-7 (1997)
Centre De Recherches De Vitry-Alfortville
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 281: 1303-11 (1997)
Smithkline Beecham Pharmaceuticals
Anthracyclines modulate multidrug resistance protein (MRP) mediated organic anion transport.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochim Biophys Acta 1326: 12-22 (1997)
Academic Hospital Vrije Universiteit
Cloning and functional expression of a human liver organic cation transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Pharmacol 51: 913-21 (1997)
University of California San Francisco
Rabbit cerebral cortex 5HT1a receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Comp Biochem Physiol C, Pharmacol Toxicol Endocrinol 117: 19-24 (1997)
University of Montana
Perhydrogenation of tabersonine, ans Aspidiosperma indole alkaloid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 419-20 (1997)
UniversitÉ
A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nature 387: 620-4 (1997)
The University of Tokyo
Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1755-61 (1997)
Cnrs-Biocis
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1749-54 (1997)
Pfizer
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1738-48 (1997)
University of Michigan Medical Center
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1726-30 (1997)
University of Kansas
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1720-5 (1997)
University of Minnesota
Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1707-9 (1997)
Dupont Pharmaceuticals
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1690-7 (1997)
Immunopharmaceutics
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1682-9 (1997)
Immunopharmaceutics
Halogenated 4-(phenoxymethyl)piperidines as potential radiolabeled probes for sigma-1 receptors: in vivo evaluation of [123I]-1-(iodopropen-2-yl)-4-[(4-cyanophenoxy)methyl]pip eri dine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1657-67 (1997)
Ansto
Synthesis and structure-activity relationships of a new model of arylpiperazines. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1648-56 (1997)
Universidad Complutense
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1634-47 (1997)
Searle Research and Development
1,2-Diarylpyrroles as potent and selective inhibitors of cyclooxygenase-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1619-33 (1997)
Searle Research and Development
Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1608-18 (1997)
Brigham Young University
Synthesis and pharmacological properties of a close analogue of an antithrombotic pentasaccharide (SR 90107A/ORG 31540).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1600-7 (1997)
Sanofi Recherche
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1585-99 (1997)
Abbott Laboratories
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1565-9 (1997)
Merck Research Laboratories
Identification of the novel antimicrobial fatty acid (5Z,9Z)-14-methyl-5,9-pentadecadienoic acid in Eunicea succinea.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 502-4 (1997)
University of Puerto Rico
Differential expression of multiple somatostatin receptors in the rat cerebellum during development.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 68: 2263-72 (1997)
Dynamique Des Systemes Neuroendocriniens
The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 325: 145-53 (1997)
Cns-Pharmacology
Fagomine isomers and glycosides from Xanthocercis zambesiaca.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 312-4 (1997)
Hokuriku University
Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1550-8 (1997)
Institut De Chimie Des Substances Naturelles Cnrs
Binding affinities for sulfonamide inhibitors with human thrombin using Monte Carlo simulations with a linear response method.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1539-49 (1997)
Yale University
Tyrosine kinase inhibitors. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1519-29 (1997)
University of Auckland
Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1495-510 (1997)
The Institute of Cancer Research
Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: synthesis, structure-activity relationship, and X-ray crystal structure analysis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1465-74 (1997)
Dupont Pharmaceuticals
Smart region definition: a new way to improve the predictive ability and interpretability of three-dimensional quantitative structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1455-64 (1997)
University of Perugia
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1447-54 (1997)
Sapienza University of Rome
Synthesis and structure-activity relationships of 17beta-substituted 14beta-hydroxysteroid 3-(alpha-L-rhamnopyranoside)s: steroids that bind to the digitalis receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1439-46 (1997)
University of Manitoba
Conformationally constrained [p-(omega-aminoalkyl)phenacetyl]-L-seryl-L-lysyl dipeptide amides as potent peptidomimetic inhibitors of Candida albicans and human myristoyl-CoA:protein N-myristoyl transferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1422-38 (1997)
G. D. Searle Research and Development
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1417-21 (1997)
Dipartimento Di Scienze Farmaceutiche, Firenze, Italy.
Novel cyclic peptide agonist of high potency and selectivity for the type II vasoactive intestinal peptide receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 281: 629-33 (1997)
University of California San Francisco
The 5-HT7 receptor: orphan found.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Trends Pharmacol Sci 18: 104-7 (1997)
Roche Bioscience
BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 36: 233-9 (1997)
Smithkline Beecham Pharmaceuticals
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Science 276: 955-60 (1997)
New York University Medical Center
Synthesis and ligand binding of nortropane derivatives: N-substituted 2beta-carbomethoxy-3beta-(4'-iodophenyl)nortropane and N-(3-iodoprop-(2E)-enyl)-2beta-carbomethoxy-3beta-(3',4'-disubstituted phenyl)nortropane. New high-affinity and selective compounds for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1366-72 (1997)
University of Tours
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1347-65 (1997)
Searle Research and Development
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1316-26 (1997)
Georgetown University Medical Center
Pharmacological options in the treatment of benign prostatic hyperplasia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1293-315 (1997)
Pfizer
Isolation and structure determination of sulfonoquinovosyl dipalmitoyl glyceride, a P-selectin receptor inhibitor from the alga Dictyochloris fragrans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 387-9 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pharmacology and functions of metabotropic glutamate receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Annu Rev Pharmacol Toxicol 37: 205-37 (1997)
Emory University
Identification and characterization of the leech CNS cannabinoid receptor: coupling to nitric oxide release.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Brain Res 753: 219-24 (1997)
State University of New York At Old Westbury
Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1270-5 (1997)
Institute of Cancer Research
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1252-7 (1997)
Yamanouchi Pharmaceutical
Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1247-51 (1997)
Research Triangle Institute
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1230-46 (1997)
The University of Toledo
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1211-8 (1997)
Oregon State University
Novel indole-2-carboxamide and cycloalkeno[1,2-b]indole derivatives. Structure-activity relationships for high inhibition of human LDL peroxidation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1201-10 (1997)
Université
Arylamide inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1186-94 (1997)
National Cancer Institute-Bethesda
Molecular cloning and characterization of a new receptor for galanin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
FEBS Lett 405: 285-90 (1997)
Merck Research Laboratories
PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 281: 440-7 (1997)
Pharmacia & Upjohn
Multispecific organic anion transporter is responsible for the biliary excretion of the camptothecin derivative irinotecan and its metabolites in rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 281: 304-14 (1997)
University of Tokyo
Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochim Biophys Acta 1324: 296-308 (1997)
Medical College of Georgia
Rigidone, a sesquiterpene o-quinone from the gorgonian Pseudopterogorgia rigida.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 309-11 (1997)
Smithkline Beecham Pharmaceuticals
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Naunyn Schmiedebergs Arch Pharmacol 355: 365-75 (1997)
Northwestern University
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1173-7 (1997)
Duquesne University
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1169-72 (1997)
Abbott Laboratories
4-substituted cubylcarbinylamines: a new class of mechanism-based monoamine oxidase B inactivators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1165-8 (1997)
Northwestern University
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 1149-64 (1997)
Upjohn
Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1130-5 (1997)
Warner-Lambert
19-nor-10-azasteroids: a novel class of inhibitors for human steroid 5alpha-reductases 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1112-29 (1997)
Universit£
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1104-11 (1997)
Universit£
Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1075-89 (1997)
Vrije Universiteit
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1063-74 (1997)
Warner-Lambert
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1049-62 (1997)
Abbott Laboratories
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1026-40 (1997)
Merck Research Laboratories
Structural analogues of the calanolide anti-HIV agents. Modification of the trans-10,11-dimethyldihydropyran-12-ol ring (ring C).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1005-17 (1997)
Medichem Research
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 996-1004 (1997)
Zeneca Pharmaceuticals
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 990-5 (1997)
Hungarian Academy of Sciences
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 980-9 (1997)
Boehringer Ingelheim Pharmaceuticals
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 952-60 (1997)
Cooperation Pharmaceutique Fran�Aise
Depsides and depsidones as inhibitors of HIV-1 integrase: discovery of novel inhibitors through 3D database searching.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 942-51 (1997)
National Cancer Institute-Bethesda
Hydrazide-containing inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 937-41 (1997)
National Cancer Institute-Bethesda
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 930-6 (1997)
National Cancer Institute-Bethesda
HIV-1 integrase pharmacophore: discovery of inhibitors through three-dimensional database searching.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 920-9 (1997)
National Cancer Institute-Bethesda
Design, synthesis, and biological activities of four angiotensin II receptor ligands with gamma-turn mimetics replacing amino acid residues 3-5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 903-19 (1997)
Uppsala University
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 885-97 (1997)
Uppsala University
Synthesis and pharmacology of novel analogues of oxytocin and deaminooxytocin: directed methods for the construction of disulfide and trisulfide bridges in peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 864-76 (1997)
University of Minnesota
Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 858-63 (1997)
University of New Orleans
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 851-7 (1997)
National Institutes of Health
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 841-50 (1997)
Glaxo Wellcome
GRID/GOLPE 3D quantitative structure-activity relationship study on a set of benzamides and naphthamides, with affinity for the dopamine D3 receptor subtype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 833-40 (1997)
University Centre For Pharmacy
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 830-2 (1997)
Merck Research Laboratories
Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neuropsychiatry Clin Neurosci 8: 223-6 (1996)
TBA
Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 280: 1304-11 (1997)
Sankyo
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 280: 1241-9 (1997)
Institut De Recherches Servier
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 819-24 (1997)
Abbott Laboratories
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 754-65 (1997)
Merck Sharp and Dohme Research Laboratories
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 749-53 (1997)
University of Washington
Three-dimensional quantitative structure-activity relationship of melatonin receptor ligands: a comparative molecular field analysis study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 739-48 (1997)
Universit£
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 730-8 (1997)
Cocensys
From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 717-29 (1997)
Genentech
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 705-16 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 695-704 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Highly selective aldose reductase inhibitors. 3. Structural diversity of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 684-94 (1997)
Nippon Zoki Pharmaceutical
Structure-based design of substituted diphenyl sulfones and sulfoxides as lipophilic inhibitors of thymidylate synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 677-83 (1997)
Agouron Pharmaceuticals
Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 659-67 (1997)
Hebrew University
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 647-58 (1997)
University of Paris
Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 639-46 (1997)
Pharmacia & Upjohn
(+)-7-Deaza-5'-noraristeromycin as an anti-trypanosomal agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 622-4 (1997)
Auburn University
New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 608-21 (1997)
Cnrs-Biocis
Effects of log P and phenyl ring conformation on the binding of 5-phenylhydantoins to the voltage-dependent sodium channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 602-7 (1997)
University of Alabama At Birmingham
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 586-93 (1997)
Faes
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 574-85 (1997)
Università
Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 538-46 (1997)
Lilly Research Laboratories
Meta-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 506-14 (1997)
Ciba-Geigy
Ortho-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 495-505 (1997)
Novartis Pharmaceuticals
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 479-85 (1997)
Duquesne University
Synthesis and dihydrofolate reductase inhibitory activities of 2,4-diamino-5-deaza and 2,4-diamino-5,10-dideaza lipophilic antifolates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 470-8 (1997)
Duquesne University
Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 427-36 (1997)
Schering-Plough Research Institute
Tyrosine kinase inhibitors. 6. Structure-activity relationships among N- and 3-substituted 2,2'-diselenobis(1H-indoles) for inhibition of protein tyrosine kinases and comparative in vitro and in vivo studies against selected sulfur congeners.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 40: 413-26 (1997)
Parke-Davis Pharmaceutical Research
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 408-12 (1997)
Charles University
Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Clin Invest 99: 789-98 (1997)
Cedars-Sinai Research Institute
Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 280: 1102-8 (1997)
University of Cambridge
Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 280: 802-12 (1997)
Sanofi Recherche
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 385-90 (1997)
Abbott Laboratories
Selectin-ligand interactions revealed by molecular dynamics simulation in solution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 362-9 (1997)
Kanebo
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 331-41 (1997)
Ferring Research Institute
Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 322-30 (1997)
Abbott Laboratories
Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 313-21 (1997)
Dainippon Pharmaceutical
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 300-12 (1997)
Solvay Pharma
Dopamine D2-like sites in schizophrenia, but not in Alzheimer's, Huntington's, or control brains, for [3H]benzquinoline.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Synapse 25: 137-46 (1997)
University of Toronto
Characterization of recombinant human P2X4 receptor reveals pharmacological differences to the rat homologue.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 51: 109-18 (1997)
Max-Planck Institute For Experimental Medicine
Diltiazem-like calcium entry blockers: a hypothesis of the receptor-binding site based on a comparative molecular field analysis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 125-31 (1997)
Universita' Degli Studi Di Siena
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 117-24 (1997)
Groningen University Hospital
Synthesis and evaluation of trimetoquinol derivatives: novel thromboxane A2/prostaglandin H2 antagonists with diminished beta-adrenergic agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 85-91 (1997)
Ohio State University
3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 73-84 (1997)
Cocensys
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 61-72 (1997)
Cocensys
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 50-60 (1997)
Dupont Pharmaceuticals
Highly selective, novel analogs of 4-[2-(diphenylmethoxy)ethyl]- 1-benzylpiperidine for the dopamine transporter: effect of different aromatic substitutions on their affinity and selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 35-43 (1997)
Organix
Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 18-23 (1997)
Allergan
Synthesis and characterization of technetium-99m-labeled tropanes as dopamine transporter-imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 9-17 (1997)
University of Pennsylvania
Rationally designed inhibitors of inosine monophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 4-8 (1997)
University of Chicago
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 1-3 (1997)
Neurogen
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropsychopharmacology 16: 93 (1997)
University of Toronto
Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 60: 6-8 (1997)
Xenova
Pharmacological properties of recombinant "diazepam-insensitive" GABAA receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropharmacology 35: 1307-14 (1996)
National Institute of Diabetes, Digestive and Kidney Diseases
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 39: 5119-36 (1997)
Eli Lilly
3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 250-9 (1997)
Division of Warner Lambert
Coumarin-based inhibitors of HIV integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 242-9 (1997)
National Cancer Institute-Bethesda
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 226-35 (1997)
Eli Lilly
Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 216-25 (1997)
University of Alberta
Synthesis and inhibition studies of sulfur-substituted squalene oxide analogues as mechanism-based inhibitors of 2,3-oxidosqualene-lanosterol cyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 201-9 (1997)
Simon Fraser University
Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 192-200 (1997)
Warner-Lambert
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 40: 181-91 (1997)
Dupont Pharmaceuticals
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)