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Interactions of glycyrrhizin with organic anion transporting polypeptides of rat and human liver.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hepatol Res 26: 343-347 (2003)
University of Zurich
N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 307: 322-30 (2003)
Novartis Pharma
In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 307: 138-45 (2003)
National Institute On Drug Abuse
The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 10: 705-12 (2003)
Merck Research Laboratories
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4196-204 (2003)
Georgetown University Medical Center
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4188-95 (2003)
Alcon Research
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4182-7 (2003)
University of Innsbruck
In vitro analysis of stable, receptor-selective neurotensin[8-13] analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4141-8 (2003)
Medical University of South Carolina
Orally active oxime derivatives of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and pharmacological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4136-40 (2003)
University Center For Pharmacy
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4104-12 (2003)
Ligand Pharmaceuticals
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4087-103 (2003)
Ligand Pharmaceuticals
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4070-86 (2003)
Glaxosmithkline
Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4063-9 (2003)
Moscow State University
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 4050-62 (2003)
Pharmacia
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4043-9 (2003)
Pharmacia
Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4032-42 (2003)
Università
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4021-31 (2003)
Johnson and Johnson Pharmaceutical Research and Development
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 4002-8 (2003)
University of Maryland
Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone sscaffold: analysis of X-ray crystal structure of enzyme inhibitor complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3985-4001 (2003)
Link£Ping University
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3975-84 (2003)
Dr. Reddy'S Laboratories
Receptor-mediated targeting of a photosensitizer by its conjugation to gonadotropin-releasing hormone analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3965-74 (2003)
Institute of Science
Discovery and preclinical characterization of (+)-3-[4-(1- piperidinoethoxy)phenyl]spiro[indene- 1,1'-indane]-5,5'-diol hydrochloride: a promising nonsteroidal estrogen receptor agonist for hot flush.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3961-4 (2003)
Dainippon Pharmaceutical
The first potent and selective non-imidazole human histamine H4 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3957-60 (2003)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3953-6 (2003)
Eli Lilly
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3375-9 (2003)
Neurocrine Biosciences
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3371-4 (2003)
Neurocrine Biosciences
Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3367-70 (2003)
Neurocrine Biosciences
Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3361-5 (2003)
Berlex Biosciences
N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3355-9 (2003)
Virginia Commonwealth University
Stereoselective synthesis of phosphoramidate alpha(2-6)sialyltransferase transition-state analogue inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3351-4 (2003)
Universitaet Konstanz
Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3341-4 (2003)
Shire Biochem
Alpha-keto amides as inhibitors of histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3331-5 (2003)
Abbott Laboratories
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3323-6 (2003)
Merck Research Laboratories
Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3317-22 (2003)
Neurocrine Biosciences
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3311-5 (2003)
Neurocrine Biosciences
Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3301-3 (2003)
University of California
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3297-300 (2003)
Mcgill University/Royal Victoria Hospital
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3293-6 (2003)
Friedrich-Alexander University
Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3277-80 (2003)
Eli Lilly
Synthesis and PDF inhibitory activities of novel benzothiazolylidenehydroxamic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3273-6 (2003)
Senju Pharmaceutical
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3247-52 (2003)
Purdue Pharma
Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3243-6 (2003)
Pfizer
Cyclohexanedione herbicides are inhibitors of rat heart acetyl-CoA carboxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3237-42 (2003)
Eli Lilly
Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3231-5 (2003)
Universidad De Buenos Aires
Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3203-5 (2003)
Nih
Design and synthesis of fluorinated RXR modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3191-5 (2003)
Eli Lilly
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3185-90 (2003)
Merck Research Laboratories
Regulation of gene expression by synthetic dimerizers with novel specificity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3181-4 (2003)
Ariad Gene Therapeutics
Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3177-80 (2003)
Universidad Complutense
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3171-6 (2003)
University of Ljubljana
Reversed hydroxamate-bearing thermolysin inhibitors mimic a high-energy intermediate along the enzyme-catalyzed proteolytic reaction pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3161-6 (2003)
Pohang University of Science and Technology
1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3155-9 (2003)
F. Hoffmann-La Roche
Biological activities of alpha-mangostin derivatives against acidic sphingomyelinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3151-3 (2003)
Keio University
Analysis of the critical structural determinant(s) of species-selective peroxisome proliferator-activated receptor alpha (PPAR alpha)-activation by phenylpropanoic acid-type PPAR alpha agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3145-9 (2003)
Kyorin Pharmaceutical
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3129-32 (2003)
Abbott Laboratories
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 332: 13-21 (2003)
Morphochem
Potent small molecule inhibitors of spleen tyrosine kinase (Syk).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3111-4 (2003)
Aventis Pharmaceuticals
Mapping the kinase domain of Janus Kinase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3105-10 (2003)
Aventis Pharmaceuticals
The kinetics of binding to p38MAP kinase by analogues of BIRB 796.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3101-4 (2003)
Boehringer Ingelheim Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3097-100 (2003)
Aventis Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3091-5 (2003)
Aventis Pharmaceuticals
Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3087-90 (2003)
Scios
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3083-6 (2003)
University of Newcastle
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3079-82 (2003)
University of Newcastle
Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3071-4 (2003)
Ariad Pharmaceuticals
Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3067-70 (2003)
Ariad Pharmaceuticals
Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3063-6 (2003)
Ariad Pharmaceuticals
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3059-62 (2003)
Glaxosmithkline
6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3055-7 (2003)
Glaxosmithkline
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3049-53 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3045-8 (2003)
Ghent University
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3041-4 (2003)
Abbott Laboratories
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3031-4 (2003)
Wyeth Research
Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3027-30 (2003)
Instituto De QuíMica MéDica (Csic)
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 3021-6 (2003)
Astrazeneca
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3015-9 (2003)
Kyoto University
Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3005-7 (2003)
Nih
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 3001-4 (2003)
Kyowa Hakko Kogyo
2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2993-6 (2003)
Academy of Sciences of The Czech Republic
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2989-92 (2003)
Academy of Sciences of The Czech Republic
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2985-8 (2003)
Glaxosmithkline
Synthesis of three enantiomeric pairs of scyllo-inositol phosphate and molecular interactions between all possible regioisomers of scyllo-inositol phosphate and inositol 1,4,5-trisphosphate 3-kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2981-4 (2003)
Pohang University of Science & Technology
Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2977-80 (2003)
Wyeth Research
Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2973-6 (2003)
Merck Research Laboratories
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2967-71 (2003)
Novartis Pharma
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2961-6 (2003)
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2955-60 (2003)
Astrazeneca
Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 31: 398-411 (2003)
Johns Hopkins University School of Medicine
Understanding binding affinity: a combined isothermal titration calorimetry/molecular dynamics study of the binding of a series of hydrophobically modified benzamidinium chloride inhibitors to trypsin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 125: 10570-9 (2003)
University of Groningen
10-Methoxydihydrofuscin, fuscinarin, and fuscin, novel antagonists of the human CCR5 receptor from Oidiodendron griseum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1116-7 (2003)
Merlion Pharmaceuticals
CT2108A and B: New fatty acid synthase inhibitors as antifungal agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 1041-6 (2003)
Panlabs
Pyrazole derivatives as partial agonists for the nicotinic acid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3945-51 (2003)
Leiden/Amsterdam Center For Drug Research
Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3930-7 (2003)
Virginia Commonwealth University
Synthesis and biological evaluation of novel flavone-8-acetic acid derivatives as reversible inhibitors of aminopeptidase N/CD13.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3900-13 (2003)
Institut Curie
N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3883-99 (2003)
Johann Wolfgang Goethe-UniversitäT
Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3877-82 (2003)
Institute of Research
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3865-76 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3853-64 (2003)
Universit£
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3840-52 (2003)
Institut De Recherches Servier
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3822-39 (2003)
Universit£
3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3811-21 (2003)
Ghent University
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3778-81 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3775-7 (2003)
Ewha Womans University
Structure-based design of a macrocyclic inhibitor for peptide deformylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3771-4 (2003)
The Ohio State University
Characterization of the role of polar amino acid residues within predicted transmembrane helix 17 in determining the substrate specificity of multidrug resistance protein 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochemistry 42: 9989-10000 (2003)
Queen'S University
Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 474: 137-40 (2003)
Harvard University
New potential uroselective NO-donor alpha1-antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3762-5 (2003)
Università
Bispyridinium cyclophanes: novel templates for human choline kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3754-7 (2003)
Universidad De Granada
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3728-33 (2003)
University of Arizona
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 3709-27 (2003)
Merck Frosst Centre For Therapeutic Research
A comparison of phosphonothioic acids with phosphonic acids as phosphatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3703-8 (2003)
Utah State University
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3655-61 (2003)
Procter & Gamble Pharmaceuticals
Structure-based design and synthesis of novel potent Na+,K+ -ATPase inhibitors derived from a 5alpha,14alpha-androstane scaffold as positive inotropic compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3644-54 (2003)
Prassis Istituto Di Ricerche Sigma-Tau
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3612-22 (2003)
Lg Life Sciences
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3581-99 (2003)
Kyorin Pharmaceutical
Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3568-71 (2003)
Universit£
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3563-4 (2003)
Institut F£R Molekularbiologie Und Biophysik
Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3559-62 (2003)
National Institutes of Health
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Struct Biol 10: 764-9 (2003)
Merck Research Laboratories
A natural product ligand of the oxysterol receptor, liver X receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 307: 291-6 (2003)
Eli Lilly
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem J 375: 255-62 (2003)
University of Dundee
[BRCA1 protein expression in sporadic breast and its clinical significance].![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Zhonghua Wai Ke Za Zhi 41: 186-8 (2003)
Anhui Medical University
Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Neurosci 18: 290-5 (2003)
University of Innsbruck
Acetophenone derivatives from Acronychia pedunculata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 990-3 (2003)
National Cheng Kung University
Antiparasitic alkaloids from Psychotria klugii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 962-7 (2003)
University of Mississippi
Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 954-7 (2003)
Universidad De Chile
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3555-8 (2003)
Università
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3526-35 (2003)
Purdue University
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3514-25 (2003)
Pfizer
Development of a water-soluble matrix metalloproteinase inhibitor as an intra-arterial infusion drug for prevention of restenosis after angioplasty.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3497-501 (2003)
National Cardiovascular Center Research Institute
A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3483-96 (2003)
Organix
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3463-75 (2003)
Domp&Egrove
Design and synthesis of dihydrofolate reductase inhibitors encompassing a bridging ester group. Evaluation in a mouse colitis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3455-62 (2003)
Uppsala University
Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3452-4 (2003)
Johns Hopkins University School of Medicine
Identification of"latent hits" in compound screening collections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3441-4 (2003)
Organon Laboratories
Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3437-40 (2003)
Abbott Laboratories
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2799-803 (2003)
Wyeth Research
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2795-8 (2003)
Merck Research Laboratories
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2781-4 (2003)
Merck Research Laboratories
Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2777-80 (2003)
Institute of Chemical Technology
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2773-5 (2003)
Gedeon Richter
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2759-63 (2003)
Università
Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2745-8 (2003)
Mrl Rome
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2741-4 (2003)
Hokkaido Collaboration Center
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2737-40 (2003)
Hokkaido Collaboration Center
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2719-25 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2715-8 (2003)
British Biotech Pharmaceuticals
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2709-13 (2003)
British Biotech Pharmaceuticals
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2687-92 (2003)
University of Mainz
Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2659-62 (2003)
Universit£
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2655-8 (2003)
The University of Tokyo
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2647-50 (2003)
University of Cincinnati
Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2625-8 (2003)
Astrazeneca R&D Charnwood
GABA(C) receptors as drug targets.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Curr Drug Targets CNS Neurol Disord 2: 260-8 (2003)
University of Sydney
High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Comb Chem 5: 456-64 (2003)
Uppsala University
2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2591-4 (2003)
Wyeth Research
Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2587-90 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2583-6 (2003)
Kyowa Hakko Kogyo
Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2577-81 (2003)
National Cancer Institute-Frederick
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2573-6 (2003)
Merck Research Laboratories
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2569-72 (2003)
Merck Research Laboratories
Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2565-8 (2003)
Virginia Commonwealth University
Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2561-3 (2003)
Inha University
Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2535-8 (2003)
National Research Institute of Chinese Medicine
Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2513-8 (2003)
Guilford Pharmaceuticals
3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2509-12 (2003)
University of California
2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2497-500 (2003)
Neurogen
High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2493-6 (2003)
Mcmaster University
Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2485-8 (2003)
Merck Research Laboratories
Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2481-4 (2003)
Central Drug Research Institute
Comparative molecular field analysis (CoMFA) of phthalazine derivatives as phosphodiesterase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2473-9 (2003)
National Institute of Pharmaceutical Education and Research
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2465-8 (2003)
Hoffmann-La Roche
Effect of catechol derivatives on cell growth and lipoxygenase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2435-9 (2003)
Aston University
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3412-23 (2003)
Industrial Research
Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3403-11 (2003)
Washington University
Novel benzylidene-9(10H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3382-94 (2003)
Westphalian Wilhelms-University
Tethered dimers as NAD synthetase inhibitors with antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3371-81 (2003)
University of Alabama At Birmingham
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3354-70 (2003)
F. Hoffmann-La Roche
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3333-41 (2003)
Novo Nordisk
Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3326-32 (2003)
Institute of Biomedical Chemistry of Russian Academy of Medical Sciences
A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3314-25 (2003)
University of California
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3292-9 (2003)
National Cancer Institute-Frederick
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3257-74 (2003)
Glaxosmithkline
l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3245-56 (2003)
The University of Georgia
Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3230-44 (2003)
Eberhard-Karls-University T£Bingen
Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3221-9 (2003)
National Hellenic Research Foundation
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3201-9 (2003)
Kobe Gakuin University
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3197-200 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
First dual aromatase-steroid sulfatase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 3193-6 (2003)
University of Bath
Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3189-92 (2003)
Eli Lilly
Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Chem Neuroanat 25: 233-47 (2003)
University of Michigan
Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biosci Biotechnol Biochem 67: 980-8 (2003)
Gifu University
Pochonins A-F, new antiviral and antiparasitic resorcylic acid lactones from Pochonia chlamydosporia var. catenulata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 829-37 (2003)
Bayer Healthcare
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 739-42 (2003)
University of Karachi
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3174-7 (2003)
University of Bath
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3162-5 (2003)
Osaka University
Structural determinants of selective thyromimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3152-61 (2003)
University of California
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3138-51 (2003)
Guilford Pharmaceuticals
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3127-37 (2003)
Research Triangle Institute
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3116-26 (2003)
Seoul National University
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3102-8 (2003)
Università
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3060-71 (2003)
Eli Lilly
Histamine-releasing activity and binding to the FcepsilonRI alpha human mast cell receptor subunit of mast cell degranulating peptide analogues with alanine substitutions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 3008-12 (2003)
Mount Sinai School of Medicine
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2973-84 (2003)
Merck Research Laboratories
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2945-57 (2003)
Novartis Pharmaceuticals
A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2932-44 (2003)
University of Illinois At Urbana-Champaign
Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2917-31 (2003)
Institut FüR Molekulare Physiologie
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2908-16 (2003)
National Institute On Drug Abuse
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2877-94 (2003)
Universit£
Docking and database screening reveal new classes of Plasmodium falciparum dihydrofolate reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2834-45 (2003)
Università
Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2816-8 (2003)
University of Minnesota
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2795-812 (2003)
Virginia Commonwealth University
Novel IKK inhibitors: beta-carbolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2419-22 (2003)
Millennium Pharmaceuticals
Identification of oxidation product of arbutin in mushroom tyrosinase assay system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2409-12 (2003)
University of California
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2405-8 (2003)
Bristol-Myers Squibb
Constrained phytoestrogens and analogues as ERbeta selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2399-403 (2003)
Wyeth Research
Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2393-7 (2003)
Eli Lilly
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2389-91 (2003)
Cnrs
Synthesis and inhibitory activity of ubiquinone-acetogenin hybrid inhibitor with bovine mitochondrial complex I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2385-8 (2003)
Kyoto University
Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2381-4 (2003)
Combichem
Synthesis and biological testing of non-fluorinated analogues of levofloxacin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2373-5 (2003)
Procter & Gamble Pharmaceuticals
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2369-72 (2003)
Pharmacia
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2363-7 (2003)
Pharmacia
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2355-8 (2003)
Lead Gene
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2347-50 (2003)
Tanabe Seiyaku
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2341-5 (2003)
Tanabe Seiyaku
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2337-40 (2003)
Amgen
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2331-6 (2003)
Pfizer
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2319-25 (2003)
Pharmacia
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2307-10 (2003)
Abbott Laboratories
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2297-302 (2003)
Boehringer Ingelheim Pharma
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2291-5 (2003)
Boehringer Ingelheim Pharma
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2281-4 (2003)
University of Sydney
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2261-7 (2003)
Eli Lilly
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem J 374: 639-46 (2003)
University of Padova
Complexation and chiral recognition thermodynamics of gamma-cyclodextrin with N-acetyl- and N-carbobenzyloxy-dipeptides possessing two aromatic rings.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Org Chem 68: 5228-35 (2003)
Japan Science and Technology Agency
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 64: 143-53 (2003)
Abbott Laboratories
Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2790-3 (2003)
National Cancer Institute-Frederick
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2774-89 (2003)
Novartis Institute For Biomedical Research
Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2740-54 (2003)
University of Pittsburgh
Synthesis of substituted 6-anilinouracils and their inhibition of DNA polymerase IIIC and Gram-positive bacterial growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2731-9 (2003)
Glsynthesis
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2716-30 (2003)
University of Vermont
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2683-96 (2003)
Ligand Pharmaceuticals
The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2641-55 (2003)
Wroclaw University of Technology
Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2631-40 (2003)
Chinese Academy of Sciences
Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2621-30 (2003)
National Cancer Institute-Frederick
Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2606-20 (2003)
Umr C8076 (Cnrs)
Characterization of a series of 3-amino-2-phenylpropene derivatives as novel bovine chromaffin vesicular monoamine transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2599-605 (2003)
Wichita State University
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2589-98 (2003)
Nida-Irp
Inhibition of Cdc25 phosphatases by indolyldihydroxyquinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2580-8 (2003)
Duke University
QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2572-9 (2003)
Uppsala University
Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2569-71 (2003)
Wyeth Research
Borrelidin induces the transcription of amino acid biosynthetic enzymes via a GCN4-dependent pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2235-7 (2003)
Boston University
Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2231-4 (2003)
Cubist Pharmaceutical
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2217-22 (2003)
Indiana University School of Medicine
4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2211-5 (2003)
Pfizer
6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2205-9 (2003)
University of Alberta
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2199-203 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2195-8 (2003)
Wyeth Research
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2191-4 (2003)
Wyeth Research
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2179-83 (2003)
National Institute On Drug Abuse-Intramural Research Program
Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2173-7 (2003)
National Cancer Institute-Frederick
Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2167-72 (2003)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Bivalent biogenic amine reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2151-4 (2003)
Human Biomolecular Research Institute
Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2145-9 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Nicotinyl aspartyl ketones as inhibitors of caspase-3.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 2137-40 (2003)
Merck Frosst Canada
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2131-5 (2003)
Abbott Laboratories
2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2113-8 (2003)
Glaxosmithkline
Novel inhibitors of procollagen C-terminal proteinase. Part 1: diamino Acid hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2101-4 (2003)
Combichem
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2097-100 (2003)
Guilford Pharmaceuticals
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropsychopharmacology 28: 1400-11 (2003)
Case Western Reserve University
Urea small molecule agonists on mouse melanocortin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2079-82 (2003)
University of Florida
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2075-8 (2003)
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2071-4 (2003)
Ligand Pharmaceuticals
Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2059-63 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2055-8 (2003)
Pfizer
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2051-3 (2003)
Ligand Pharmaceuticals
Inhibition of mandelate racemase by alpha-fluorobenzylphosphonates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2041-4 (2003)
Dalhousie University
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2035-40 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2029-33 (2003)
Basf
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2021-4 (2003)
Organon K.K.
The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 2003-7 (2003)
Abbott Laboratories
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1997-2001 (2003)
Novartis Pharma
The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1993-6 (2003)
The University of Georgia
Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1989-92 (2003)
Pfizer
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1985-8 (2003)
Georgia Institute of Technology
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1981-4 (2003)
Schering
Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1977-80 (2003)
Umr Cnrs 5074
Sphingomyelin analogues as inhibitors of sphingomyelinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1963-6 (2003)
Taisho Pharmaceutical
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1959-61 (2003)
The Schering Plough Research Institute
Analysis of 6-(2,2-Dichloroacetamido)chrysene interaction with the hypoxanthine phosphoribosyltransferase from Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2548-50 (2003)
University of Connecticut
Synthesis and antitumor activity of novel O-carbamoylmethyloxime derivatives of radicicol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2534-41 (2003)
Pharmaceutical Research Institute
Design, synthesis, and evaluation of analogues of 3,3,3-trifluoro-2-hydroxy-2-phenyl-propionamide as orally available general anesthetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2494-501 (2003)
University of Virginia
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2482-93 (2003)
Sapienza University of Rome
Discovery and structure-activity relationships of novel piperidine inhibitors of farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2467-73 (2003)
Pharmaceutical Research Institute
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2446-55 (2003)
Shionogi
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2436-45 (2003)
Shionogi
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2413-26 (2003)
Merck Frosst Centre For Therapeutic Research
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2404-12 (2003)
Abbott
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2376-96 (2003)
Wyeth Research
Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2361-75 (2003)
Wyeth Research
Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2352-60 (2003)
Università
Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2345-51 (2003)
Accelrys
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2334-44 (2003)
Novartis Pharma
Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2304-12 (2003)
F. Hoffmann-La Roche
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2283-6 (2003)
Pfizer
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2279-82 (2003)
University of Bologna
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2261-70 (2003)
Technische Universit£T Darmstadt
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Biophys Res Commun 305: 909-14 (2003)
St. Mary'S Hospital
Isolation and synthesis of a new bioactive ellagic acid derivative from Combretum yunnanensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 729-31 (2003)
Teikyo University
New sesquiterpene quinols from a Micronesian sponge, Aka sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 686-9 (2003)
University of Oklahoma
Brominated polyacetylenes from the Philippines sponge Diplastrella sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 667-70 (2003)
University of California At San Diego
Developmental expression of heteromeric nicotinic receptor subtypes in chick retina.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 63: 1329-37 (2003)
University of Milan
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 63: 1223-9 (2003)
Case Western Reserve University
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Life Sci 73: 371-9 (2003)
Merck Research Laboratories
The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 306: 954-64 (2003)
Institut De Recherches Servier
Synthesis and SAR of cis-1-benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1943-6 (2003)
Rheogene
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1939-42 (2003)
Sugen
Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1935-7 (2003)
Gpc Biotech
Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1931-4 (2003)
Neurocrine Biosciences
6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1927-30 (2003)
Neurocrine Biosciences
Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1923-6 (2003)
Merck Frosst Centre For Therapeutic Research
A novel estrogen receptor ligand template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1919-22 (2003)
Bayer
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1911-4 (2003)
Rensselaer Polytechnic Institute
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1907-10 (2003)
Eli Lilly
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1903-5 (2003)
Eli Lilly
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1897-901 (2003)
Abbott Laboratories
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1891-5 (2003)
Merck Research Laboratories
Potent, selective inhibitors of protein tyrosine phosphatase 1B.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1887-90 (2003)
Abbott Laboratories
Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1883-6 (2003)
Rheogene
Design and synthesis of novel pyrrolidine-containing bradykinin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1879-82 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1873-8 (2003)
Roche Bioscience
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1865-8 (2003)
Universit£
Amide analogues of TSA: synthesis, binding mode analysis and HDAC inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1861-4 (2003)
Vrije Universiteit Brussel
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1857-9 (2003)
Eli Lilly
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2246-9 (2003)
The Danish University of Pharmaceutical Sciences
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2227-40 (2003)
Merck Sharp & Dohme Research Laboratories
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2216-26 (2003)
University of North Carolina At Chapel Hill
Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2205-15 (2003)
Wayne State University
Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2197-204 (2003)
University of Montpellier
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2187-96 (2003)
University of Agricultural Sciences and Veterinary Medicine
Metal coordination-based inhibitors of adenylyl cyclase: novel potent P-site antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2177-86 (2003)
Millennium Pharmaceuticals
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2169-76 (2003)
Universit£
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2152-68 (2003)
Pfizer
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2117-24 (2003)
Universit£
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2110-6 (2003)
Bristol-Myers Squibb
Structure-activity relationships of dynorphin a analogues modified in the address sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2104-9 (2003)
University of California
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2093-103 (2003)
Abbott Laboratories
Binding structures and potencies of oxidosqualene cyclase inhibitors with the homologous squalene-hopene cyclase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2083-92 (2003)
Albert-Ludwigs-University of Freiburg
Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2074-82 (2003)
Johnson & Johnson Pharmaceutical Research and Development
3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2031-48 (2003)
Institut F£R Pharmazeutische Chemie Der Philipps-Universit£T Marburg
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 2027-30 (2003)
Eli Lilly
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2023-6 (2003)
Neurocrine Biosciences
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2017-22 (2003)
Aventis Pharmaceuticals
Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Mol Biol 329: 93-120 (2003)
Celera
Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Comb Chem 5: 336-44 (2003)
University of Anterwerp
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 20: 537-44 (2003)
Schering-Plough Research Institute
Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 42: 5333-40 (2003)
Medical College of Ohio
Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1829-35 (2003)
Aventis Pharmaceuticals
Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1825-7 (2003)
Instituto PolitéCnico Nacional
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1821-4 (2003)
Merck Research Laboratories
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1809-12 (2003)
Merck Research Laboratories
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1801-4 (2003)
Merck Research Laboratories
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1795-9 (2003)
Bristol-Myers Squibb
A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1791-4 (2003)
Schering-Plough Research Institute
Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1783-6 (2003)
Université
Non-imidazole heterocyclic histamine H3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1767-70 (2003)
Johnson & Johnson Pharmaceutical Research and Development
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1759-62 (2003)
F. Hoffmann-La Roche
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1741-4 (2003)
Abbott Laboratories
Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1729-32 (2003)
Peking University
Solid-phase synthesis of endothelin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1721-4 (2003)
Basf
New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1705-8 (2003)
Institut De Recherches Servier
Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1691-4 (2003)
Roche Discovery Welwyn
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1673-7 (2003)
Merck Research Laboratories
Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5'-thioadenosine derivatives. Antiviral effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1649-52 (2003)
Umr 6519
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1639-43 (2003)
Dr. Reddy'S Laboratories
Structure-activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1623-6 (2003)
The University of Birmingham
Synthesis and tyrosinase inhibitory activity of novel N-hydroxybenzyl-N-nitrosohydroxylamines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 31: 129-35 (2003)
Keio University
Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 10: 341-9 (2003)
University of North Carolina At Chapel Hill
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 2008-16 (2003)
Vrije Universiteit
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1997-2007 (2003)
Georgetown University Medical Center
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1989-96 (2003)
Guilford Pharmaceuticals
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1980-8 (2003)
Hokkaido University
Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1962-79 (2003)
Université
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1940-7 (2003)
National Cancer Institute-Frederick
Design of selective peptidomimetic agonists for the human orphan receptor BRS-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1918-30 (2003)
Technische UniversitäT MüNchen
Antiviral amphipathic oligo- and polyribonucleotides: analogue development and biological studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1878-85 (2003)
University of Utah
2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1870-7 (2003)
Deakin University
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1858-69 (2003)
University of Pennsylvania
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1845-57 (2003)
Ajinomoto
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 1831-44 (2003)
University of Pennsylvania
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1811-23 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzodiazepines as potent and selective bradykinin B1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1803-6 (2003)
Merck Research Laboratories
Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1799-802 (2003)
Elan Pharmaceuticals
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1775-94 (2003)
Research Triangle Institute
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 306: 377-86 (2003)
Pudue Pharma Discovery Research
Dihydropiperazine neonicotinoid compounds. Synthesis and insecticidal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Agric Food Chem 51: 3035-42 (2003)
Dow Agrosciences
Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 278: 27652-7 (2003)
Schering-Plough Research Institute
Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 569-71 (2003)
The University of Tokyo
Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 551-3 (2003)
Merck Research Laboratories
Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria lateriflora.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 535-7 (2003)
Tom'S of Maine
Insights into antifolate resistance from malarial DHFR-TS structures.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Struct Biol 10: 257-65 (2003)
Mahidol University
Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 565-72 (2003)
University of Tennessee
Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
AIDS 17: 1092-4 (2003)
Tufts University School of Medicine
The selective inhibition of phosphatases by natural toxins: the anhydride domain of tautomycin is not a primary factor in controlling PP1/PP2A selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1597-600 (2003)
University of California Irvine
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1591-5 (2003)
Wayne State University
New scaffolds in the development of mu opioid-receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1585-9 (2003)
Astrazeneca R&D Montreal
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1581-4 (2003)
Glaxosmithkline
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1577-80 (2003)
Glaxosmithkline
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1571-4 (2003)
Abbott Laboratories
Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1561-4 (2003)
University of Montpellier
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1553-5 (2003)
Ufr Des Sciences Pharmaceutiques
Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1549-52 (2003)
Sookmyung Women'S University
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1543-7 (2003)
Johnson & Johnson Pharmaceutical Research & Development
A novel metal-chelating inhibitor of protein farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1523-6 (2003)
Kumamoto University
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1517-21 (2003)
Glaxosmithkline
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1513-5 (2003)
Genentech
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1769-72 (2003)
Neurocrine Biosciences
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1764-8 (2003)
Kyoto University
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1758-63 (2003)
University of Innsbruck
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1726-36 (2003)
Harvard Medical School
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1716-25 (2003)
F. Hoffmann-La Roche
Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1670-82 (2003)
Purdue University
Aromatic reduced amide bond peptidomimetics as selective inhibitors of neuronal nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1661-9 (2003)
Northwestern University
An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 1636-44 (2003)
Academy of Sciences of The Czech Republic
Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 1627-35 (2003)
Glaxosmithkline
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 1580-8 (2003)
Karo Bio
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1571-9 (2003)
National Cancer Institute-Frederick
Pharmacological studies of thyrotropin-releasing hormone (TRH) receptors from Xenopus laevis: is xTRHR3 a TRH receptor?![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Endocrinology 144: 1842-6 (2003)
National Institute of Diabetes and Digestive and Kidney Diseases
Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Pharmacol 63: 1094-103 (2003)
The Netherlands Cancer Institute
[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 63: 1082-93 (2003)
Johnson and Johnson Pharmaceutical Research and Development, Beerse
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Biochem 270: 1746-58 (2003)
Uppsala University
Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzyme Inhib Med Chem 17: 409-14 (2002)
UniversitÉ
SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 306: 407-20 (2003)
Sanofi-Synthelabo Research
Interactions of human organic anion as well as cation transporters with indoxyl sulfate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Pharmacol 466: 13-20 (2003)
Nagoya University School of Medicine
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1563-6 (2003)
University of Bath
Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1538-45 (2003)
Organix
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1523-30 (2003)
Freie Universit£T Berlin
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1512-22 (2003)
Universidad Complutense
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1492-503 (2003)
Leiden University
Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1484-91 (2003)
Free University of Berlin
Kinase inhibitors: not just for kinases anymore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1478-83 (2003)
Northwestern University
Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1465-9 (2003)
Niddk
Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1456-64 (2003)
Georgia Institute of Technology
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1429-39 (2003)
Universit£
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1419-28 (2003)
Università
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1408-18 (2003)
Signalgene
Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1390-407 (2003)
University of Wuerzburg
Mechanism of action of the diazabicyclononanone-type kappa-agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1383-9 (2003)
UniversitäT WüRzburg
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1350-8 (2003)
The Danish University of Pharmaceutical Sciences
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1337-49 (2003)
Boehringer Ingelheim Pharmaceuticals
Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1318-29 (2003)
Università
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1306-17 (2003)
Novo Nordisk
Generation of ligand conformations in continuum solvent consistent with protein active site topology: application to thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1293-305 (2003)
Thrombosis Research Institute
Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1283-5 (2003)
Shire Biochem
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1279-82 (2003)
University of Maryland
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 125: 4087-96 (2003)
Abbott Laboratories
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1495-8 (2003)
3-Dimensional Pharmaceuticals
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1487-90 (2003)
Wyeth-Ayerst Research
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1483-6 (2003)
Glaxosmithkline
Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1475-8 (2003)
The Ohio State University
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1463-7 (2003)
Aventis Pharma Deutschland
From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1459-62 (2003)
Centre De Recherche Pierre Fabre
Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1455-8 (2003)
Centre De Recherche Pierre Fabre
Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1451-4 (2003)
Oxford University
High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1445-9 (2003)
Molecumetics
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1441-4 (2003)
Merck Research Laboratories
Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1429-32 (2003)
Universidad Complutense
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1425-8 (2003)
Pfizer
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1415-8 (2003)
Boehringer Ingelheim Pharmaceuticals
Peptoid mimics of agouti related protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1409-13 (2003)
University of California
3D-QSAR studies on thieno[3,2-d]pyrimidines as phosphodiesterase IV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1403-8 (2003)
National Institute of Pharmaceutical Education and Research (NIPER)
Two new carbazole alkaloids from Murraya koenigii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 416-8 (2003)
Chinese Academy of Sciences
Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 306: 253-61 (2003)
Lcg Bioscience
Synthesis of potent oxindole CDK2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 11: 1873-81 (2003)
Hoffmann-La Roche
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1385-9 (2003)
Niddk
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1367-71 (2003)
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1363-6 (2003)
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1359-62 (2003)
Abbott Laboratories
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1353-7 (2003)
Merck Research Laboratories
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1345-8 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure--activity relationships of aroylpyrrole alkylamide bradykinin (B2) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1341-4 (2003)
Johnson & Johnson Pharmaceutical Research and Development
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1337-40 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibition of telomerase by BIBR 1532 and related analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1333-6 (2003)
University of Texas At Dallas
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1325-8 (2003)
Abbott Laboratories
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1317-20 (2003)
Wyeth Research
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1313-6 (2003)
Wyeth Research
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1307-11 (2003)
Roche Research Center
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1301-5 (2003)
Dainippon Pharmaceutical
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1297-300 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1293-6 (2003)
Abbott Laboratories
[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1291-2 (2003)
Pfizer
Phenylacetic acid derivatives as hPPAR agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1277-80 (2003)
Merck Research Laboratories
Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1273-6 (2003)
Bristol-Myers Squibb Pri
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1269-72 (2003)
Tohoku Pharmaceutical University
The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1261-4 (2003)
Instituto Universitario De Bio-Org£Nica
Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1241-4 (2003)
Utrecht University
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1231-5 (2003)
Eli Lilly
Interaction of human and rat organic anion transporter 2 with various cephalosporin antibiotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Pharmacol 465: 1-7 (2003)
Kyorin University
Inhibition of P-glycoprotein by newer antidepressants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 305: 197-204 (2003)
University of Heidelberg
Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 143-50 (2003)
Georgetown University
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 131-42 (2003)
Case Western Reserve University
Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 57-69 (2003)
Bristol-Myers Squibb Pharmaceuticals Research Institute
Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 1037-44 (2003)
Schering-Plough Research Institute
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1273-6 (2003)
F. Hoffmann-La Roche
2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1257-65 (2003)
Massachusetts General Hospital
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1229-41 (2003)
Universit£
High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1220-8 (2003)
Wayne State University
New active series of growth hormone secretagogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1191-203 (2003)
University of Montpellier
Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1165-79 (2003)
Link£Ping University
Use of a pharmacophore model to discover a new class of influenza endonuclease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1153-64 (2003)
Roche Discovery Welwyn
Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1144-52 (2003)
Universidade Federal Do Rio De Janeiro
Virtual screening for submicromolar leads of tRNA-guanine transglycosylase based on a new unexpected binding mode detected by crystal structure analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1133-43 (2003)
Philipps-UniversitäT Marburg
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1127-9 (2003)
Université
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1123-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1120-2 (2003)
Ontogen
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 1116-9 (2003)
Sugen
Synthesis and biological evaluation of non-peptidic cyclophilin ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1112-5 (2003)
Guilford Pharmaceuticals
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1081-111 (2003)
The Feinberg School of Medicine of Northwestern University
Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1215-9 (2003)
National Cancer Institute-Bethesda
Structure-activity relationships of some opiate glycosides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1207-14 (2003)
Ultrafine Ufc
Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1203-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Indanyl piperazines as melatonergic MT2 selective agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1199-202 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1195-8 (2003)
Merck Frosst Centre For Therapeutic Research
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1191-4 (2003)
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1183-6 (2003)
Glaxosmithkline
Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1175-7 (2003)
Purdue University
Benzamide derivatives as blockers of Kv1.3 ion channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1161-4 (2003)
Merck Research Laboratories
Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1157-60 (2003)
Bristol-Myers Squibb
Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1141-5 (2003)
Astrazeneca R&D
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1137-9 (2003)
Pfizer
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1133-6 (2003)
Bristol-Myers Squibb
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1129-32 (2003)
Merck Frosst Centre For Therapeutic Research
Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 1115-8 (2003)
Fujisawa Pharmaceutical
Glycine alpha-ketoamides as HCV NS3 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1111-4 (2003)
Pharmaceutical Research Institute
Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1093-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Alkoxysulfamide, N-hydroxysulfamide, and sulfamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1087-92 (2003)
Seoul National University
Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1071-4 (2003)
Bayer
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1067-70 (2003)
Glaxosmithkline
Identification of a novel series of selective 5-HT7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1055-8 (2003)
Glaxosmithkline
Synthesis and binding affinity of neuropeptide Y at opiate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1029-31 (2003)
University of North Carolina At Wilmington
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1023-8 (2003)
Bristol-Myers Squibb
N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1015-8 (2003)
Genentech
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1005-9 (2003)
Universit£
Syntheses and biological properties of cysteine-reactive epibatidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 1001-4 (2003)
Universit£
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 767-70 (2003)
Bristol-Myers Squibb
Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 761-5 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 753-6 (2003)
Johnson & Johnson Pharmaceutical Research & Development
1,4-dibenzylpiperazines possess anticocaine activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 749-51 (2003)
University of Maryland
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 741-4 (2003)
Merck Frosst Centre For Therapeutic Research
Functional expression and characterization of EryA, the erythritol kinase of Brucella abortus, and enzymatic synthesis of L-erythritol-4-phosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 737-9 (2003)
Brown University
Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 733-5 (2003)
Virginia Commonwealth University
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 729-32 (2003)
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 723-8 (2003)
Millennium Pharmaceuticals
Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 713-7 (2003)
Merck Research Laboratories
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 709-12 (2003)
Schering-Plough Research Institute
Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 705-8 (2003)
Schering-Plough Research Institute
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 701-4 (2003)
Neurogen
Orally efficacious NR2B-selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 697-700 (2003)
Merck Research Laboratories
Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 693-6 (2003)
Merck Sharp & Dohme Research Laboratories
Exploring new non-sugar sulfated molecules as activators of antithrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 679-83 (2003)
Virginia Commonwealth University
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 669-73 (2003)
Sankyo
Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 665-8 (2003)
Glaxosmithkline
Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 657-60 (2003)
Vittal Mallya Scientific Research Foundation
Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 649-52 (2003)
Roche Research Center
Inhibition of inosine monophosphate dehydrogenase (IMPDH) by 2-[2-(Z)-fluorovinyl]inosine 5'-monophosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 645-7 (2003)
The University of Georgia
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 637-40 (2003)
Glaxosmithkline
Identification of a high-affinity phosphopeptide inhibitor of Stat3.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 633-6 (2003)
The University of Texas At Houston
Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 629-32 (2003)
University of New Orleans
Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 609-12 (2003)
Seoul National University
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 605-8 (2003)
Bristol-Myers Squibb
Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 601-4 (2003)
Seoul National University
Pyridazinones as selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 597-600 (2003)
Merck Frosst Centre For Therapeutic Research
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 20: 161-8 (2003)
The University of Kansas
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropsychopharmacology 28: 519-26 (2003)
Case Western Reserve University
Synthesis and pharmacological evaluation of substituted naphth[1,2,3-de]isoquinolines (dinapsoline analogues) as D1 and D2 dopamine receptor ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 11: 1451-64 (2003)
Purdue University
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 1104-15 (2003)
University of Kansas
QSAR and classification of murine and human soluble epoxide hydrolase inhibition by urea-like compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1066-80 (2003)
The Pennsylvania State University
Systematic development of high affinity bis(ammonio)alkane-type allosteric enhancers of muscarinic ligand binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1031-40 (2003)
University of W£Rzburg
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1016-30 (2003)
Abbott Laboratories
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 954-66 (2003)
University of Bologna
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 925-35 (2003)
Emory University
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 921-4 (2003)
Georgetown University Medical Center
Simple, potent, and selective pyrrole inhibitors of monoamine oxidase types A and B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 917-20 (2003)
Sapienza University of Rome
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 913-6 (2003)
Astrazeneca R&D Charnwood
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 883-908 (2003)
The Feinberg School of Medicine of Northwestern University
Modification of the N-terminus of peptidomimetic protein tyrosine phosphatase 1B (PTP1B) inhibitors: identification of analogues with cellular activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 971-5 (2003)
Pharmacia
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 955-9 (2003)
Actelion Pharmaceuticals
Bis-sulfonamides as endothelin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 951-4 (2003)
Actelion Pharmaceuticals
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 931-5 (2003)
Merck Research Laboratories
Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA(20) 3beta-hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 927-30 (2003)
Tunghai University
Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 913-8 (2003)
Kyoto 619-0216
Synthesis of (+),(-)-neamine and their positional isomers as potential antibiotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 901-3 (2003)
Harvard Medical School
Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 895-9 (2003)
National Cancer Institute-Frederick
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 885-90 (2003)
Merck Research Laboratories
Design and synthesis of the tumor-activated prodrug of dihydropyrimidine dehydrogenase (DPD) inhibitor, RO0094889 for combination therapy with capecitabine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 867-72 (2003)
Nippon Roche Research Center
Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 863-5 (2003)
University of Bath
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 851-4 (2003)
Friedrich-Alexander University
Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 841-5 (2003)
Universit£
Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 837-40 (2003)
Universit£
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 829-32 (2003)
F. Hoffmann-La Roche
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 817-20 (2003)
Seoul National University
Dehydrophenylalanine derivatives as VLA-4 integrin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 805-8 (2003)
Celltech R&D
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 799-803 (2003)
Tulane University Health Sciences Center
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 795-8 (2003)
Merck Research Laboratories
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 789-94 (2003)
University of Ljubljana
Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 785-8 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 783-4 (2003)
University of Tennessee Health Science Center
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 4: 181-5 (2003)
University of Queensland Brisbane
Exploring sponge-derived terpenoids for their potency and selectivity against 12-human, 15-human, and 15-soybean lipoxygenases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 230-5 (2003)
University of California Santa Cruz
Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Pharmacol 63: 489-98 (2003)
University of Arizona
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 740-8 (2003)
State University of New York
A tertiary alcohol analog of gamma-hydroxybutyric acid as a specific gamma-hydroxybutyric acid receptor ligand.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 675-9 (2003)
University of Maryland
Prolactin releasing peptide has high affinity and efficacy at neuropeptide FF2 receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 825-32 (2003)
Juvantia Pharma
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 305: 887-96 (2003)
Abbott Laboratories
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 304: 1161-71 (2003)
Merck Research Laboratories
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 876-9 (2003)
Martin-Luther-University Halle-Wittenberg
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 868-71 (2003)
Senju Pharmaceutical
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 856-67 (2003)
Johannes Gutenberg-University of Mainz
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 838-49 (2003)
Rensselaer Polytechnic Institute
Synthesis and flow cytometric evaluation of novel 1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of nitrobenzylmercaptopurine riboside (NBMPR) designed for probing its conformation when bound to the es nucleoside transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 831-7 (2003)
University of Tennessee Health Sciences Center
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 820-30 (2003)
Methylgene
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 810-9 (2003)
University of Arizona
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 768-81 (2003)
Università
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 734-46 (2003)
Uppsala University
Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 716-26 (2003)
University of Innsbruck
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 702-15 (2003)
Dainippon Pharmaceutical
Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 691-701 (2003)
Sumitomo Pharmaceuticals
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 685-90 (2003)
Aventis Pharma
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 681-4 (2003)
Aventis Pharmaceuticals
2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 677-80 (2003)
Harvard University
Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 674-6 (2003)
Enanta Pharmaceuticals
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 670-3 (2003)
Pfizer
Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 666-9 (2003)
Tsukuba Research Institute
Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 10: 15-24 (2003)
Tohoku University
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 646-9 (2003)
Università
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 642-5 (2003)
National Institute On Drug Abuse
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 623-33 (2003)
Glaxosmithkline
Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 601-8 (2003)
Columbia University
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 591-600 (2003)
Duquesne University
Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 584-90 (2003)
University Centre For Pharmacy
Design, synthesis, and biological evaluation of a series of fluoroquinoanthroxazines with contrasting dual mechanisms of action against topoisomerase II and G-quadruplexes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 571-83 (2003)
The University of Arizona
Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 542-57 (2003)
Universit£
Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 486-98 (2003)
Aventis Pharma Deutschland
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 461-73 (2003)
Merck Research Laboratories
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 457-60 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 453-6 (2003)
Merck Research Laboratories
Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Fundam Clin Pharmacol 16: 317-23 (2002)
Shinshu University
Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Anticancer Drugs 14: 175-81 (2003)
Korea Research Institute of Chemical Technology
Condensed aromatic peptide family of microbial metabolites, inhibitors of CD28-CD80 interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 573-5 (2003)
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 567-71 (2003)
Schering-Plough Research Institute
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 561-6 (2003)
Millennium Pharmaceuticals
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 553-6 (2003)
National Institute of Diabetes and Digestive and Kidney Diseases
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 547-51 (2003)
Bristol-Myers Squibb Pri
Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 543-6 (2003)
Bristol-Myers Squibb Pri
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 533-8 (2003)
Bristol-Myers Squibb Pharmaceuticals
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 529-32 (2003)
Southern Research Institute
5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 525-7 (2003)
University of California
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 513-7 (2003)
University of Michigan
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 507-11 (2003)
Berlex Biosciences
Thiophene-based vitronectin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 503-6 (2003)
Shire Biochem
1,4-Diazepane-2-ones as novel inhibitors of LFA-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 499-502 (2003)
Novartis Institute For Biomedical Research
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 479-83 (2003)
Merck Research Laboratories
p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 467-70 (2003)
Merck
Modelling of carbonic anhydrase inhibitory activity of sulfonamides using molecular negentropy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 447-53 (2003)
A.P.S. University
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 443-6 (2003)
Università
Discovery of orally bioavailable NK1 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 437-42 (2003)
Ucb Pharma
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 427-31 (2003)
Merck Research Laboratories
A series of 2(Z)-2-benzylidene-6,7-dihydroxybenzofuran-3[2H]-ones as inhibitors of chorismate synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 423-6 (2003)
Pantherix
2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 413-7 (2003)
Amorepacific
SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 405-8 (2003)
Solvay Pharma
Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 387-9 (2003)
The Oxford Centre For Molecular Sciences and The Dyson Perrins Laboratory
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 379-82 (2003)
Pfizer
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 369-73 (2003)
Bristol-Myers Squibb
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 351-4 (2003)
Merck Research Laboratories
Imidazopyrimidines, potent inhibitors of p38 MAP kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 347-50 (2003)
Johnson & Johnson Pharmaceutical Research and Development
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 331-4 (2003)
Leiden University
AF2 interaction with Ascaris suum body wall muscle membranes involves G-protein activation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Biophys Res Commun 301: 456-9 (2003)
Pharmacia
Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 112-4 (2003)
University of California
Chemical and biological investigation of the fungus Pulveroboletus ravenelii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 103-7 (2003)
The University of Mississippi
Flavanone glycosides from Miconia trailii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 66: 39-41 (2003)
University of Mississippi
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 441-4 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 417-26 (2003)
Aristotle University of Thessaloniki
Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 399-408 (2003)
Glaxosmithkline
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 364-73 (2003)
Georgetown University Medical Center
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 353-5 (2003)
Pfizer
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 349-52 (2003)
Merck Research Laboratories
Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 345-8 (2003)
Mrl Rome
5-HT4 receptor ligands: applications and new prospects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 319-44 (2003)
Paris-Sud University
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Protein Sci 12: 349-60 (2003)
Gsk
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 304: 818-26 (2003)
Taisho Pharmaceutical
Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 304: 810-7 (2003)
University of Cologne
Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 304: 610-6 (2003)
Kitasato University
Interaction of cysteine conjugates with human and rabbit organic anion transporter 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 304: 560-6 (2003)
University of Arizona
The specificities of protein kinase inhibitors: an update.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem J 371: 199-204 (2003)
University of Dundee
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 42: 631-8 (2003)
The Johns Hopkins University
Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Cancer Ther 2: 105-12 (2003)
Japanese Foundation For Cancer Research
Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Pharmacol 65: 435-40 (2003)
Aventis Pharma
Prodrugs of purine and pyrimidine analogues for the intestinal di/tri-peptide transporter PepT1: affinity for hPepT1 in Caco-2 cells, drug release in aqueous media and in vitro metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Control Release 86: 279-92 (2003)
The Royal Danish School of Pharmacy
Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem J 371: 361-7 (2003)
The Netherlands Cancer Institute
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 314-7 (2003)
University of Bath
Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 310-3 (2003)
University of Firenze
Discovery of a long-chain carbamoyl aminocarnitine derivative, a reversible carnitine palmitoyltransferase inhibitor with antiketotic and antidiabetic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 303-9 (2003)
Sigma Tau Pharmaceutical Industries
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 265-83 (2003)
H. Lundbeck
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 255-64 (2003)
F. Hoffmann-La Roche
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 244-54 (2003)
National Cancer Institute-Frederick
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 237-43 (2003)
University of Pennsylvania
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 46: 222-36 (2003)
Faculte De Medecine Et De Pharmacie
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 210-3 (2003)
Pfizer
Potential tumor-selective nitroimidazolylmethyluracil prodrug derivatives: inhibitors of the angiogenic enzyme thymidine phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 207-9 (2003)
University of Manchester
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 204-6 (2003)
Merck Research Laboratories
Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 125: 363-73 (2003)
Weizmann Institute of Science
Activity of opioid ligands in cells expressing cloned mu opioid receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
BMC Pharmacol 3: 1 (2003)
Molecular Research Institute
New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 161-8 (2002)
Universit£
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 155-60 (2002)
Industrial Research
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 138-47 (2002)
Université
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 125-37 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 113-24 (2002)
Takeda Chemical Industries
Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 105-12 (2002)
Kissei Pharmaceutical
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 74-86 (2002)
Vrije Universiteit
Hydantoin-substituted 4,6-dichloroindole-2-carboxylic acids as ligands with high affinity for the glycine binding site of the NMDA receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 64-73 (2002)
Johannes Gutenberg-UniversitäT
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 49-63 (2002)
Wyeth Research
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 34-48 (2002)
Universit£
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 9-11 (2002)
Amgen
Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 46: 1-4 (2002)
Universit£
Sodium 1-(12-hydroxy)octadecanyl sulfate, an MMP2 inhibitor, isolated from a tunicate of the family Polyclinidae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1936-8 (2002)
The University of Tokyo
New polyhydroxylated pyrrolidine, piperidine, and pyrrolizidine alkaloids from Scilla sibirica.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1875-81 (2002)
Hokuriku University
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1749-53 (2002)
Université
Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 9: 1323-8 (2002)
Massachusetts Institute of Technology
Synthesis and evaluation of phosphoramidate amino acid-based inhibitors of sialyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 301-4 (2002)
University of Colorado
Design and synthesis of factor Xa inhibitors and their prodrugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 297-300 (2002)
Millennium Pharmaceuticals
CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 289-91 (2003)
Bristol-Myers Squibb
Development of a presynaptic 5-HT1A antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 285-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 277-80 (2002)
Merck Research Laboratories
p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 273-6 (2003)
Merck Research Laboratories
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 269-71 (2003)
Pfizer
Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 261-4 (2002)
Ligand Pharmaceuticals
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 257-60 (2002)
Novo Nordisk
Synthesis of non-competitive inhibitors of sphingomyelinases with significant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 229-36 (2002)
Tokyo University of Pharmacy & Life Science
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 13: 217-22 (2003)
University of Newcastle
Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 209-12 (2002)
Institut Henri Beaufour
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 201-4 (2002)
National Institute of Radiological Sciences
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 175-8 (2002)
University of Santiago
alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 171-3 (2002)
Università
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 165-9 (2002)
Basf
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 161-4 (2002)
Merck Research Laboratories
Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5755-75 (2002)
Novo Nordisk
Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5745-54 (2002)
The Royal Danish School of Pharmacy
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5736-44 (2002)
University of Florida
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5727-35 (2002)
Universit£
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5710-20 (2002)
Università
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5687-93 (2002)
Novartis Pharma
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5671-86 (2002)
Bulgarian Academy of Sciences
Metal-dependent inhibition of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5661-70 (2002)
University of Southern California
In silico and NMR identification of inhibitors of the IGF-I and IGF-binding protein-5 interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5655-60 (2002)
Institute For Biochemistry
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5640-8 (2002)
Merck Research Laboratories
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5628-39 (2002)
Abbott Laboratories
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5617-9 (2002)
University of Maryland
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5609-16 (2002)
Merck Research Laboratories
Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochemistry 41: 14916-14924 (2002)
Ucla and The Wadsworth Veterans Administration Hospital
Urate transport via human PAH transporter hOAT1 and its gene structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kidney Int 63: 143-55 (2003)
Jikei University School of Medicine
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 139-41 (2002)
Currently Naeja Pharmaceutical
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 133-7 (2002)
Roche Research Center
Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 129-31 (2003)
Bristol-Myers Squibb
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 125-8 (2003)
Bristol-Myers Squibb
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 119-23 (2002)
Merck Research Laboratories
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 111-3 (2002)
Banyu Tsukuba Research Institute
Design of novel N-(2,4-dioxo-1,2,3,4-tetrahydro-thieno[3,2-d]pyrimidin-7-yl)-guanidines as thymidine phosphorylase inhibitors, and flexible docking to a homology model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 107-10 (2002)
Attenuon
N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 97-100 (2002)
Chinese Academy of Sciences
Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 93-6 (2002)
Kyoto Pharmaceutical University
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 87-91 (2003)
Nippon Roche Research Center
Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 83-6 (2002)
The University of Tokyo
Rational approaches towards reversible inhibition of type B monoamine oxidase. Design and evaluation of a novel 5H-Indeno[1,2-c]pyridazin-5-one derivative.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 69-73 (2002)
FacultéS Universitaires Notre-Dame De La Paix
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 61-4 (2003)
Meiji Seika Kaisha
Homologues and isomers of noladin ether, a putative novel endocannabinoid: interaction with rat cannabinoid CB(1) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 43-6 (2002)
Discaff
Synthesis and gamma-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 37-41 (2002)
Merck Sharp & Dohme Research Laboratories
Identification of a stable chymase inhibitor using a pharmacophore-Based database search.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 13: 25-9 (2002)
Toa Eiyo
Hybrid ubiquinone: novel inhibitor of mitochondrial complex I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochim Biophys Acta 1556: 106-12 (2002)
Kyoto University
Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5576-93 (2002)
University of California
Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5564-75 (2002)
Dainippon Pharmaceutical
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5556-63 (2002)
University of Cagliari
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5506-13 (2002)
National Institute of Environmental Health Sciences
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5492-505 (2002)
Glaxosmithkline
Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5471-82 (2002)
Boehringer Ingelheim Pharmaceuticals
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5430-9 (2002)
Uppsala University
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5415-8 (2002)
Schering-Plough Research Institute
Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1715-8 (2002)
University of Puerto Rico
Aldehyde dehydrogenase inhibitors from the mushroom Clitocybe clavipes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1712-4 (2002)
Shizuoka University
Triterpenoid constituents isolated from the bark of Abies sachalinensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1657-9 (2002)
Osaka University of Pharmaceutical Sciences
Antioxidant and free-radical scavenging activity of constituents of the leaves of Tachigalia paniculata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1526-9 (2002)
Università
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1517-21 (2002)
Uppsala University
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3635-9 (2002)
Agouron Pharmaceuticals
Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3629-33 (2002)
Sapienza University of Rome
Silanediol-based inhibitor of thermolysin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3625-7 (2002)
State University of New York
Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3611-3 (2002)
Institutet
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3601-4 (2002)
Université
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3595-9 (2002)
British Biotech Pharmaceuticals
Novel 1',1'-chain substituted Delta(8)-tetrahydrocannabinols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3583-6 (2002)
National Hellenic Research Foundation
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3573-7 (2002)
Janssen-Cilag
Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3565-7 (2002)
Biovitrum
Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3551-5 (2002)
University of Bari
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 3537-41 (2002)
Merck Research Laboratories
SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 1171-9 (2002)
Sanofi-SynthÉLabo Recherche
Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 1052-60 (2002)
Merck Sharp and Dohme Research Laboratories
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 1044-51 (2002)
Merck Research Laboratories
The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 303: 959-68 (2002)
University of Manitoba
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Neuropsychopharmacology 27: 699-711 (2002)
Eli Lilly
Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5410-3 (2002)
Università
Adenosine 5'-O-(1-boranotriphosphate) derivatives as novel P2Y(1) receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5384-96 (2002)
Bar-Ilan University
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5378-83 (2002)
University of Innsbruck
Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5358-64 (2002)
Free University of Berlin
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5353-7 (2002)
Universit£
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5321-9 (2002)
National Research Council of Canada
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5303-10 (2002)
Johnson & Johnson Pharmaceutical Research & Development
Sulfamide-based inhibitors for carboxypeptidase A. Novel type transition state analogue inhibitors for zinc proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5295-302 (2002)
Pohang University of Science and Technology
Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5287-94 (2002)
University of Arizona
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5280-6 (2002)
Purdue Pharma
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 5260-79 (2002)
Teva Pharmaceutical Industries
Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5249-59 (2002)
Chinese Academy of Sciences
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 5233-48 (2002)
Bristol-Myers Squibb
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 5224-32 (2002)
Bristol-Myers Squibb
Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 278: 1831-6 (2003)
University of Padova
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3491-5 (2002)
Neurocrine Biosciences
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3487-90 (2002)
Wyeth Research
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3483-6 (2002)
Merck Research Laboratories
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3479-82 (2002)
Schering-Plough Research Institute
Synthesis of [difluoro-(3-alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP1B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3471-4 (2002)
University of Waterloo
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3467-70 (2002)
Agouron Pharmaceuticals
Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3453-7 (2002)
University of Florida
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3449-52 (2002)
Glaxosmithkline
Trifluoromethyl ketones as inhibitors of histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3443-7 (2002)
Abbott Laboratories
Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 3431-3 (2002)
Glaxosmithkline
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3421-4 (2002)
Bayer Research Center
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3417-9 (2002)
Currently Naeja Pharmaceutical
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3413-5 (2002)
Currently Naeja Pharmaceutical
Natural PTP1B inhibitors from Broussonetia papyrifera.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3387-90 (2002)
Chinese Academy of Sciences
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3383-6 (2002)
Pharmacia
Chemical modification of reveromycin A and its biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3363-6 (2002)
Riken (The Institute of Physical and Chemical Research)
Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3359-62 (2002)
Glaxosmithkline
Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5182-5 (2002)
Université
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5173-81 (2002)
Duquesne University
Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5150-6 (2002)
Forschungszentrum JüLich
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5136-49 (2002)
University of LièGe
Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5081-9 (2002)
Daiichi Fine Chemical
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5043-51 (2002)
Neurogen
Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 5030-6 (2002)
Università
Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 5005-22 (2002)
Sunesis Pharmaceuticals
Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4995-5004 (2002)
Universidade Federal Do Rio De Janeiro
Synthesis, solution structure, and biological evaluation of urokinase type plasminogen activator (uPA)-derived receptor binding domain mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4984-94 (2002)
Technische UniversitäT MüNchen
Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4975-83 (2002)
The University of Liverpool
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4961-74 (2002)
Pfizer
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4954-7 (2002)
Bristol-Myers Squibb
Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4950-3 (2002)
Acadia Pharmaceuticals
The human bile salt export pump: characterization of substrate specificity and identification of inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Gastroenterology 123: 1649-58 (2002)
King'S College Hospital
Crystal structures of Candida albicans N-myristoyltransferase with two distinct inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 9: 1119-28 (2002)
Nippon Roche Research Center
Panepophenanthrin, from a mushroom strain, a novel inhibitor of the ubiquitin-activating enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1491-3 (2002)
Institute of Microbial Chemistry
Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1479-85 (2002)
University of Bonn
Constituents of the stigmas of Crocus sativus and their tyrosinase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1452-6 (2002)
National Cheng Kung University
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3341-4 (2002)
Glaxosmithkline
3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: a potent and highly selective inducible nitric oxide synthase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3337-9 (2002)
Pharmacia
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3329-32 (2002)
Merck Research Laboratories
Capped dipeptide alpha-ketoacid inhibitors of the HCV NS3 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3325-8 (2002)
Irbm, Mrl Rome
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3317-20 (2002)
Merck Frosst Centre For Therapeutic Research
Novel human histamine H(3) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3309-12 (2002)
Johnson and Johnson Pharmaceutical Research and Development
The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3305-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3291-6 (2002)
Institut De Recherches Servier
Identification of novel inhibitors of fibroblast growth factor (FGF-2) binding to heparin and endothelial cell survival from a structurally diverse carbohybrid library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3287-90 (2002)
University College Dublin
Synthesis and biological activity of olomoucine II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3283-6 (2002)
Palack£
Discovery and biological characterization of capromorelin analogues with extended half-lives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3279-82 (2002)
Pfizer
Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3271-3 (2002)
Kyorin Pharmaceutical
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 791-804 (2002)
Institut De Recherches Servier
Elucidation of the vasoactive intestinal peptide pharmacophore for VPAC(2) receptors in human and rat and comparison to the pharmacophore for VPAC(1) receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 445-60 (2002)
Nih
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4923-30 (2002)
Pharmazeutisches Institut Der Universit£T Freiburg
Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4913-22 (2002)
Eisai
Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4875-87 (2002)
Universit£
Computer-aided design of selective COX-2 inhibitors: comparative molecular field analysis, comparative molecular similarity indices analysis, and docking studies of some 1,2-diarylimidazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4847-57 (2002)
University of Hyderabad
Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4838-46 (2002)
University of Catania
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4816-27 (2002)
Chinese Academy of Sciences
Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4806-15 (2002)
Universidad Complutense
Synthesis of potent and highly selective inhibitors of human tryptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3235-8 (2002)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3229-33 (2002)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3219-22 (2002)
Glaxosmithkline
Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3203-5 (2002)
Schering-Plough Research Institute
P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3199-202 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3195-8 (2002)
Ucb Pharma
Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3191-3 (2002)
Daiichi Pharmaceutical
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3187-90 (2002)
Bayer
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3183-6 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
New irreversible adenosine A(1) antagonists based on FSCPX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3179-82 (2002)
Monash University (Parkville Campus)
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3175-8 (2002)
Institute For Molecular Studies
A mechanism-based probe for gp120-Hydrolyzing antibodies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3167-70 (2002)
University of Texas-Houston Medical School
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3161-5 (2002)
Schering-Plough Research Institute
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3157-60 (2002)
Schering-Plough Research Institute
Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3153-6 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3149-52 (2002)
Schering-Plough Research Institute
Synthesis and biological activity of retinoic acid receptor-alpha specific amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3145-8 (2002)
Allergan
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3141-3 (2002)
Shire Biochem
Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3129-33 (2002)
Celera
A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3125-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3111-5 (2002)
Neurogen
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3105-9 (2002)
Neurogen
Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3097-9 (2002)
Egis Pharmaceuticals
Hydroxamate based inhibitors of adenylyl cyclase. Part 2: the effect of cyclic linkers on P-site binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3089-92 (2002)
Millennium Pharmaceuticals
Hydroxamate based inhibitors of adenylyl cyclase. Part 1: the effect of acyclic linkers on P-site binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3085-8 (2002)
Millennium Pharmaceuticals
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3081-4 (2002)
Johnson and Johnson Pharmaceutical Research and Development
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3077-9 (2002)
Abbott Laboratories
Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3073-6 (2002)
F. Hoffmann-La Roche
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3067-71 (2002)
University of Kentucky
Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3059-62 (2002)
Novartis Institute For Biomedical Research
Synthesis and evaluation of potent pyrrolidine H(3) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3055-8 (2002)
Abbott Laboratories
alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3047-50 (2002)
The Ohio State University
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3041-5 (2002)
Tsukuba Research Institute
Solvent and guest isotope effects on complexation thermodynamics of alpha-, beta-, and 6-amino-6-deoxy-beta-cyclodextrins.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 124: 12361-71 (2002)
Japan Science and Technology Agency
2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Enzyme Inhib Med Chem 17: 45-8 (2002)
University of Porto-Rua Anibal Cunha
Synthesis and structure-activity relationship of the isoindolinyl benzisoxazolpiperidines as potent, selective, and orally active human dopamine D4 receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 3: 999-1009 (2002)
Aventis Pharmaceuticals
Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4794-8 (2002)
Université
Synthesis and investigation of conformationally restricted analogues of lavendustin A as cytotoxic inhibitors of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4774-85 (2002)
Purdue University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4755-61 (2002)
Research Triangle Institute
The effect of exchanging various substituents at the 2-position of 2-methoxyestradiol on cytotoxicity in human cancer cell cultures and inhibition of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4748-54 (2002)
Purdue University
Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4737-47 (2002)
Salk Institute
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4724-31 (2002)
Universita Di Camerino
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4716-23 (2002)
University of Pennsylvania
Imidazole inhibitors of cytokine release: probing substituents in the 2 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4695-705 (2002)
Eberhard-Karls-University TüBingen
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4669-78 (2002)
Bristol-Myers Squibb
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4655-68 (2002)
Universit£
Cyclosporins: structure-activity relationships for the inhibition of the human FPR1 formylpeptide receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4613-28 (2002)
Strasbourg 1 University
Cyclosporins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4598-612 (2002)
Strasbourg 1 University
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4594-7 (2002)
Friedrich-Alexander University
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4589-93 (2002)
Merck
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Am Chem Soc 124: 11852-3 (2002)
Millennium Pharmaceuticals
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3009-13 (2002)
Merck Frosst Centre For Therapeutic Research
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 3001-4 (2002)
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2997-3000 (2002)
Merck Research Laboratories
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2993-6 (2002)
University of California
Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2989-92 (2002)
Wyeth Research
Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2977-80 (2002)
Glaxosmithkline
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2973-5 (2002)
Idun Pharmaceuticals
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2969-71 (2002)
Idun Pharmaceuticals
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2963-7 (2002)
Wyeth Research
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2957-61 (2002)
Wyeth Research
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2935-9 (2002)
Cv Therapeutics
Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2931-4 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2925-30 (2002)
Corvas International
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2919-23 (2002)
Abbott Laboratories
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2913-7 (2002)
Genentech
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2907-11 (2002)
Universit£
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2893-7 (2002)
Wyeth Research
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2887-91 (2002)
Celera
Albumin affinity tags increase peptide half-life in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2883-6 (2002)
Genentech
Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2879-82 (2002)
Bristol-Myers Squibb Pri
Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2875-8 (2002)
Bayer Research Center
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2871-3 (2002)
Kyorin Pharmaceutical
Benzodiazepine inhibitors of the MMPs and TACE.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2867-70 (2002)
Wyeth Research
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2859-61 (2002)
Upres Ea 1085
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2855-8 (2002)
Merck Research Laboratories
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2829-31 (2002)
Cephalon
Development of potent and selective dipeptidyl peptidase II inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2825-8 (2002)
University of Antwerp (Uia)
Convenient synthesis and evaluation of enzyme inhibitory activity of several N-alkyl-, N-phenylalkyl, and cyclic isourea derivatives of 5a-carba-alpha-DL-fucopyranosylamine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2811-4 (2002)
Keio University
Structural basis for Chk1 inhibition by UCN-01.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 277: 46609-15 (2002)
Glaxosmithkline
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 19: 1244-7 (2002)
University of California
Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4581-4 (2002)
University of Kuopio
Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4571-80 (2002)
Takeda Chemical Industries
4-Substituted D-glutamic acid analogues: the first potent inhibitors of glutamate racemase (MurI) enzyme with antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4559-70 (2002)
Eli Lilly
Inactivation and inhibition of gamma-aminobutyric acid aminotransferase by conformationally restricted vigabatrin analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4531-9 (2002)
Northwestern University
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4513-23 (2002)
Kyowa Hakko Kogyo
Enhancement of nucleoside cytotoxicity through nucleotide prodrugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4505-12 (2002)
Southern Research Institute
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4471-84 (2002)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4443-59 (2002)
Novo Nordisk
Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4419-32 (2002)
Research and Development
A sorbitol dehydrogenase inhibitor of exceptional in vivo potency with a long duration of action: 1-(R)-[4-[4-(4,6-dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl]ethanol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4398-401 (2002)
Pfizer
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4395-7 (2002)
Abbott Laboratories
A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4391-4 (2002)
University of Naples Federico Ii
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4383-6 (2002)
Eli Lilly
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4379-82 (2002)
Women'S Health Research Institute
High affinity antagonists of the vanilloid receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Mol Pharmacol 62: 947-56 (2002)
National Cancer Institute-Bethesda
Identification of a mechanism by which the methylmercury antidotes N-acetylcysteine and dimercaptopropanesulfonate enhance urinary metal excretion: transport by the renal organic anion transporter-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mol Pharmacol 62: 921-6 (2002)
University of Rochester School of Medicine
Interaction of cytochrome P450 3A inhibitors with P-glycoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 303: 323-32 (2002)
St. Jude Children'S Research Hospital
Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 303: 308-13 (2002)
Avmax
Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 303: 29-35 (2002)
University of Arkansas
[Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine].![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Encephale 28: 350-5 (2002)
Emory University
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
FASEB J 16: 1829-31 (2002)
Chul
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2781-4 (2002)
National Institutes of Health
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2767-70 (2002)
Merck Research Laboratories
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2761-5 (2002)
Wyeth-Ayerst Research
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2753-6 (2002)
University of Alberta
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2719-22 (2002)
Merck Sharp & Dohme Research Laboratories
Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2711-4 (2002)
Mogam Biotechnology Research Institute
Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 2: substitution of the glycine part.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2703-5 (2002)
University of Antwerp (Uia)
Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2695-8 (2002)
Ghent University
Analogue based design of MMP-13 (Collagenase-3) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2689-93 (2002)
Gvk Biosciences
Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2667-72 (2002)
Universita Degli Studi Di Firenze
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4371-4 (2002)
Niddk
Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4359-70 (2002)
Duke University
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4344-9 (2002)
Purdue University
2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4310-20 (2002)
Novartis Research Institute Vienna
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4276-81 (2002)
Universita' Degli Studi Di Siena
N-[(2-Sulfo)-9-fluorenylmethoxycarbonyl](3)-gentamicin C(1) is a long-acting prodrug derivative.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4264-70 (2002)
Institute of Science
Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4254-63 (2002)
Instituto De Qu£Mica M£Dica (Csic)
Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4240-5 (2002)
The Royal Danish School of Pharmacy
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4222-39 (2002)
Takeda Chemical Industries
Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4212-21 (2002)
Takeda Chemical Industries
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4202-11 (2002)
University of Gda£?Sk
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4171-87 (2002)
Novo Nordisk Research and Development
DrugScore meets CoMFA: adaptation of fields for molecular comparison (AFMoC) or how to tailor knowledge-based pair-potentials to a particular protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4153-70 (2002)
Philipps-Universit£T Marburg
Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4128-39 (2002)
Universidad De Navarra
Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4119-27 (2002)
National Institute On Drug Abuse-Intramural Research Program/Nih
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4110-8 (2002)
Drew University
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4097-109 (2002)
Drew University
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4094-6 (2002)
Johnson & Johnson Pharmaceutical Research & Development
Purine and pyrimidine (P2) receptors as drug targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4057-93 (2002)
National Institute of Diabetes
Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 3: 897-901 (2002)
New York University
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 450: 191-202 (2002)
Schering-Plough Research Institute
A quick diversity-oriented amide-forming reaction to optimize P-subsite residues of HIV protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 9: 891-6 (2002)
The Scripps Research Institute
X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 41: 10810-8 (2002)
Weizmann Institute of Science
New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Prunus mume.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1151-5 (2002)
Kyoto Pharmaceutical University
Naturally occurring cembranes from an Australian sarcophyton species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1147-50 (2002)
Astrazeneca R&D Griffith University
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Proc Natl Acad Sci U S A 99: 11934-9 (2002)
Case Western Reserve University
Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4047-54 (2002)
Vienna University of Technology
Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4038-46 (2002)
Columbia University
Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4029-37 (2002)
Research Triangle Institute
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 4000-10 (2002)
Freie Universit£T Berlin
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3972-83 (2002)
Astrazeneca Pharmaceuticals
Divalent and trivalent alpha-ketocarboxylic acids as inhibitors of protein tyrosine phosphatases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3946-52 (2002)
Brown University
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3934-45 (2002)
Instituto De Qu£Mica M£Dica (Csic)
Synthesis and evaluation of Glypsi(PO(2)R-N)Pro-containing pseudopeptides as novel inhibitors of the human cyclophilin hCyp-18.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3928-33 (2002)
Departement D'Ingenierie Et D'Etudes Des Proteines
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3905-27 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3891-904 (2002)
Pharmacia
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3878-90 (2002)
Gsk
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3865-77 (2002)
Pfizer
Exploring the role of bromine at C(10) of (+)-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- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3854-64 (2002)
Schering-Plough Research Institute
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3844-53 (2002)
University of Bologna
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3829-35 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3820-3 (2002)
University of Maryland
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3813-5 (2002)
Biovitrum
Effects of pyridine ring substitutions on affinity, efficacy, and subtype selectivity of neuronal nicotinic receptor agonist epibatidine.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 1246-52 (2002)
University of Miami
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2643-6 (2002)
The Schering Plough Research Institute
Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2607-9 (2002)
Universidade De Vigo
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2603-6 (2002)
Glaxosmithkline
8-Aryl xanthines potent inhibitors of phosphodiesterase 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2587-90 (2002)
Novartis Horsham Research Centre
Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2583-6 (2002)
Merck Frosst Centre For Therapeutic Research
Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2569-72 (2002)
Organon Laboratories
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2565-8 (2002)
Organon Laboratories
Dihydroquinolines as novel n-NOS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2561-4 (2002)
Schering
Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2553-6 (2002)
University of Antwerp (Uia)
Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles: new selective ligands of the 5-HT(7) receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2549-52 (2002)
Meiji Seika Kaisha
Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2545-8 (2002)
Atherogenics
A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2535-9 (2002)
Universit£
Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2519-22 (2002)
F. Hoffmann-La Roche
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2515-8 (2002)
Merck Sharp and Dohme Research Laboratories
Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2501-5 (2002)
University of Nottingham
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Eur J Pharmacol 450: 37-41 (2002)
Aventis Pharmaceuticals
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Biophys Res Commun 296: 644-50 (2002)
Kyushu University
Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3809-12 (2002)
University of Bonn
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3805-8 (2002)
Otsuka Pharmaceutical
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3794-804 (2002)
Bristol-Myers Squibb
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3772-93 (2002)
Millennium Pharmaceuticals
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3755-64 (2002)
Boehringer Ingelheim Pharma
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3746-54 (2002)
University of California
N-Acylvanillamides: development of an expeditious synthesis and discovery of new acyl templates for powerful activation of the vanilloid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3739-45 (2002)
Istituto Per La Chimica Di Molecole Di Interesse Biologico
Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3709-20 (2002)
Utrecht University
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3703-8 (2002)
Nutrition Research Institute
The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3692-702 (2002)
The Institute of Cancer Research
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3684-91 (2002)
National Institutes of Health
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3660-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3649-59 (2002)
Kennesaw State University
Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3639-48 (2002)
Abbott Laboratories
Alpha(1)-adrenoceptor antagonists. 4. Pharmacophore-based design, synthesis, and biological evaluation of new imidazo-, benzimidazo-, and indoloarylpiperazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3603-11 (2002)
Università
Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3588-602 (2002)
University of Marburg
Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: role of hydrogen-bonding networks in ligand binding and drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3583-7 (2002)
Universit£
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3579-82 (2002)
TBA
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3569-72 (2002)
TBA
Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2487-90 (2002)
National Institute of Diabetes and Digestive and Kidney Diseases
N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2479-82 (2002)
Hoffmann-La Roche
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2475-8 (2002)
Roche Research Center
Investigation of the PDZ domain ligand binding site using chemically modified peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2471-4 (2002)
University of California
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2463-5 (2002)
Merck Research Laboratories
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2451-4 (2002)
Nps Pharmaceuticals
An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2447-50 (2002)
The Ohio State University
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2443-6 (2002)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2423-6 (2002)
Merck Research Laboratories
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2419-22 (2002)
Merck Research Laboratories
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2407-10 (2002)
Roche Research Center
C-3 Amido-indole cannabinoid receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2399-402 (2002)
Bristol-Myers Squibb
Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2391-4 (2002)
Kingston University
Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2387-90 (2002)
University of New Orleans
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2377-80 (2002)
Friedrich-Alexander University
Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2367-70 (2002)
Xenova
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2355-8 (2002)
Schering-Plough Research Institute
Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2349-53 (2002)
Minase Research Institute
Synthesis of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: new leads as selective beta-galactosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2335-9 (2002)
Universidad De Sevilla
A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2313-6 (2002)
Korea Institute of Science & Technology
Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2291-4 (2002)
Fukui Research Institute
3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2287-90 (2002)
Chinese Academy of Sciences
3D-QSAR studies on 4-hydroxyphenylpyruvate dioxygenase inhibitors by comparative molecular field analysis (CoMFA).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2271-5 (2002)
Zhejiang University
L-Cysteine based N-type calcium channel blockers: structure-activity relationships of the C-terminal lipophilic moiety, and oral analgesic efficacy in rat pain models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2267-9 (2002)
Minase Research Institute
Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2263-6 (2002)
Universita' Di Firenze
Sequencing, modeling, and selective inhibition of Trypanosoma brucei hexokinase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 9: 839-47 (2002)
Universite Paul Sabatier
Agonodepsides a and B: two new depsides from a filamentous fungus F7524.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1037-8 (2002)
Institute of Molecular and Cell Biology
Bioactive abietane and seco-abietane diterpenoids from Salvia prionitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 1016-20 (2002)
Chinese Academy of Sciences
Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3558-68 (2002)
Guilford Pharmaceuticals
Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3549-57 (2002)
Guilford Pharmaceuticals
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3524-30 (2002)
Research Triangle Institute
Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3509-23 (2002)
Astrazeneca
Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3482-90 (2002)
Pfizer
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3451-7 (2002)
Genentech
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3440-50 (2002)
University of Bonn
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3418-29 (2002)
Menarini Ricerche
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3406-17 (2002)
Saarland University
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3394-405 (2002)
Boehringer Ingelheim Pharmaceuticals
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3381-93 (2002)
University of Newcastle
(4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines: ligands for the estrogen receptor with a novel binding mode.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3356-65 (2002)
Free University of Berlin
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3337-44 (2002)
Instituto De QuíMica MéDica (Csic)
Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 19: 773-9 (2002)
The University of Kansas
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharm Res 19: 765-72 (2002)
The University of Kansas
SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 731-41 (2002)
Sanofi-Synthelabo Recherche
Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 687-95 (2002)
University of Kentucky
Characterization of methotrexate transport and its drug interactions with human organic anion transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 302: 666-71 (2002)
Kyorin University
Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 302: 645-50 (2002)
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Pharm Sci 16: 159-65 (2002)
Kyoto Pharmaceutical University
Binding modes of two novel dinucleotide inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2233-6 (2002)
The University of Iowa
Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2225-8 (2002)
Southern Research Institute
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2205-8 (2002)
Merck Research Laboratories
Design and synthesis of novel inhibitors of gelatinase B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2201-4 (2002)
University of California
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2197-200 (2002)
Merck Research Laboratories
Phosphonate and phosphinate analogues of N-acylated gamma-glutamylglutamate. potent inhibitors of glutamate carboxypeptidase II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2189-92 (2002)
Guilford Pharmaceuticals
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2185-7 (2002)
Neurocrine Biosciences
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2179-83 (2002)
Neurocrine Biosciences
Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185(erbB)) tyrosine kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2153-7 (2002)
Sugen
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2145-8 (2002)
Johnson & Johnson Pharmaceutical Research and Development
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2141-4 (2002)
Merck Research Laboratories
Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2137-40 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2133-6 (2002)
Neurogen
Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2125-8 (2002)
The Schering Plough Research Institute
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2121-3 (2002)
Abbott Laboratories
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2113-6 (2002)
Abbott
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2109-12 (2002)
Novartis Pharma
4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2093-5 (2002)
Novartis Research Institute Vienna
Essential structural factors of acetogenins, potent inhibitors of mitochondrial complex I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2089-92 (2002)
Kyoto University
A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2073-7 (2002)
Takeda Chemical Industries
Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2065-8 (2002)
Novartis Pharma
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2043-6 (2002)
Millennium Pharmaceuticals
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2035-7 (2002)
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2031-4 (2002)
Abbott Laboratories
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2027-30 (2002)
Merck Research Laboratories
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2023-6 (2002)
Celera
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2019-22 (2002)
Celera
Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 2011-4 (2002)
Wyeth Research
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 2001-5 (2002)
University of Paris
Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1997-9 (2002)
Purdue University
Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 1993-6 (2002)
University of Illinois At Chicago
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1967-71 (2002)
Wyeth Research
The synthesis and effect of fluorinated chalcone derivatives on nitric oxide production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1951-4 (2002)
Universidad De Valencia
Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1941-6 (2002)
Korea Research Institute of Chemical Technology
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1937-40 (2002)
Friedrich-Alexander University
Synthesis and anti-influenza virus activity of 7-O-alkylated derivatives related to zanamivir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1925-8 (2002)
Sankyo
Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1921-4 (2002)
Sankyo
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1909-12 (2002)
Ghent University
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Psychopharmacology (Berl) 162: 193-202 (2002)
WestfÄLische Wilhelms-UniversitÄ
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Br J Pharmacol 136: 829-36 (2002)
University of Bonn
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3321-4 (2002)
University of The Mediterranean
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3310-20 (2002)
University of California
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3296-309 (2002)
WestfäLische Wilhelms-UniversitäT MüNster
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3286-95 (2002)
University of Bologna
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3280-5 (2002)
University Center For Pharmacy
N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3271-9 (2002)
Universit£
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 3246-56 (2002)
Glaxosmithkline
Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3235-45 (2002)
University of Bath
Structure-based approach for binding site identification on AmpC beta-lactamase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3222-34 (2002)
Northwestern University
4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3210-21 (2002)
University of Chicago Medical Center
Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3184-94 (2002)
National Cancer Institute/Nih
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3171-83 (2002)
Parc Club Orsay Universit£
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3161-70 (2002)
Georgetown University Medical Center
Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochem Pharmacol 64: 151-8 (2002)
Deutsches Krebsforschungszentrum
Amplification of the effects of drug resistance mutations by background polymorphisms in HIV-1 protease from African subtypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 41: 8613-9 (2002)
The Johns Hopkins University
Molecular identification of a novel carnitine transporter specific to human testis. Insights into the mechanism of carnitine recognition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Biol Chem 277: 36262-71 (2002)
Kyorin University
Callyspongynic acid, a polyacetylenic acid which inhibits alpha-glucosidase, from the marine sponge Callyspongia truncata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 65: 922-4 (2002)
The University of Tokyo
Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3143-60 (2002)
Schering-Plough Research Institute
Potent, novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3112-29 (2002)
Chiron
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3094-102 (2002)
Pfizer
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3073-81 (2002)
University of Florida
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3057-66 (2002)
Pharmaceutical Research Institute
Modification of the structure of a metallopeptide: synthesis and biological evaluation of (111)In-labeled DOTA-conjugated rhenium-cyclized alpha-MSH analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3048-56 (2002)
University of Missouri-Columbia
Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3041-7 (2002)
University of New Orleans
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3022-31 (2002)
University of Groningen
Novel, non-acylguanidine-type Na(+)/H(+) exchanger inhibitors: synthesis and pharmacology of 5-tetrahydroquinolinylidene aminoguanidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 3009-21 (2002)
Takeda Chemical Industries
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2994-3008 (2002)
Boehringer Ingelheim Pharmaceuticals
Identification of potent and novel alpha4beta1 antagonists using in silico screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2988-93 (2002)
Biogen
Structural requirements for inhibition of the neuronal nitric oxide synthase (NOS-I): 3D-QSAR analysis of 4-oxo- and 4-amino-pteridine-based inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2923-41 (2002)
Aventis Pharma
Principles governing the binding of a class of non-peptidic inhibitors to the SH2 domain of src studied by X-ray analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2915-22 (2002)
Aventis Pharma
Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2887-90 (2002)
University of Minnesota
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hepatology 36: 164-72 (2002)
University Hospital
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1785-9 (2002)
Bristol-Myers Squibb
Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1775-8 (2002)
University of Michigan
High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1771-4 (2002)
Lundbeck Research Usa
Discovery of potent and selective small molecule NPY Y5 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1767-9 (2002)
Lundbeck Research Usa
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1763-6 (2002)
University College Dublin
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1759-62 (2002)
Merck Sharp & Dohme Research Laboratories
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1755-8 (2002)
Merck Sharp & Dohme Research Laboratories
Discovery of imidazole glycerol phosphate dehydratase inhibitors through 3-D database searching.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1743-6 (2002)
Monsanto
Synthesis of triazole-Tethered pyrrolidine libraries: novel ECE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1727-30 (2002)
F. Hoffmann-La Roche
Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1719-22 (2002)
Glaxosmithkline
Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1709-13 (2002)
Tunghai University
8-Carboxamidocyclazocine: a long-acting, novel benzomorphan.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 374-80 (2002)
University of Rochester
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 359-68 (2002)
Bayer
A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 328-36 (2002)
University of North Carolina At Chapel Hill
Biochemistry and pharmacology of epitope-tagged alpha(1)-adrenergic receptor subtypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 302: 58-65 (2002)
Emory University
Pharmacological characterization of cloned chicken neuropeptide Y receptors Y1 and Y5.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Neurochem 81: 462-71 (2002)
Uppsala University
Identification of a novel human eicosanoid receptor coupled to G(i/o).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Biol Chem 277: 31459-65 (2002)
Tanabe Seiyaku
Role of human organic anion transporter 4 in the transport of ochratoxin A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biochim Biophys Acta 1590: 64-75 (2002)
Kyorin University
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2877-85 (2002)
Methylgene
Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2841-9 (2002)
National Institute On Drug Abuse
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2832-40 (2002)
University of California
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2801-10 (2002)
University of Florida
Synthesis and structure-affinity-activity relationships of novel benzofuran derivatives as MT(2) melatonin receptor selective ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2788-800 (2002)
Institut De Chimie Pharmaceutique Albert Lespagnol
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2770-80 (2002)
Harvard University
Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 2749-69 (2002)
Aventis Pharma Deutschland
From imidazoles to pyrimidines: new inhibitors of cytokine release.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2733-40 (2002)
Eberhard-Karls-University T£Bingen
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2708-19 (2002)
Research Triangle Institute
Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2695-707 (2002)
University of California San Francisco
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem 10: 2807-16 (2002)
Purdue University
The motilin pharmacophore in CHO cells expressing the human motilin receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochem Biophys Res Commun 293: 1223-7 (2002)
Katholieke Universiteit Leuven
DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 41: 7217-23 (2002)
Umr Cnrs 6032
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 1687-90 (2002)
Abbott Bioresearch Center
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1683-6 (2002)
Abbott Bioresearch Center
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1679-82 (2002)
Roche Research Center
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1671-4 (2002)
Aventis Pharmaceuticals
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1667-70 (2002)
Aventis Pharmaceuticals
Cephalosporin-derived inhibitors of beta-lactamase. Part 4: The C3 substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1663-6 (2002)
Southern Methodist University
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1657-61 (2002)
Millennium Pharmaceuticals
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1651-5 (2002)
Millennium Pharmaceuticals
Synthesis and profile of SCH351591, a novel PDE4 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1621-3 (2002)
Schering-Plough
8-Methoxyquinolines as PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1617-9 (2002)
Schering-Plough
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1613-5 (2002)
Celltech R&D
Exploration of peptidyl hydrazones as water-soluble calpain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1603-6 (2002)
Senju Pharmaceutical
Development of tripeptidyl farnesyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1599-602 (2002)
Department of Chemistry and School of Molecular Science(Bk21)
N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1595-8 (2002)
Celltech R&D
Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1591-4 (2002)
Celltech R&D
Solid-phase synthesis of thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1571-3 (2002)
Basf
2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1563-6 (2002)
University of Virginia
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1559-62 (2002)
Bayer Research Center
Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1551-7 (2002)
Universit£
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2670-3 (2002)
Australian National University
Synthesis and antitumor activity of 1,5,6-substituted E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2666-9 (2002)
Università
Synthesis of (+)-cis-N-(4-isothiocyanatobenzyl)-N-normetazocine, an isothiocyanate derivative of N-benzylnormetazocine as acylant agent for the sigma(1) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2662-5 (2002)
University of Catania
Structure-activity relationship studies of nordihydroguaiaretic acid inhibitors toward soybean, 12-human, and 15-human lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2659-61 (2002)
University of California
Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2651-8 (2002)
Florida International University
Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2644-50 (2002)
University of Arizona
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 2624-43 (2002)
Sphinx Laboratories
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2589-98 (2002)
Yamanouchi Pharmaceutical
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2579-88 (2002)
University of Montpellier
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2571-8 (2002)
Universit£
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2534-42 (2002)
Arizona State University
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2526-33 (2002)
Vrije Universiteit
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2520-5 (2002)
Vrije Universiteit
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2484-93 (2002)
Berlex Biosciences
Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2469-83 (2002)
University of Parma
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2454-68 (2002)
The Royal Danish School of Pharmacy
Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2432-53 (2002)
Pfizer
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2417-24 (2002)
Pfizer
Inhibition of MIF bioactivity by rational design of pharmacological inhibitors of MIF tautomerase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2410-6 (2002)
Institute For Medical Research
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 2388-409 (2002)
Merck Research Laboratories
SAR and X-ray. A new approach combining fragment-based screening and rational drug design: application to the discovery of nanomolar inhibitors of Src SH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2379-87 (2002)
Aventis
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2366-78 (2002)
Aventis Pharma Deutschland
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2362-5 (2002)
TBA
Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2352-4 (2002)
TBA
CoMFA and HQSAR of acylhydrazide cruzain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1537-41 (2002)
Universidade Federal Do Rio De Janeiro
Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Med Chem Lett 12: 1525-8 (2002)
Novo Nordisk
Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1521-3 (2002)
Georgetown University Medical Center
Nicotinanilides as inhibitors of neutrophil chemotaxis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1517-20 (2002)
Celltech R&D
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1511-5 (2002)
Millennium Pharmaceuticals
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1501-5 (2002)
Merck Research Laboratories
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1497-500 (2002)
Merck Research Laboratories
SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1477-80 (2002)
Pfizer
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1457-61 (2002)
Merck Frosst Centre For Therapeutic Research
CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1451-6 (2002)
Celltech R&D
Novel lipoic acid analogues that inhibit nitric oxide synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 12: 1439-42 (2002)
Institute Henri Beaufour
Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 301: 1179-89 (2002)
University of North Carolina At Chapel Hill
Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 301: 1166-78 (2002)
University of North Carolina
Effects of norepinephrine and serotonin transporter inhibitors on hyperactivity induced by neonatal 6-hydroxydopamine lesioning in rats.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Pharmacol Exp Ther 301: 1097-102 (2002)
Harvard University
Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Pharmacol Exp Ther 301: 797-802 (2002)
Nagoya University School of Medicine
Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2342-5 (2002)
Wyeth Research
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2319-24 (2002)
Yale University
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2289-93 (2002)
Preclinical Research Novartis Pharma
Homodimeric tacrine congeners as acetylcholinesterase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 45: 2277-82 (2002)
National Defense Medical Center
Synthesis and in vitro pharmacology of substituted quinoline-2,4-dicarboxylic acids as inhibitors of vesicular glutamate transport.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2260-76 (2002)
The University of Montana
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2229-39 (2002)
Glaxosmithkline Research Laboratories
Mode of action of 4-hydroxyphenylpyruvate dioxygenase inhibition by triketone-type inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2222-8 (2002)
Tunghai University
Molecular docking and high-throughput screening for novel inhibitors of protein tyrosine phosphatase-1B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2213-21 (2002)
Pfizer
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2197-206 (2002)
Meiji Seika Kaisha
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2185-96 (2002)
University of Illinois At Urbana-Champaign
An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2173-84 (2002)
Aventis Pharma
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2160-72 (2002)
Novartis Institute For Medical Sciences
Rational design and evaluation of new lead compound structures for selective betaARK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2150-9 (2002)
Daiichi Pharmaceutical
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2131-8 (2002)
National Institute of Diabetes & Digestive & Kidney Diseases
Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2127-30 (2002)
TBA
Arylamidrazones as novel corticotropin releasing factor receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 45: 2123-6 (2002)
TBA
Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 41: 6383-90 (2002)
Merck Research Laboratories
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)