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Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.EBI
J Med Chem 48: 4596-607 (2005)
Serono Pharmaceutical Research Institute
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.EBI
J Med Chem 48: 4586-95 (2005)
University of Maryland
Adamantyl cannabinoids: a novel class of cannabinergic ligands.EBI
J Med Chem 48: 4576-85 (2005)
Northeastern University
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.EBI
J Med Chem 48: 4547-57 (2005)
Irbm (Merck Research Laboratories Rome)
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.EBI
J Med Chem 48: 4535-46 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and biological evaluation of geminal disulfones as HIV-1 integrase inhibitors.EBI
J Med Chem 48: 4526-34 (2005)
University of California
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.BDB
J Med Chem 48: 4511-25 (2005)
Aventis Pharma
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.EBI
J Med Chem 48: 4507-10 (2005)
Glaxosmithkline
Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.BDB
Neuropsychopharmacology 31: 265-77 (2006)
Case Western Reserve University
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.BDB
Biochemistry 44: 9430-40 (2005)
Merck Research Laboratories
Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters.BDB
Bioorg Med Chem 13: 5240-52 (2005)
National Taiwan University
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.EBI
Bioorg Med Chem Lett 15: 3834-7 (2005)
Zhejiang University
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.EBI
Bioorg Med Chem Lett 15: 3665-9 (2005)
Merck Sharp and Dohme Research Laboratories
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.EBI
Bioorg Med Chem Lett 15: 3925-9 (2005)
Merck
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.EBI
Bioorg Med Chem Lett 15: 3930-3 (2005)
Università
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.EBI
Bioorg Med Chem Lett 15: 3816-20 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.EBI
Bioorg Med Chem Lett 15: 3744-7 (2005)
Harvard Medical School
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.EBI
Bioorg Med Chem Lett 15: 3891-5 (2005)
Glaxosmithkline
Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes.EBI
Bioorg Med Chem Lett 15: 4100-4 (2005)
University of Mysore
Hydrophobicity in the design of P2/P2' tetrahydropyrimidinone HIV protease inhibitors.EBI
Bioorg Med Chem Lett 15: 3767-70 (2005)
Clarkson University
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.EBI
Bioorg Med Chem Lett 15: 3758-62 (2005)
University of Nottingham
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB
Bioorg Med Chem Lett 15: 3881-5 (2005)
Naeja Pharmaceutical
QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools.EBI
Bioorg Med Chem Lett 15: 3737-43 (2005)
Jadavpur University
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.EBI
Bioorg Med Chem Lett 15: 3912-6 (2005)
Merck Research Laboratories
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.EBI
Bioorg Med Chem Lett 15: 4143-50 (2005)
Seoul National University
Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.EBI
Bioorg Med Chem Lett 15: 3778-81 (2005)
Glaxosmithkline
L-arginine analogs as alternate substrates for nitric oxide synthase.EBI
Bioorg Med Chem Lett 15: 3934-41 (2005)
University of California
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.EBI
Bioorg Med Chem Lett 15: 3732-6 (2005)
Graduate School of The Chinese Academy of Sciences
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.EBI
Bioorg Med Chem Lett 15: 3900-7 (2005)
Bayer Healthcare
BCUT descriptors to predicting affinity toward A3 adenosine receptors.EBI
Bioorg Med Chem Lett 15: 3491-5 (2005)
Experimental Sugar Cane Station&Quot;Villa Clara-Cienfuegos&Quot
The molecular basis for coxib inhibition of p38alpha MAP kinase.EBI
Bioorg Med Chem Lett 15: 3506-9 (2005)
Universidade Federal Do Rio De Janeiro (Ufrj)
Interaction of chiral MS-245 analogs at h5-HT6 receptors.EBI
Bioorg Med Chem Lett 15: 3510-3 (2005)
Virginia Commonwealth University
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.BDB
Bioorg Med Chem Lett 15: 3519-23 (2005)
Glaxosmithkline
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 3870-3 (2005)
Pharmaceutical Research Institute
Synthesis of an N-acyl sulfamate analog of luciferyl-AMP: a stable and potent inhibitor of firefly luciferase.EBI
Bioorg Med Chem Lett 15: 3860-4 (2005)
Connecticut College
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.BDB
J Biol Chem 280: 31220-9 (2005)
Chinese Academy of Sciences
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.EBI
Bioorg Med Chem Lett 15: 2986-2989 (2005)
TBA
Efficient synthetic inhibitors of anthrax lethal factor.BDB
Proc Natl Acad Sci U S A 102: 9499-504 (2005)
Burnham Institute For Medical Research
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 4029-32 (2005)
Pharmaceutical Research Institute
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.EBI
Bioorg Med Chem Lett 15: 3540-6 (2005)
Glaxosmithkline
3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists.EBI
Bioorg Med Chem Lett 15: 3555-9 (2005)
Institut Henri Beaufour
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.EBI
Bioorg Med Chem Lett 15: 3568-72 (2005)
University of Virginia
Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1.EBI
Bioorg Med Chem Lett 15: 3514-8 (2005)
Wyeth Research
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.EBI
Bioorg Med Chem Lett 15: 3501-5 (2005)
Merck Research Laboratories
Investigation of glycine alpha-ketoamide HCV NS3 protease inhibitors: effect of carboxylic acid isosteres.EBI
Bioorg Med Chem Lett 15: 3487-90 (2005)
Pharmaceutical Research Institute
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.EBI
Bioorg Med Chem Lett 15: 3696-700 (2005)
Pharmacopeia Drug Discovery
SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.EBI
Bioorg Med Chem Lett 15: 3600-3 (2005)
Wyeth Research
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.EBI
Bioorg Med Chem Lett 15: 3670-4 (2005)
Schering-Plough Research Institute
Dibenzodioxocinones--a new class of CETP inhibitors.EBI
Bioorg Med Chem Lett 15: 3611-4 (2005)
Bayer Healthcare Pharma Research
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.BDB
Bioorg Med Chem Lett 15: 3560-4 (2005)
Glaxosmithkline
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.EBI
Bioorg Med Chem Lett 15: 3604-8 (2005)
Vernalis Research
Features of selective kinase inhibitors.EBI
Chem Biol 12: 621-37 (2005)
University of California San Francisco
Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.EBI
J Nat Prod 68: 947-50 (2005)
University of Mississippi
Constituents of the leaves of Macaranga tanarius.EBI
J Nat Prod 68: 927-30 (2005)
Ramkhamhaeng University
Indole alkaloids and other constituents of Rauwolfia serpentina.EBI
J Nat Prod 68: 848-52 (2005)
Kobe Pharmaceutical University
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.BDB
J Med Chem 48: 4469-73 (2005)
National Taiwan University
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.EBI
J Med Chem 48: 4457-68 (2005)
Merck Research Laboratories
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.BDB
J Med Chem 48: 4444-56 (2005)
University of Bologna
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.BDB
J Med Chem 48: 4420-31 (2005)
Harvard Medical School
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.EBI
J Med Chem 48: 4410-9 (2005)
Martin-Luther-University Halle-Wittenberg
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II.EBI
J Med Chem 48: 4400-9 (2005)
LinköPing University
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.EBI
J Med Chem 48: 4378-88 (2005)
Sapienza University of Rome
Quinic acid derivatives as sialyl Lewis(x)-mimicking selectin inhibitors: design, synthesis, and crystal structure in complex with E-selectin.EBI
J Med Chem 48: 4346-57 (2005)
Wyeth
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.BDB
J Med Chem 48: 4332-45 (2005)
Vernalis (R&D)
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.EBI
J Med Chem 48: 4312-31 (2005)
Domp£
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.EBI
J Med Chem 48: 4254-65 (2005)
Emory University
Functionalized pyrrolidines inhibit alpha-mannosidase activity and growth of human glioblastoma and melanoma cells.EBI
J Med Chem 48: 4237-46 (2005)
Institute of Chemical Sciences and Engineering
Peptoid-peptide hybrids as potent novel melanocortin receptor ligands.EBI
J Med Chem 48: 4224-30 (2005)
Utrecht University
Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.EBI
J Med Chem 48: 4220-3 (2005)
Sapienza University of Rome
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.EBI
J Med Chem 48: 4216-9 (2005)
Universidad Complutense
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.BDB
J Med Chem 48: 4212-5 (2005)
Vernalis (R&D)
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.BDB
J Med Chem 48: 4208-11 (2005)
Johnson & Johnson Pharmaceutical
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.EBI
J Med Chem 48: 4204-7 (2005)
Università
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.EBI
J Med Chem 48: 4200-3 (2005)
Eli Lilly
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.BDB
J Enzyme Inhib Med Chem 20: 135-41 (2005)
Cardiff University
3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3.EBI
Bioorg Med Chem Lett 15: 3344-6 (2005)
Lund University
Rhodanine derivatives as inhibitors of JSP-1.EBI
Bioorg Med Chem Lett 15: 3374-9 (2005)
Ceptyr
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.EBI
Cancer Res 65: 5399-407 (2005)
Cyclacel
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.EBI
Bioorg Med Chem Lett 15: 3407-11 (2005)
Glaxosmithkline
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.EBI
Bioorg Med Chem Lett 15: 3338-43 (2005)
The Institute of Cancer Research
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.EBI
Bioorg Med Chem 13: 4835-41 (2005)
Hoffmann-La Roche
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.EBI
Bioorg Med Chem Lett 15: 3691-5 (2005)
Pharmacopeia Drug Discovery
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.EBI
Bioorg Med Chem Lett 15: 3352-5 (2005)
Merck Frosst Centre For Therapeutic Research
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.EBI
Bioorg Med Chem Lett 15: 3385-8 (2005)
Pfizer
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.BDB
Biochemistry 44: 8643-51 (2005)
Case Western Reserve University
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.BDB
J Pharmacol Exp Ther 315: 109-17 (2005)
Universit&Aagrove
Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.BDB
J Pharmacol Exp Ther 314: 1274-89 (2005)
Wyeth
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.EBI
Bioorg Med Chem Lett 15: 3389-93 (2005)
Seoul National University
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.EBI
Bioorg Med Chem Lett 15: 3430-3 (2005)
Merck Research Laboratories
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.EBI
Bioorg Med Chem Lett 15: 3685-90 (2005)
Neurocrine Biosciences
Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.EBI
Bioorg Med Chem Lett 15: 3446-9 (2005)
F. Hoffmann-La Roche
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.EBI
Bioorg Med Chem Lett 15: 3459-62 (2005)
Astrazeneca
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.EBI
Bioorg Med Chem Lett 15: 3434-8 (2005)
Neurocrine Biosciences
Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).EBI
Bioorg Med Chem Lett 15: 3439-45 (2005)
Neurocrine Biosciences
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.EBI
Bioorg Med Chem Lett 15: 3402-6 (2005)
Glaxosmithkline
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.EBI
Bioorg Med Chem Lett 15: 3347-51 (2005)
Merck Research Laboratories
Identification of aminopiperidine benzamides as MCHr1 antagonists.EBI
Bioorg Med Chem Lett 15: 3412-6 (2005)
Abbott Laboratories
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.BDB
Biochem Biophys Res Commun 333: 194-9 (2005)
National Taiwan University
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.BDB
J Pharmacol Exp Ther 314: 1310-21 (2005)
Vrije Universiteit Amsterdam
Carboxylate bioisosteres of gabapentin.EBI
Bioorg Med Chem Lett 16: 2333-6 (2006)
Pfizer
Rapid computational identification of the targets of protein kinase inhibitors.EBI
J Med Chem 48: 4138-52 (2005)
University of Iowa
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.EBI
J Med Chem 48: 4100-10 (2005)
Neurocrine Biosciences
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.EBI
J Med Chem 48: 4087-99 (2005)
Arizona State University
Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies.EBI
J Med Chem 48: 4061-7 (2005)
University of Alberta
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.EBI
J Med Chem 48: 4049-60 (2005)
Universit£
Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.EBI
J Med Chem 48: 4025-30 (2005)
University of Pennsylvania
New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists.EBI
J Med Chem 48: 4009-24 (2005)
Uppsala University
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.EBI
J Med Chem 48: 3991-4008 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.BDB
J Med Chem 48: 3980-90 (2005)
Abbott Laboratories
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.EBI
J Med Chem 48: 3953-79 (2005)
Wyeth Research
Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform.EBI
J Med Chem 48: 3945-8 (2005)
National Cancer Institute-Frederick
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.EBI
Bioorg Med Chem Lett 15: 3197-200 (2005)
Merck Research Laboratories
Sialyl Lewis(x) analogs based on a quinic acid scaffold as the fucose mimic.EBI
Bioorg Med Chem Lett 15: 3224-8 (2005)
National Chemical Engineering Institute In Paris
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.EBI
Bioorg Med Chem Lett 15: 3229-32 (2005)
Glaxosmithkline
A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor.EBI
Bioorg Med Chem Lett 15: 3193-6 (2005)
Institute of Medical Research
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.EBI
Bioorg Med Chem Lett 15: 3279-83 (2005)
Fujisawa Pharmaceutical
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.EBI
Bioorg Med Chem Lett 15: 3284-7 (2005)
Fujisawa Pharmaceutical
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.EBI
Bioorg Med Chem Lett 15: 3292-5 (2005)
Roche Palo Alto
Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands.EBI
Bioorg Med Chem Lett 15: 3201-2 (2005)
University of Maryland
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.EBI
Bioorg Med Chem Lett 15: 3271-5 (2005)
National Health Research Institutes
6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.EBI
Bioorg Med Chem Lett 15: 3237-40 (2005)
Virginia Commonwealth University
Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.EBI
Bioorg Med Chem Lett 15: 3241-6 (2005)
Semmelweis University
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.EBI
Bioorg Med Chem Lett 15: 3203-6 (2005)
Glaxosmithkline
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.EBI
Bioorg Med Chem Lett 15: 3257-62 (2005)
Peking University
Novel phomactin analogues as PAF receptor ligands.EBI
Bioorg Med Chem Lett 15: 3263-6 (2005)
The University of Nottingham
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.EBI
Bioorg Med Chem Lett 15: 3296-301 (2005)
Merck Research Laboratories
Petrosamine B, an inhibitor of the Helicobacter pylori enzyme aspartyl semialdehyde dehydrogenase from the Australian sponge Oceanapia sp.EBI
J Nat Prod 68: 804-6 (2005)
Griffith University
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.EBI
J Nat Prod 68: 674-7 (2005)
University of Antwerp
Structural bioinformatics-based design of selective, irreversible kinase inhibitors.EBI
Science 308: 1318-21 (2005)
University of California
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.EBI
J Med Chem 48: 3930-4 (2005)
Nitromed
Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo.BDB
J Med Chem 48: 3919-29 (2005)
Glsynthesis
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.BDB
J Med Chem 48: 3891-902 (2005)
Wyeth Research
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.EBI
J Med Chem 48: 3858-73 (2005)
Universit£
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.EBI
J Med Chem 48: 3852-7 (2005)
Research Triangle Institute
Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7,8-hexaazaacenaphthylene as analogues of triEBI
J Med Chem 48: 3840-51 (2005)
University of Michigan
Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.EBI
J Med Chem 48: 3816-22 (2005)
Umr Cnrs 7081
Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors.EBI
J Med Chem 48: 3808-15 (2005)
University of Kuopio
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.EBI
J Med Chem 48: 3776-83 (2005)
Cephalon
Comparison of ligand-based and structure-based 3D-QSAR approaches: a case study on (aryl-)bridged 2-aminobenzonitriles inhibiting HIV-1 reverse transcriptase.EBI
J Med Chem 48: 3756-67 (2005)
University of Perugia
Decoys for docking.EBI
J Med Chem 48: 3714-28 (2005)
University of California San Francisco
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.BDB
J Med Chem 48: 3704-13 (2005)
University of Washington At Seattle
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.EBI
J Med Chem 48: 3696-9 (2005)
Friedrich-Alexander University
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.BDB
J Med Chem 48: 3680-3 (2005)
Chemical Diversity Research Institute
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.EBI
J Med Chem 48: 3663-79 (2005)
National Institute On Drug Abuse-Intramural Research Program
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.EBI
Bioorg Med Chem Lett 15: 3091-5 (2005)
Fujisawa Pharmaceutical
Synthetic lanostane-type triterpenoids as inhibitors of DNA topoisomerase II.EBI
Bioorg Med Chem Lett 15: 2966-9 (2005)
Osaka University of Pharmaceutical Sciences
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.EBI
Bioorg Med Chem Lett 15: 2990-3 (2005)
Daiichi Suntory Biomedical Research
4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.EBI
Bioorg Med Chem Lett 15: 2998-3001 (2005)
Korea Research Institute of Chemical Technology
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa.EBI
Bioorg Med Chem Lett 15: 3006-11 (2005)
Pfizer
Synthesis and characterization of azole isoflavone inhibitors of aromatase.BDB
Bioorg Med Chem 13: 4063-70 (2005)
Ohio State University
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.EBI
Bioorg Med Chem Lett 15: 2926-31 (2005)
Merck Research Laboratories
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.BDB
Bioorg Med Chem Lett 15: 2918-22 (2005)
Abbott Laboratories
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.EBI
Bioorg Med Chem Lett 15: 2910-3 (2005)
Vrije Universiteit Amsterdam
New inhibitors of rabbit muscle triose-phosphate isomerase.EBI
Bioorg Med Chem Lett 15: 2906-9 (2005)
Paris-Sud University
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism.EBI
Bioorg Med Chem Lett 15: 2898-901 (2005)
Janssen-Cilag
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.EBI
Bioorg Med Chem Lett 15: 2894-7 (2005)
Salk Institute
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.EBI
Bioorg Med Chem Lett 15: 2891-3 (2005)
Chinese Academy of Sciences
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.EBI
Bioorg Med Chem Lett 15: 2886-90 (2005)
Reverse Proteomics Research Institute
Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes.EBI
Bioorg Med Chem Lett 15: 2881-5 (2005)
Nagoya City University
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.BDB
Bioorg Med Chem Lett 15: 2870-5 (2005)
Pfizer
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.EBI
Bioorg Med Chem Lett 15: 2865-9 (2005)
Wyeth Research
Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.EBI
Bioorg Med Chem Lett 15: 2857-60 (2005)
Institute of Science & Technology
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization.EBI
Bioorg Med Chem Lett 15: 2840-4 (2005)
The Scripps Research Institute
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.EBI
Bioorg Med Chem Lett 15: 2824-8 (2005)
Merck Research Laboratories
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.EBI
Bioorg Med Chem Lett 15: 2819-23 (2005)
Procter & Gamble Pharmaceuticals
Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid.EBI
Bioorg Med Chem Lett 15: 2812-8 (2005)
Pfizer
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13.EBI
Bioorg Med Chem Lett 15: 2808-11 (2005)
Pfizer
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.EBI
Bioorg Med Chem Lett 15: 2803-7 (2005)
Abbott Laboratories
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.EBI
Bioorg Med Chem Lett 15: 2771-5 (2005)
Merck Research Laboratories
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.EBI
Bioorg Med Chem Lett 15: 2758-60 (2005)
University of Tennessee
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.EBI
Bioorg Med Chem Lett 15: 2752-7 (2005)
Abbott Laboratories
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.EBI
Bioorg Med Chem Lett 15: 2734-7 (2005)
Aventis Pharmaceuticals
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.EBI
Bioorg Med Chem Lett 15: 2970-3 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.EBI
Bioorg Med Chem Lett 15: 2974-9 (2005)
Pfizer
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.EBI
Bioorg Med Chem Lett 15: 3020-3 (2005)
Schering-Plough Research Institute
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.BDB
Bioorg Med Chem Lett 15: 3048-52 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes.EBI
Bioorg Med Chem Lett 15: 3096-101 (2005)
Ospedale San Lazzaro
QSAR analysis of thiazole benzenesulfonamide substituted 3-pyridylethanolamines as beta3-adrenergic receptor agonist.EBI
Bioorg Med Chem Lett 15: 3167-73 (2005)
S.G.S.I.T.S.
Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumors.EBI
Bioorg Med Chem Lett 15: 3302-6 (2005)
Università
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.EBI
Bioorg Med Chem Lett 15: 3102-8 (2005)
Universit£
Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.BDB
J Pharmacol Exp Ther 314: 876-82 (2005)
University of Tokyo
NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.BDB
J Biol Chem 280: 30273-81 (2005)
India Central Drug Research Institute
Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.EBI
Bioorg Med Chem Lett 15: 3058-62 (2005)
Development Center For Biotechnology
Acyclic cyanamide-based inhibitors of cathepsin K.EBI
Bioorg Med Chem Lett 15: 3039-43 (2005)
Glaxosmithkline
Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors.EBI
Bioorg Med Chem Lett 15: 3109-13 (2005)
Tohoku University
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.BDB
J Enzyme Inhib Med Chem 20: 61-7 (2005)
Crefsip
Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.BDB
J Enzyme Inhib Med Chem 20: 41-7 (2005)
Quaid-I-Azam University
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease.EBI
Bioorg Med Chem Lett 15: 3086-90 (2005)
University of Debrecen
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators.EBI
Bioorg Med Chem Lett 15: 3119-25 (2005)
Universidade De SãO Paulo
4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR.EBI
Bioorg Med Chem Lett 15: 3053-7 (2005)
Bayer Research Center
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.BDB
J Med Chem 48: 3654-8 (2005)
Universidad Central De Venezuela
Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase?EBI
J Med Chem 48: 3649-53 (2005)
Florida International University
A new structural motif for mu-opioid antagonists.EBI
J Med Chem 48: 3644-8 (2005)
Vrije Universiteit Brussel
Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility.EBI
J Med Chem 48: 3621-9 (2005)
Department of Entomology and University of California Davis Cancer Center
Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1.EBI
J Med Chem 48: 3613-20 (2005)
Vanderbilt University
Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.EBI
J Med Chem 48: 3605-12 (2005)
Eli Lilly
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.EBI
J Med Chem 48: 3586-604 (2005)
Central Pharmaceutical Research Institute
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.BDB
J Med Chem 48: 3576-85 (2005)
University of Illinois At Chicago
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.EBI
J Med Chem 48: 3564-75 (2005)
Universit£
AFMoC enhances predictivity of 3D QSAR: a case study with DOXP-reductoisomerase.EBI
J Med Chem 48: 3547-63 (2005)
Philipps University
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI
J Med Chem 48: 3478-80 (2005)
Glaxosmithkline
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.EBI
J Med Chem 48: 3474-7 (2005)
Pfizer
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.EBI
J Med Chem 48: 3467-70 (2005)
Wyeth Research
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.EBI
J Med Chem 48: 3463-6 (2005)
University of Southern California
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.EBI
J Med Chem 48: 3449-62 (2005)
Monash University (Parkville Campus)
Pyrazole derivatives as photosynthetic electron transport inhibitors: new leads and structure-activity relationship.EBI
J Agric Food Chem 53: 3848-55 (2005)
Universit£
Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue.BDB
J Pharmacol Exp Ther 314: 575-83 (2005)
Duquesne University
Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.BDB
J Pharmacol Exp Ther 314: 568-74 (2005)
Imperial College
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.EBI
Bioorg Med Chem Lett 15: 2790-4 (2005)
Chinese Academy of Sciences
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.EBI
Bioorg Med Chem Lett 15: 2711-5 (2005)
Universidad Nacional De Rosario
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.EBI
Bioorg Med Chem Lett 15: 2943-7 (2005)
Merck Research Laboratories
Total asymmetric synthesis of (-)-conduramine B-1 and of its enantiomer. N-Benzyl derivatives of conduramine B-1 are beta-glucosidase inhibitors.EBI
Bioorg Med Chem Lett 15: 3071-5 (2005)
Ecole Polytechnique FéDéRale De Lausanne (Epfl)
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.EBI
Bioorg Med Chem Lett 15: 3137-42 (2005)
Wyeth Research
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.EBI
Bioorg Med Chem Lett 15: 3081-5 (2005)
Novartis Institutes For Biomedical Research
The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1.EBI
Drug Metab Dispos 33: 1097-100 (2005)
Medical University of South Carolina
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).EBI
Bioorg Med Chem Lett 15: 2761-5 (2005)
Mclean Hospital
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.BDB
Biochemistry 44: 6858-66 (2005)
University of Bath
Aryl sulfones: a new class of gamma-secretase inhibitors.EBI
Bioorg Med Chem Lett 15: 2685-8 (2005)
Merck Sharp & Dohme Research Laboratories
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.EBI
Bioorg Med Chem Lett 15: 2679-84 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Identification of chemokine receptor CCR4 antagonist.EBI
Bioorg Med Chem Lett 15: 2669-72 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of novel diphenacoum-derived, conformation-restricted vitamin K 2,3-epoxide reductase inhibitors.EBI
Bioorg Med Chem Lett 15: 2665-8 (2005)
Tunghai University
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.EBI
Bioorg Med Chem Lett 15: 2647-52 (2005)
Adolor
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists.EBI
Bioorg Med Chem Lett 15: 2641-5 (2005)
Experimental Sugar Cane Station
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.EBI
Bioorg Med Chem Lett 15: 2611-5 (2005)
Pfizer
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.EBI
Bioorg Med Chem Lett 15: 2565-9 (2005)
Taisho Pharmaceutical
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.EBI
Bioorg Med Chem Lett 15: 2541-6 (2005)
Neurocrine Biosciences
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones.EBI
Bioorg Med Chem Lett 15: 2537-40 (2005)
Nps Pharmaceuticals
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.BDB
Bioorg Med Chem Lett 15: 2533-6 (2005)
Merck Research Laboratories
4-Alkyl and 4,4'-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis.EBI
Bioorg Med Chem Lett 15: 2527-31 (2005)
Wyeth Research
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.EBI
Bioorg Med Chem Lett 15: 2523-6 (2005)
Roche Palo Alto
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.EBI
Bioorg Med Chem Lett 15: 2519-22 (2005)
Neurocrine Biosciences
Structure-based design of protein tyrosine phosphatase-1B inhibitors.EBI
Bioorg Med Chem Lett 15: 2503-7 (2005)
Astrazeneca
Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid.EBI
Bioorg Med Chem Lett 15: 2481-6 (2005)
Pfizer
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.EBI
Bioorg Med Chem Lett 15: 2471-5 (2005)
University of Arizona
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.EBI
Bioorg Med Chem Lett 15: 2467-9 (2005)
University of Catania
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.EBI
Bioorg Med Chem Lett 15: 2461-5 (2005)
Acenta Discovery
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.EBI
Bioorg Med Chem Lett 15: 2441-5 (2005)
Mitsubishi Pharma
Selective PPARgamma modulators with improved pharmacological profiles.EBI
Bioorg Med Chem Lett 15: 2437-40 (2005)
Merck Research Laboratories
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.EBI
J Med Chem 48: 3438-42 (2005)
The Danish University of Pharmaceutical Sciences
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.BDB
J Med Chem 48: 3433-7 (2005)
Universita Di Messina
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.EBI
J Med Chem 48: 3428-32 (2005)
Sapienza University of Rome
C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging.EBI
J Med Chem 48: 3400-9 (2005)
University Hospital of The Westf£Lische Wilhelms-Universit£T
Adenosine kinase inhibitors. 4. 6,8-Disubstituted purine nucleoside derivatives. Synthesis, conformation, and enzyme inhibition.EBI
J Med Chem 48: 3389-99 (2005)
Metabasis Therapeutics
Design of benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties.EBI
J Med Chem 48: 3379-88 (2005)
University of Montpellier
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.EBI
J Med Chem 48: 3372-8 (2005)
Sapienza University of Rome
Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line.EBI
J Med Chem 48: 3354-63 (2005)
Universidad De Granada
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.EBI
J Med Chem 48: 3344-53 (2005)
Sapienza University of Rome
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.EBI
J Med Chem 48: 3337-43 (2005)
Universit£
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.EBI
J Med Chem 48: 3328-36 (2005)
University of Florida
Structure-activity relationships of fluorinated lysophosphatidic acid analogues.EBI
J Med Chem 48: 3319-27 (2005)
The University of Utah
Conformation mining: an algorithm for finding biologically relevant conformations.EBI
J Med Chem 48: 3313-8 (2005)
Rational Discovery
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.BDB
J Med Chem 48: 3290-312 (2005)
Aventis Pharma Deutschland
Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds.EBI
J Med Chem 48: 3280-9 (2005)
Kyoto University
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.EBI
J Med Chem 48: 3239-50 (2005)
University of Szeged
Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening.EBI
J Med Chem 48: 3221-30 (2005)
Protana
Successful in silico discovery of novel nonsteroidal ligands for human sex hormone binding globulin.EBI
J Med Chem 48: 3203-13 (2005)
University of British Columbia
Synthesis and antibacterial activity of 1-(2-fluorovinyl)-7-substituted-4-quinolone-3-carboxylic acid derivatives, conformationally restricted analogues of fleroxacin.EBI
J Med Chem 48: 3194-202 (2005)
Kyorin Pharmaceutical
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.EBI
J Med Chem 48: 3171-81 (2005)
University of Michigan
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor.EBI
J Med Chem 48: 3153-63 (2005)
Università
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.BDB
J Med Chem 48: 3141-52 (2005)
The Institute For Diabetes Discovery
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.BDB
J Med Chem 48: 3118-21 (2005)
Abbott Laboratories
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.BDB
J Med Chem 48: 3114-7 (2005)
Karo Bio
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.EBI
J Med Chem 48: 3110-3 (2005)
University of Ljubljana
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.BDB
J Med Chem 48: 3107-9 (2005)
Gsk
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.EBI
J Med Chem 48: 3103-6 (2005)
Fujisawa Pharmaceutical
Discovery of a beta-MSH-derived MC-4R selective agonist.EBI
J Med Chem 48: 3095-8 (2005)
Eli Lilly
Pharmacodynamic characterization of ZP120 (Ac-RYYRWKKKKKKK-NH2), a novel, functionally selective nociceptin/orphanin FQ peptide receptor partial agonist with sodium-potassium-sparing aquaretic activity.BDB
J Pharmacol Exp Ther 314: 652-60 (2005)
Louisiana State University
Chemistry and biology of dihydroisoxazole derivatives: selective inhibitors of human transglutaminase 2.BDB
Chem Biol 12: 469-75 (2005)
Stanford University
Switching between allosteric and dimerization inhibition of HIV-1 protease.BDB
Chem Biol 12: 439-44 (2005)
Purdue University
Novel behavior of O-methylated beta-cyclodextrins in inclusion of meso-tetraarylporphyrins.BDB
J Org Chem 70: 3667-73 (2005)
Doshisha University
Structures and aldose reductase inhibitory effects of bromophenols from the red alga Symphyocladia latiuscula.EBI
J Nat Prod 68: 620-2 (2005)
Jilin Province Academy of Traditional Chinese Medicine and Materia Medica
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.EBI
J Nat Prod 68: 617-9 (2005)
Merck Research Laboratories
Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.EBI
J Nat Prod 68: 611-3 (2005)
Merck Research Laboratories
The psammaplysenes, specific inhibitors of FOXO1a nuclear export.EBI
J Nat Prod 68: 574-6 (2005)
Harvard Medical School
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.EBI
J Nat Prod 68: 572-3 (2005)
Mitsubishi Pharma
QSAR for phospholipase A2 inhibitions by 1-acyloxy-3-N-n-octylcarbamyl-benzenes.EBI
Bioorg Med Chem Lett 15: 2405-8 (2005)
National Chung-Hsing University
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.EBI
Bioorg Med Chem Lett 15: 2399-403 (2005)
Procter and Gamble Pharmaceuticals
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 2385-8 (2005)
Merck Research Laboratories
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.EBI
Bioorg Med Chem Lett 15: 2381-4 (2005)
RhôNe-Poulenc Rorer
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.EBI
Bioorg Med Chem Lett 15: 2371-4 (2005)
Pfizer
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.EBI
Bioorg Med Chem Lett 15: 2365-9 (2005)
Schering-Plough Research Institute
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds.EBI
Bioorg Med Chem Lett 15: 2359-64 (2005)
Ospedale San Lazzaro
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors.EBI
Bioorg Med Chem Lett 15: 2353-8 (2005)
Universit£
Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols.EBI
Bioorg Med Chem Lett 15: 2347-52 (2005)
University of Bucharest
Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies.EBI
Bioorg Med Chem Lett 15: 2315-20 (2005)
University of Naples Federico Ii
A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs.EBI
Bioorg Med Chem Lett 15: 2311-4 (2005)
Università
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.BDB
Bioorg Med Chem Lett 15: 2305-9 (2005)
Gsk
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.EBI
Bioorg Med Chem Lett 15: 2295-9 (2005)
Celltech R&D
Oximinoarylsulfonamides as potent HIV protease inhibitors.BDB
Bioorg Med Chem Lett 15: 2275-8 (2005)
Abbott Laboratories
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives.EBI
Bioorg Med Chem Lett 15: 2265-9 (2005)
Kyoto 619-0216
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.EBI
Bioorg Med Chem Lett 15: 2259-63 (2005)
Merck Research Laboratories
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.BDB
Bioorg Med Chem Lett 15: 2253-8 (2005)
Merck Research Laboratories
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI
Bioorg Med Chem Lett 15: 2249-52 (2005)
Berlex Biosciences
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.EBI
Bioorg Med Chem Lett 15: 2235-8 (2005)
Kudos Horsham
NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.EBI
Bioorg Med Chem Lett 15: 2231-4 (2005)
Ludwig-Maximilians-UniversitäT MüNchen
Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.EBI
Bioorg Med Chem Lett 15: 2225-30 (2005)
Duquesne University
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.BDB
Bioorg Med Chem Lett 15: 2221-4 (2005)
Johnson & Johnson Pharmaceutical
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action.EBI
Bioorg Med Chem Lett 15: 2215-9 (2005)
Dartmouth College
A structural screening approach to ketoamide-based inhibitors of cathepsin K.EBI
Bioorg Med Chem Lett 15: 2209-13 (2005)
Glaxosmithkline
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.BDB
Bioorg Med Chem Lett 15: 2203-7 (2005)
Glaxosmithkline
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.BDB
J Pharmacol Exp Ther 314: 77-85 (2005)
Taisho Pharmaceutical
Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines.BDB
Bioorg Med Chem 13: 2263-83 (2005)
Cnrs
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.BDB
J Med Chem 48: 3080-4 (2005)
Nerviano Medical Sciences
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.EBI
J Med Chem 48: 3076-9 (2005)
Lundbeck Research Usa
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.EBI
J Med Chem 48: 3060-75 (2005)
University of Florida
Applying linear interaction energy method for rational design of noncompetitive allosteric inhibitors of the sarco- and endoplasmic reticulum calcium-ATPase.EBI
J Med Chem 48: 3005-14 (2005)
Johns Hopkins University
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.EBI
J Med Chem 48: 2972-84 (2005)
University of Maryland
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.EBI
J Med Chem 48: 2964-71 (2005)
Glaxosmithkline
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.EBI
J Med Chem 48: 2957-63 (2005)
University of Illinois At Urbana-Champaign
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.BDB
J Med Chem 48: 2944-56 (2005)
Nerviano Medical Sciences
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.EBI
J Med Chem 48: 2936-43 (2005)
Università
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.BDB
J Med Chem 48: 2906-15 (2005)
University of Mississippi
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.EBI
J Med Chem 48: 2892-905 (2005)
Memorial Sloan-Kettering Cancer Center
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.EBI
J Med Chem 48: 2882-91 (2005)
Korea Research Institute of Chemical Technology
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.EBI
J Med Chem 48: 2876-81 (2005)
Medical University of South Carolina
Design, synthesis, and antiviral activity of adenosine 5'-phosphonate analogues as chain terminators against hepatitis C virus.EBI
J Med Chem 48: 2867-75 (2005)
Valeant Pharmaceuticals International
N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo.EBI
J Med Chem 48: 2778-89 (2005)
Technische Universit£T M£Nchen
Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.EBI
J Med Chem 48: 2759-62 (2005)
University of Bath
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.BDB
J Am Chem Soc 127: 5463-8 (2005)
Yale University
Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP.EBI
Bioorg Med Chem Lett 15: 2177-80 (2005)
University of Minnesota
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.EBI
Bioorg Med Chem Lett 15: 2163-7 (2005)
Merck Research Laboratories
The role of QSAR in dopamine interactions.EBI
Bioorg Med Chem Lett 15: 2149-57 (2005)
Pomona College
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.EBI
Bioorg Med Chem Lett 15: 2129-34 (2005)
Merck Research Laboratories
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.EBI
Bioorg Med Chem Lett 15: 2119-22 (2005)
Schering-Plough Research Institute
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.EBI
Bioorg Med Chem Lett 15: 2107-10 (2005)
Rensselaer Polytechnic Institute
Discovery, synthesis and biological evaluation of novel glucokinase activators.EBI
Bioorg Med Chem Lett 15: 2103-6 (2005)
Astrazeneca
QSAR analyses of conformationally restricted 1,5-diaryl pyrazoles as selective COX-2 inhibitors: application of connection table representation of ligands.EBI
Bioorg Med Chem Lett 15: 2097-102 (2005)
Devi Ahilya Vishwavidyalaya
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.EBI
Bioorg Med Chem Lett 15: 2093-6 (2005)
Ranbaxy Research Laboratories
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.EBI
Bioorg Med Chem Lett 15: 2087-91 (2005)
Genzyme
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.EBI
Bioorg Med Chem Lett 15: 2073-7 (2005)
Targacept
Inhibitory activities against topoisomerase I and II by isoaurostatin derivatives and their structure-activity relationships.EBI
Bioorg Med Chem Lett 15: 2065-8 (2005)
Kumamoto University
A general carbometalation, three component coupling strategy for the synthesis of alpha,beta-unsaturated gamma-sultines including thio-rofecoxib, a selective COX-2 inhibitor.EBI
Bioorg Med Chem Lett 15: 2057-60 (2005)
Methylgene
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.EBI
Bioorg Med Chem Lett 15: 2041-5 (2005)
Merck Research Laboratories
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.BDB
Bioorg Med Chem Lett 15: 2033-9 (2005)
Abbott Laboratories
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.EBI
Bioorg Med Chem Lett 15: 1997-2001 (2005)
Merck Research Laboratories
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.EBI
Bioorg Med Chem Lett 15: 1993-6 (2005)
Merck Research Laboratories
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.EBI
Bioorg Med Chem Lett 15: 1987-91 (2005)
Virginia Commonwealth University
Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.EBI
Bioorg Med Chem Lett 15: 1973-7 (2005)
Bayer Research Center
Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.EBI
Bioorg Med Chem Lett 15: 1969-72 (2005)
Miikana Therapeutics
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.EBI
J Med Chem 48: 2695-700 (2005)
Biota
Anchor-GRIND: filling the gap between standard 3D QSAR and the GRid-INdependent descriptors.EBI
J Med Chem 48: 2687-94 (2005)
Imim/Universitat Pompeu Fabra
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.EBI
J Med Chem 48: 2678-86 (2005)
Mitsubishi Pharma
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.EBI
J Med Chem 48: 2646-54 (2005)
Universit£
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.EBI
J Med Chem 48: 2638-45 (2005)
Universit£
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.EBI
J Med Chem 48: 2627-37 (2005)
University Walk
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.EBI
J Med Chem 48: 2559-70 (2005)
Columbia University College of Physicians and Surgeons
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.EBI
J Med Chem 48: 2548-2558 (2005)
TBA
Virtual screening workflow development guided by the"receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.EBI
J Med Chem 48: 2534-47 (2005)
Universit£
Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.EBI
J Med Chem 48: 2509-17 (2005)
Université
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.EBI
J Med Chem 48: 2493-508 (2005)
Friedrich-Alexander University
Architecture of the human urotensin II receptor: comparison of the binding domains of peptide and non-peptide urotensin II agonists.EBI
J Med Chem 48: 2480-92 (2005)
Università
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.EBI
J Med Chem 48: 2469-79 (2005)
Molecular Discovery
LEA3D: a computer-aided ligand design for structure-based drug design.EBI
J Med Chem 48: 2457-68 (2005)
University of Montpellier
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.EBI
J Med Chem 48: 2420-31 (2005)
Università
Sulfur-substituted alpha-alkyl phenethylamines as selective and reversible MAO-A inhibitors: biological activities, CoMFA analysis, and active site modeling.EBI
J Med Chem 48: 2407-19 (2005)
Universidad De Chile
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.BDB
J Med Chem 48: 2388-406 (2005)
Pfizer
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB
J Med Chem 48: 2371-87 (2005)
Pfizer
Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.EBI
J Med Chem 48: 2336-45 (2005)
Decode Biostructures
Enantiospecificity of glutamate carboxypeptidase II inhibition.BDB
J Med Chem 48: 2319-24 (2005)
Guilford Pharmaceuticals
9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI
J Med Chem 48: 2282-93 (2005)
Merck Research Laboratories
Virtual docking approaches to protein kinase B inhibition.BDB
J Med Chem 48: 2278-81 (2005)
The Burnham Institute
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.EBI
J Med Chem 48: 2274-7 (2005)
Schering-Plough Research Institute
Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.EBI
J Med Chem 48: 2270-3 (2005)
Eli Lilly
3-Substituted imidazo[1,2-d][1,2,4]-thiadiazoles: a novel class of factor XIIIa inhibitors.EBI
J Med Chem 48: 2266-9 (2005)
Apotex Research
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.EBI
J Med Chem 48: 2262-5 (2005)
Merck Research Laboratories
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.EBI
J Med Chem 48: 2258-61 (2005)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.BDB
J Pharmacol Exp Ther 314: 244-51 (2005)
Kyowa Hakko Kogyo
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.BDB
J Biol Chem 280: 21847-53 (2005)
University of Texas Southwestern Medical Center
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.EBI
J Nat Prod 68: 447-9 (2005)
Chiba University
Terphenylquinone inhibitors of the src protein tyrosine kinase from Stilbella sp.EBI
J Nat Prod 68: 323-6 (2005)
Boehringer Ingelheim Pharma
Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.BDB
J Pharmacol Exp Ther 314: 191-200 (2005)
Abbott Laboratories
UDP-glucuronosyltransferases and clinical drug-drug interactions.EBI
Pharmacol Ther 106: 97-132 (2005)
The University of British Columbia
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.BDB
Bioorg Med Chem Lett 15: 1943-7 (2005)
Eli Lilly
Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II.EBI
Bioorg Med Chem Lett 15: 1937-42 (2005)
University of Naples 'Federico Ii
Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.EBI
Bioorg Med Chem Lett 15: 1931-5 (2005)
University of Auckland
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides.EBI
Bioorg Med Chem Lett 15: 1909-13 (2005)
Università
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.EBI
Bioorg Med Chem Lett 15: 1901-7 (2005)
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 15: 1895-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.EBI
Bioorg Med Chem Lett 15: 1891-4 (2005)
Wyeth Research
Structure-activity relationship study of novel tissue transglutaminase inhibitors.EBI
Bioorg Med Chem Lett 15: 1885-9 (2005)
Harvard Medical School
Synthesis of 15R-PGD2: a potential DP2 receptor agonist.EBI
Bioorg Med Chem Lett 15: 1873-6 (2005)
Florida Institute of Technology
Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome.EBI
Bioorg Med Chem Lett 15: 1867-71 (2005)
Numazu Bio-Medical Research Institute
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.EBI
Bioorg Med Chem Lett 15: 1857-61 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.EBI
Bioorg Med Chem Lett 15: 1847-50 (2005)
Lanzhou University
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.BDB
Bioorg Med Chem Lett 15: 1841-5 (2005)
Chemical Diversity Research Institute
Novel heterocyclic thyromimetics.EBI
Bioorg Med Chem Lett 15: 1835-40 (2005)
Bayer Healthcare
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.EBI
Bioorg Med Chem Lett 15: 1829-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.EBI
Bioorg Med Chem Lett 15: 1815-9 (2005)
Glaxosmithkline
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.EBI
Bioorg Med Chem Lett 15: 1807-10 (2005)
Pfizer
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.EBI
Bioorg Med Chem Lett 15: 1799-802 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.EBI
Bioorg Med Chem Lett 15: 1793-7 (2005)
National Institute of Pharmaceutical Education and Research (NIPER)
Structure-activity relationships of the oxindole growth hormone secretagogues.EBI
Bioorg Med Chem Lett 15: 1789-92 (2005)
Sumitomo Pharmaceuticals
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands.EBI
Bioorg Med Chem Lett 15: 1779-83 (2005)
Aventis Pharma Deutschland
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.EBI
Bioorg Med Chem Lett 15: 1773-7 (2005)
Technische Universit£T M£Nchen
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.BDB
J Biol Chem 280: 19867-74 (2005)
Berlex Biosciences
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.EBI
J Med Chem 48: 2248-50 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.EBI
J Med Chem 48: 2243-7 (2005)
Glaxosmithkline Research & Development
Development of low molecular weight HIV-1 protease dimerization inhibitors.EBI
J Med Chem 48: 2239-42 (2005)
Purdue University
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.EBI
J Med Chem 48: 2229-38 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.EBI
J Med Chem 48: 2194-211 (2005)
Pharmaceutical Research Institute
Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.EBI
J Med Chem 48: 2154-66 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.EBI
J Med Chem 48: 2134-53 (2005)
Janssen-Cilag
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.EBI
J Med Chem 48: 2126-33 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.BDB
J Med Chem 48: 2121-5 (2005)
Universita Degli Studi Di Firenze
Development of spin-labeled probes for adenosine receptors.EBI
J Med Chem 48: 2108-14 (2005)
University of Bonn
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.EBI
J Med Chem 48: 2100-7 (2005)
Vrije Universiteit Amsterdam
Synthesis of new benzoxazinone derivatives as neuropeptide Y5 antagonists for the treatment of obesity.EBI
J Med Chem 48: 2080-92 (2005)
Laboratorios Dr. Esteve
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI
J Med Chem 48: 2054-71 (2005)
Janssen-Cilag
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.EBI
J Med Chem 48: 2045-53 (2005)
Leiden/Amsterdam Center For Drug Research
Biological properties of D- and L-1-deoxyazasugars.EBI
J Med Chem 48: 2036-44 (2005)
Toyama Medical and Pharmaceutical University
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.EBI
J Med Chem 48: 2026-35 (2005)
University of Ferrara
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.EBI
J Med Chem 48: 2009-18 (2005)
Biogen Idec
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.BDB
J Med Chem 48: 1984-2008 (2005)
Johnson & Johnson Pharmaceutical
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.EBI
J Med Chem 48: 1965-73 (2005)
Tibotec
Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.EBI
J Med Chem 48: 1941-7 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase.EBI
J Med Chem 48: 1930-40 (2005)
Tibotec
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.BDB
J Med Chem 48: 1919-29 (2005)
Universita Di Siena
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.BDB
J Med Chem 48: 1886-900 (2005)
Johnson & Johnson Pharmaceutical
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.EBI
J Med Chem 48: 1873-85 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.EBI
J Med Chem 48: 1857-72 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.EBI
J Med Chem 48: 1849-56 (2005)
The Scripps Research Institute
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.EBI
J Med Chem 48: 1839-48 (2005)
University of Arizona
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.EBI
J Med Chem 48: 1823-38 (2005)
Solvay Pharma
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.EBI
J Med Chem 48: 1806-12 (2005)
University of Kansas
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.BDB
J Med Chem 48: 1796-805 (2005)
Saarland University
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.EBI
J Med Chem 48: 1781-95 (2005)
Laboratorios Dr. Esteve
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.BDB
J Med Chem 48: 1768-80 (2005)
University of Antwerp
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.EBI
J Med Chem 48: 1745-58 (2005)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.BDB
J Med Chem 48: 1729-44 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI
J Med Chem 48: 1725-8 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.EBI
J Med Chem 48: 1721-4 (2005)
University of Illinois At Chicago
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.EBI
J Med Chem 48: 1717-20 (2005)
Johnson & Johnson Pharmaceutical Research and Development
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI
J Med Chem 48: 1709-12 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.EBI
J Med Chem 48: 1705-8 (2005)
Università
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.BDB
J Med Chem 48: 1701-4 (2005)
Universitat De Barcelona
Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.EBI
J Med Chem 48: 1697-700 (2005)
Research and Development
Desensitization of the human motilin receptor by motilides.BDB
J Pharmacol Exp Ther 313: 1397-405 (2005)
Katholieke Universiteit Leuven
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.BDB
Bioorg Med Chem 13: 2665-78 (2005)
Biocryst Pharmaceuticals
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.BDB
Bioorg Med Chem 13: 2657-64 (2005)
Pfizer
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.EBI
Bioorg Med Chem Lett 15: 1749-53 (2005)
Athersys
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.BDB
Bioorg Med Chem Lett 15: 1743-7 (2005)
Wyeth-Ayerst Research
A two-state homology model of the hERG K+ channel: application to ligand binding.EBI
Bioorg Med Chem Lett 15: 1737-41 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel beta-(imidazol-4-yl)-beta-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I.EBI
Bioorg Med Chem Lett 15: 1713-9 (2005)
Janssen Research Foundation
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.EBI
Bioorg Med Chem Lett 15: 1707-11 (2005)
Virginia Commonwealth University
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.EBI
Bioorg Med Chem Lett 15: 1701-5 (2005)
University of Michigan
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.EBI
Bioorg Med Chem Lett 15: 1697-700 (2005)
Roche Palo Alto
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.EBI
Bioorg Med Chem Lett 15: 1687-91 (2005)
Johnson and Johnson Pharmaceutical Research and Development
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.EBI
Bioorg Med Chem Lett 15: 1683-6 (2005)
University of Montpellier
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.EBI
Bioorg Med Chem Lett 15: 1675-81 (2005)
Merck Research Laboratories
Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).EBI
Bioorg Med Chem Lett 15: 1669-73 (2005)
Osi Pharmaceuticals
Combinatorial approaches towards the discovery of new tryptase inhibitors.EBI
Bioorg Med Chem Lett 15: 1659-64 (2005)
University of Barcelona
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.EBI
Bioorg Med Chem Lett 15: 1647-50 (2005)
Merck Research Laboratories
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.EBI
Bioorg Med Chem Lett 15: 1641-5 (2005)
Wyeth Research
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.EBI
Bioorg Med Chem Lett 15: 1623-7 (2005)
Amgen
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).EBI
Bioorg Med Chem Lett 15: 1619-21 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design.EBI
Bioorg Med Chem Lett 15: 1599-603 (2005)
F. Hoffmann-La Roche
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Bioorg Med Chem Lett 15: 1587-90 (2005)
Pfizer
Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.EBI
Bioorg Med Chem Lett 15: 1583-6 (2005)
Human Biomolecular Research Institute
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.EBI
Bioorg Med Chem Lett 15: 1577-82 (2005)
Abbott Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.EBI
Bioorg Med Chem Lett 15: 1565-71 (2005)
Merck Research Laboratories
3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.EBI
Bioorg Med Chem Lett 15: 1557-60 (2005)
Nps Pharmaceuticals
Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture.EBI
Bioorg Med Chem Lett 15: 1553-6 (2005)
Glaxosmithkline
Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.BDB
J Pharmacol Exp Ther 313: 1281-8 (2005)
Neurocrine Biosciences
Endocrinological properties of two novel nonsteroidal progesterone receptor modulators, CP8816 and CP8863.BDB
J Pharmacol Exp Ther 313: 916-20 (2005)
Meiji Seika Kaisha
Identification of small molecule chemical inhibitors of the collagen-specific chaperone Hsp47.EBI
J Med Chem 48: 1680-4 (2005)
Mcmaster University
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.EBI
J Med Chem 48: 1676-9 (2005)
University of Bath
Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach.BDB
J Med Chem 48: 1649-56 (2005)
Burnham Institute
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.EBI
J Med Chem 48: 1620-9 (2005)
University of Medicine & Dentistry of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.BDB
J Med Chem 48: 1610-9 (2005)
Glaxosmithkline
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.BDB
J Med Chem 48: 1596-609 (2005)
Quorex Pharmaceuticals
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.BDB
J Med Chem 48: 1563-75 (2005)
Saarland University
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.EBI
J Med Chem 48: 1550-62 (2005)
Universit£
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.EBI
J Med Chem 48: 1540-9 (2005)
Neurocrine Biosciences
Design and biological evaluation of linear and cyclic phosphopeptide ligands of the N-terminal SH2 domain of protein tyrosine phosphatase SHP-1.EBI
J Med Chem 48: 1528-39 (2005)
Friedrich-Schiller-University
Novel ligands for the chemokine receptor-3 (CCR3): a receptor-modeling study based on 5D-QSAR.EBI
J Med Chem 48: 1515-27 (2005)
Biographics Laboratory 3R
NMR studies reveal structural differences between the gallium and yttrium complexes of DOTA-D-Phe1-Tyr3-octreotide.EBI
J Med Chem 48: 1506-14 (2005)
Technische Universit£T M£Nchen
Dynamic receptor-based pharmacophore model development and its application in designing novel HIV-1 integrase inhibitors.EBI
J Med Chem 48: 1496-505 (2005)
University of Houston
A shape-based 3-D scaffold hopping method and its application to a bacterial protein-protein interaction.EBI
J Med Chem 48: 1489-95 (2005)
Wyeth Research
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.EBI
J Med Chem 48: 1448-69 (2005)
Duquesne University
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.EBI
J Med Chem 48: 1421-7 (2005)
University of Ferrara
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.EBI
J Med Chem 48: 1367-83 (2005)
Merck Sharp & Dohme Research Laboratories
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.EBI
J Med Chem 48: 1359-66 (2005)
Kirin Brewery
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.EBI
J Med Chem 48: 1336-43 (2005)
University of New Orleans
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.EBI
J Med Chem 48: 1318-21 (2005)
Abbott Laboratories
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.EBI
J Med Chem 48: 1314-7 (2005)
Irbm (Merck Research Laboratories Rome)
New approaches toward anti-HIV chemotherapy.EBI
J Med Chem 48: 1297-313 (2005)
Katholieke Universiteit Leuven
From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.BDB
Chembiochem 6: 531-40 (2005)
Schering
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.BDB
Chem Biol 12: 237-47 (2005)
National Institutes of Health
Structural basis for the highly selective inhibition of MMP-13.BDB
Chem Biol 12: 181-9 (2005)
Aventis Pharma Deutschland
Bioactive constituents from Boswellia papyrifera.EBI
J Nat Prod 68: 189-93 (2005)
University of Karachi
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.BDB
J Am Chem Soc 127: 2741-51 (2005)
University of North Carolina
Use of binding enthalpy to drive an allosteric transition.BDB
Biochemistry 44: 3112-21 (2005)
University of Maryland
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.EBI
J Med Chem 48: 1278-81 (2005)
Vertex Pharmaceuticals
Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.EBI
J Med Chem 48: 1274-7 (2005)
University of Michigan
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.BDB
J Med Chem 48: 1237-43 (2005)
Purdue Pharma
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.EBI
J Med Chem 48: 1229-36 (2005)
University of Kansas
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists.EBI
J Med Chem 48: 1221-8 (2005)
Research Triangle Institute
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.EBI
J Med Chem 48: 1169-78 (2005)
Neurocrine Biosciences
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.EBI
J Med Chem 48: 1145-51 (2005)
Leiden/Amsterdam Center For Drug Research
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.EBI
J Med Chem 48: 1107-31 (2005)
Wyeth Research
Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.EBI
J Med Chem 48: 1098-106 (2005)
University of Southern California
Structure-based drug discovery using GPCR homology modeling: successful virtual screening for antagonists of the alpha1A adrenergic receptor.EBI
J Med Chem 48: 1088-97 (2005)
Aventis Pharma Deutschland
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.EBI
J Med Chem 48: 1019-32 (2005)
Nagoya City University
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.EBI
J Med Chem 48: 986-94 (2005)
National Institute On Aging
Application of a flexible synthesis of (5R)-thiolactomycin to develop new inhibitors of type I fatty acid synthase.EBI
J Med Chem 48: 946-61 (2005)
Johns Hopkins University
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.EBI
J Med Chem 48: 926-34 (2005)
Johnson and Johnson Pharmaceutical Research & Development
Three-dimensional structure-activity relationships of nonsteroidal ligands in complex with androgen receptor ligand-binding domain.EBI
J Med Chem 48: 917-25 (2005)
Csc-Scientific Computing
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine.EBI
J Med Chem 48: 913-6 (2005)
Università
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.BDB
J Med Chem 48: 909-12 (2005)
Johnson & Johnson Pharmaceutical
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.EBI
J Med Chem 48: 905-8 (2005)
Pfizer
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.EBI
J Med Chem 48: 897-900 (2005)
7Tm Pharma
(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.EBI
Bioorg Med Chem Lett 15: 1525-7 (2005)
National Research Laboratory of Lipid Metabolism and Atherosclerosis
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies.BDB
Bioorg Med Chem Lett 15: 1509-13 (2005)
Pharmacor
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.EBI
Bioorg Med Chem Lett 15: 1505-7 (2005)
Chinese Academy of Sciences
Glucokinase-activating ureas.EBI
Bioorg Med Chem Lett 15: 1501-4 (2005)
Osi Pharmaceuticals
Structure-activity relationships of dimeric PPAR agonists.EBI
Bioorg Med Chem Lett 15: 1497-500 (2005)
Novo Nordisk
Aglycon specificity profiling of alpha-glucosidases using synthetic probes.EBI
Bioorg Med Chem Lett 15: 1489-92 (2005)
Institute of Physical and Chemical Research (Riken)
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.EBI
Bioorg Med Chem Lett 15: 1475-8 (2005)
Genomics Institute of The Novartis Research Foundation
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.EBI
Bioorg Med Chem Lett 15: 1467-70 (2005)
Arena Pharmaceuticals
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.EBI
Bioorg Med Chem Lett 15: 1463-6 (2005)
Ligand Pharmaceuticals
Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors.EBI
Bioorg Med Chem Lett 15: 1457-61 (2005)
Queen'S University
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.EBI
Bioorg Med Chem Lett 15: 1441-6 (2005)
Merck Research Laboratories
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.BDB
Bioorg Med Chem Lett 15: 1435-40 (2005)
Bristol-Myers Squibb
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.EBI
Bioorg Med Chem Lett 15: 1429-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.EBI
Bioorg Med Chem Lett 15: 1423-8 (2005)
The Scripps Research Institute
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.EBI
Bioorg Med Chem Lett 15: 1407-11 (2005)
Neurocrine Biosciences
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.EBI
Bioorg Med Chem Lett 15: 1401-5 (2005)
Merck Research Laboratories
Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.EBI
Bioorg Med Chem Lett 15: 1385-8 (2005)
Nih
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.EBI
Bioorg Med Chem Lett 15: 1379-83 (2005)
Maxim Pharmaceuticals
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.EBI
Bioorg Med Chem Lett 15: 1375-8 (2005)
Schering-Plough Research Institute
Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives.EBI
Bioorg Med Chem Lett 15: 1361-6 (2005)
Dainippon Pharmaceutical
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.EBI
Bioorg Med Chem Lett 15: 1345-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.EBI
Bioorg Med Chem Lett 15: 1337-40 (2005)
Korea Research Institute of Chemical Technology
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.EBI
Bioorg Med Chem Lett 15: 1327-31 (2005)
Amura Therapeutics
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.EBI
Bioorg Med Chem Lett 15: 1321-6 (2005)
Universit£
Benzodipyrazoles: a new class of potent CDK2 inhibitors.BDB
Bioorg Med Chem Lett 15: 1315-9 (2005)
Nerviano Medical Sciences
Amino acid conjugates as kappa opioid receptor agonists.EBI
Bioorg Med Chem Lett 15: 1279-82 (2005)
Adolor
A small molecule-kinase interaction map for clinical kinase inhibitors.EBI
Nat Biotechnol 23: 329-36 (2005)
Ambit Biosciences
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.BDB
J Biol Chem 280: 15761-6 (2005)
Emory University
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.BDB
Chembiochem 6: 541-9 (2005)
Technische UniversitÄT Braunschweig
Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues.BDB
Chembiochem 6: 527-31 (2005)
Max-Planck-Institut FÜR Molekulare Physiologie
Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.EBI
J Med Chem 48: 893-6 (2005)
Eli Lilly
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.EBI
J Med Chem 48: 849-56 (2005)
Unibioscreen
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.EBI
J Med Chem 48: 839-48 (2005)
National Institute On Drug Abuse-Intramural Research Program
Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.EBI
J Med Chem 48: 764-72 (2005)
National Cancer Institute-Frederick
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.BDB
J Med Chem 48: 744-52 (2005)
Abbott Laboratories
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.BDB
J Med Chem 48: 737-43 (2005)
Lawrence Berkeley National Laboratory
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.EBI
J Med Chem 48: 694-709 (2005)
Friedrich-Alexander University
Mechanism of CDK5/p25 binding by CDK inhibitors.EBI
J Med Chem 48: 671-9 (2005)
European Institute of Oncology
Alkylamino derivatives of 4-aminomethylpyridine as inhibitors of copper-containing amine oxidases.EBI
J Med Chem 48: 664-70 (2005)
Universit£
Structure of human cytidine deaminase bound to a potent inhibitor.EBI
J Med Chem 48: 658-60 (2005)
Harvard University
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.BDB
J Med Chem 48: 655-7 (2005)
Shanghai Institute of Materia Medica
N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase.EBI
Bioorg Med Chem Lett 15: 1235-8 (2005)
Novartis Institutes For Biomedical Research
Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.EBI
Bioorg Med Chem Lett 15: 1225-8 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.EBI
Bioorg Med Chem Lett 15: 1221-4 (2005)
National Institute of Diabetes and Digestive and Kidney Diseases
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.EBI
Bioorg Med Chem Lett 15: 1217-20 (2005)
Novartis Institutes For Biomedical Research
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.EBI
Bioorg Med Chem Lett 15: 1201-4 (2005)
Abbott Laboratories
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.EBI
Bioorg Med Chem Lett 15: 1197-200 (2005)
Merck Research Laboratories
1,2,4-Benzothiadiazine derivatives as alpha1 and 5-HT1A receptor ligands.EBI
Bioorg Med Chem Lett 15: 1185-8 (2005)
Universit£
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.EBI
Bioorg Med Chem Lett 15: 1173-80 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.EBI
Bioorg Med Chem Lett 15: 1165-7 (2005)
RhôNe-Poulenc Rorer
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.EBI
Bioorg Med Chem Lett 15: 1161-4 (2005)
Cerep
2,3-Diarylthiophenes as selective EP1 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 1155-60 (2005)
Merck Frosst Centre For Therapeutic Research
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.EBI
Bioorg Med Chem Lett 15: 1149-54 (2005)
Universit£
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.EBI
Bioorg Med Chem Lett 15: 1143-7 (2005)
University of Kansas
Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status.EBI
Bioorg Med Chem Lett 15: 1135-8 (2005)
Mcgill University/Royal Victoria Hospital
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.EBI
Bioorg Med Chem Lett 15: 1131-3 (2005)
Yale University
Reversal of anticancer drug resistance by COTC based on intracellular glutathione and glyoxalase I.EBI
Bioorg Med Chem Lett 15: 1111-4 (2005)
Keio University
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.EBI
Bioorg Med Chem Lett 15: 1107-9 (2005)
Kyoritsu University of Pharmacy
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).EBI
Bioorg Med Chem Lett 15: 1101-6 (2005)
Pharmaceutical Research Institute
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.EBI
Bioorg Med Chem Lett 15: 1091-5 (2005)
Adolor
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.EBI
Bioorg Med Chem Lett 15: 1083-5 (2005)
Ucb Pharma
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.EBI
Bioorg Med Chem Lett 15: 1061-4 (2005)
Dainippon Pharmaceutical
Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.EBI
Bioorg Med Chem Lett 15: 1055-9 (2005)
Dainippon Pharmaceutical
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.EBI
Bioorg Med Chem Lett 15: 1051-4 (2005)
Hokkaido University
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).EBI
Bioorg Med Chem Lett 15: 1027-32 (2005)
National Institute of Pharmaceutical Education and Research (NIPER)
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 999-1004 (2005)
Neurocrine Biosciences
Two new irreversible inhibitors of dihydrodipicolinate synthase: diethyl (E,E)-4-oxo-2,5-heptadienedioate and diethyl (E)-4-oxo-2-heptenedioate.EBI
Bioorg Med Chem Lett 15: 995-8 (2005)
University of Sydney
Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.EBI
Bioorg Med Chem Lett 15: 989-94 (2005)
Universidad Nacional AutóNoma De MéXico
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.EBI
Bioorg Med Chem Lett 15: 977-82 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.EBI
Bioorg Med Chem Lett 15: 971-6 (2005)
Universit£
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?EBI
Bioorg Med Chem Lett 15: 963-9 (2005)
Universit£
QSAR of estrogen receptor modulators: exploring selectivity requirements for ER(alpha) versus ER(beta) binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters.EBI
Bioorg Med Chem Lett 15: 957-61 (2005)
University of Calcutta
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates.EBI
Bioorg Med Chem Lett 15: 951-5 (2005)
National Chung-Hsing University
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.EBI
Bioorg Med Chem Lett 15: 945-9 (2005)
Yale University
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.EBI
Bioorg Med Chem Lett 15: 911-4 (2005)
Wyeth Research
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.BDB
Bioorg Med Chem Lett 15: 905-9 (2005)
Merck Research Laboratories
The development of potent and selective bisarylmaleimide GSK3 inhibitors.EBI
Bioorg Med Chem Lett 15: 899-903 (2005)
Lilly Research Laboratories
6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model.EBI
Bioorg Med Chem Lett 15: 877-81 (2005)
University of California
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.EBI
Bioorg Med Chem Lett 15: 869-71 (2005)
Universit£T Konstanz
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.BDB
Bioorg Med Chem Lett 15: 863-7 (2005)
Vernalis (R&D)
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.BDB
Nat Biotechnol 23: 201-7 (2005)
Plexxikon
Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2.EBI
J Nat Prod 68: 69-73 (2005)
Tokushima Bunri University
Potent CYP3A4 inhibitory constituents of Piper cubeba.EBI
J Nat Prod 68: 64-8 (2005)
Toyama Medical and Pharmaceutical University
Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.BDB
J Pharmacol Exp Ther 313: 1101-8 (2005)
Mayo Clinic
Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists.BDB
J Pharmacol Exp Ther 313: 831-9 (2005)
Taisho Pharmaceutical
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.BDB
Bioorg Med Chem 13: 949-61 (2005)
Yamanouchi Pharmaceutical
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.BDB
J Pharmacol Exp Ther 313: 549-56 (2005)
German Cancer Research Center
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.EBI
Bioorg Med Chem Lett 15: 833-7 (2005)
Neurocrine Biosciences
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.BDB
Bioorg Med Chem Lett 15: 823-5 (2005)
Martin-Luther-University Halle-Wittenberg
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.BDB
Bioorg Med Chem Lett 15: 817-22 (2005)
F. Hoffmann-La Roche
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.EBI
Bioorg Med Chem Lett 15: 805-7 (2005)
Kyoto 619-0216
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.EBI
Bioorg Med Chem Lett 15: 799-803 (2005)
Kyoto 619-0216
Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.BDB
Bioorg Med Chem Lett 15: 793-7 (2005)
University of Michigan
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.EBI
Bioorg Med Chem Lett 15: 787-91 (2005)
Dbristol-Myers Squibb
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.EBI
Bioorg Med Chem Lett 15: 783-6 (2005)
Schering-Plough Research Institute
Non-peptidic small molecule inhibitors of XIAP.BDB
Bioorg Med Chem Lett 15: 771-5 (2005)
Abbott Laboratories
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.BDB
Bioorg Med Chem Lett 15: 761-4 (2005)
Merck Research Laboratories
Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.EBI
Bioorg Med Chem Lett 15: 751-4 (2005)
Celltech R and D
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.EBI
Bioorg Med Chem Lett 15: 747-50 (2005)
Uppsala University
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.EBI
Bioorg Med Chem Lett 15: 737-41 (2005)
Glaxosmithkline
Active site directed inhibitors of replication-specific bacterial DNA polymerases.EBI
Bioorg Med Chem Lett 15: 729-32 (2005)
Glsynthesis
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.EBI
Bioorg Med Chem Lett 15: 719-23 (2005)
Purdue Pharma
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.EBI
Bioorg Med Chem Lett 15: 715-8 (2005)
Merck Research Laboratories
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.EBI
Bioorg Med Chem Lett 15: 693-8 (2005)
Neurocrine Biosciences
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.BDB
Bioorg Med Chem Lett 15: 687-91 (2005)
National Health Research Institutes
Parallel synthesis of pteridine derivatives as potent inhibitors for hepatitis C virus NS5B RNA-dependent RNA polymerase.EBI
Bioorg Med Chem Lett 15: 675-8 (2005)
Valeant Pharmaceuticals International
Pyrrolidinohydroquinazolines--a novel class of CCR3 modulators.EBI
Bioorg Med Chem Lett 15: 669-73 (2005)
Boehringer Ingelheim Pharma Gmbh And
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.EBI
Bioorg Med Chem Lett 15: 657-64 (2005)
China Pharmaceutical University
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.EBI
Bioorg Med Chem Lett 15: 645-51 (2005)
Merck Research Laboratories
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.EBI
Bioorg Med Chem Lett 15: 635-8 (2005)
Chinese Academy of Sciences
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.EBI
Bioorg Med Chem Lett 15: 631-4 (2005)
Seoul National University
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.EBI
Bioorg Med Chem Lett 15: 609-12 (2005)
Cv Therapeutics
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).EBI
Bioorg Med Chem Lett 15: 599-602 (2005)
Kobe Gakuin University
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.EBI
Bioorg Med Chem Lett 15: 589-93 (2005)
Organon Laboratories
Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'.EBI
Bioorg Med Chem Lett 15: 585-8 (2005)
Menarini Ricerche
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.EBI
Bioorg Med Chem Lett 15: 579-84 (2005)
Universit£
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.EBI
Bioorg Med Chem Lett 15: 573-8 (2005)
Università
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate.EBI
Bioorg Med Chem Lett 15: 567-71 (2005)
Universit£
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.EBI
Bioorg Med Chem Lett 15: 527-30 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.EBI
Bioorg Med Chem Lett 15: 523-6 (2005)
Chinese Academy of Sciences
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.EBI
Bioorg Med Chem Lett 15: 511-5 (2005)
Biogen Idec
Enhanced ligand affinity for receptors in which components of the binding site are independently mobile.BDB
Chem Biol 12: 89-97 (2005)
University of Sheffield
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.BDB
Chem Biol 12: 65-76 (2005)
University of Dundee
Synthesis and biological evaluation of thienopyrrolizines, a new family of CDK/GSK-3 inhibitors.BDB
J Enzyme Inhib Med Chem 19: 585-93 (2004)
UniversitÉ
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.EBI
J Med Chem 48: 586-92 (2005)
Kobe Gakuin University
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.EBI
J Med Chem 48: 569-85 (2005)
Newcastle University
Further naphthylcombretastatins. An investigation on the role of the naphthalene moiety.EBI
J Med Chem 48: 556-68 (2005)
Universidad De Salamanca
Sulfonamide drugs binding to the colchicine site of tubulin: thermodynamic analysis of the drug-tubulin interactions by isothermal titration calorimetry.EBI
J Med Chem 48: 547-55 (2005)
Institute
Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.EBI
J Med Chem 48: 515-22 (2005)
Salk Institute
Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.EBI
J Med Chem 48: 507-14 (2005)
Salk Institute
Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A.EBI
J Med Chem 48: 499-506 (2005)
Astrazeneca Discovery
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.EBI
J Med Chem 48: 483-98 (2005)
University Institute of Pathology
Investigations on the effects of basic side chains on the hormonal profile of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.EBI
J Med Chem 48: 466-74 (2005)
Free University of Berlin
Quantitative structure-activity relationship (5D-QSAR) study of combretastatin-like analogues as inhibitors of tubulin assembly.EBI
J Med Chem 48: 457-65 (2005)
University of Salford
Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme.EBI
J Med Chem 48: 440-9 (2005)
University of Kuopio
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.BDB
J Med Chem 48: 414-26 (2005)
Astex
Aminoimidazolylmethyluracil analogues as potent inhibitors of thymidine phosphorylase and their bioreductive nitroimidazolyl prodrugs.EBI
J Med Chem 48: 392-402 (2005)
University of Manchester
Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131.EBI
J Med Chem 48: 380-91 (2005)
Kyoto University
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.BDB
J Med Chem 48: 364-79 (2005)
Novartis Pharmaceuticals
Rational approach to discover multipotent anti-Alzheimer drugs.BDB
J Med Chem 48: 360-3 (2005)
University of Bologna
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.EBI
J Med Chem 48: 353-6 (2005)
Wyeth Research
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.EBI
J Med Chem 48: 345-8 (2005)
The University of Melbourne
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.BDB
J Biol Chem 280: 13728-34 (2005)
Vertex Pharmaceuticals
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.BDB
Br J Pharmacol 144: 317-22 (2005)
University of Nottingham
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.BDB
Bioorg Med Chem 13: 755-64 (2005)
Uppsala University
Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney.EBI
Drug Metab Dispos 33: 495-9 (2005)
Tokyo University of Science
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.EBI
J Med Chem 48: 330-4 (2005)
Université
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.EBI
J Med Chem 48: 321-9 (2005)
Leiden University
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI
J Med Chem 48: 306-11 (2005)
Novo Nordisk
Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.EBI
J Med Chem 48: 292-305 (2005)
Università
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.BDB
J Med Chem 48: 287-91 (2005)
Institut Claudius Regaud
Design and NMR characterization of active analogues of compstatin containing non-natural amino acids.EBI
J Med Chem 48: 274-86 (2005)
University of California Riverside
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.EBI
J Med Chem 48: 266-73 (2005)
Universit£
Discovery of corticotropin releasing factor 2 receptor selective sauvagine analogues for treatment of skeletal muscle atrophy.EBI
J Med Chem 48: 262-5 (2005)
Procter & Gamble Pharmaceuticals
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.EBI
J Med Chem 48: 224-39 (2005)
Human Biomolecular Research Institute
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.BDB
J Med Chem 48: 163-70 (2005)
Max-Planck-Institut Fuer Biochemie
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.EBI
J Med Chem 48: 152-62 (2005)
Università
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.BDB
J Med Chem 48: 141-51 (2005)
Merck Research Laboratories
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.EBI
J Med Chem 48: 134-40 (2005)
University of Kansas
Beta-diketo acid pharmacophore hypothesis. 1. Discovery of a novel class of HIV-1 integrase inhibitors.EBI
J Med Chem 48: 111-20 (2005)
University of Southern California
Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.EBI
J Med Chem 48: 100-10 (2005)
National Center For Scientific Research Demokritos
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.EBI
J Med Chem 48: 71-90 (2005)
Amgen
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.EBI
J Med Chem 48: 38-55 (2005)
Abbott Laboratories
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.EBI
J Med Chem 48: 24-7 (2005)
University of Bologna
Control of hepatitis C: a medicinal chemistry perspective.EBI
J Med Chem 48: 1-20 (2005)
University of Wollongong
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.BDB
J Biol Chem 280: 9160-9 (2005)
Genentech
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.BDB
J Pharmacol Exp Ther 313: 293-301 (2005)
University of Li&Eagrove;Ge
Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.EBI
J Nat Prod 67: 2127-9 (2004)
University of British Columbia
A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.EBI
J Nat Prod 67: 2086-9 (2004)
Cetek
Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells.EBI
J Nat Prod 67: 2002-7 (2004)
University of Mississippi
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.EBI
Drug Metab Pharmacokinet 17: 125-9 (2002)
Kyoto University Hospital
The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites.EBI
Drug Metab Pharmacokinet 17: 23-33 (2002)
University of Tokyo
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.EBI
Drug Metab Dispos 33: 537-46 (2005)
Pfizer
Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues.EBI
J Med Chem 47: 6958-63 (2004)
Harvard Medical School
Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.EBI
J Med Chem 47: 6948-57 (2004)
The Danish University of Pharmaceutical Sciences
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.EBI
J Med Chem 47: 6935-47 (2004)
Menarini Ricerche
Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.EBI
J Med Chem 47: 6921-34 (2004)
Serono Pharmaceutical Research Institute
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.EBI
J Med Chem 47: 6893-901 (2004)
Duquesne University
A screening library for peptide activated G-protein coupled receptors. 1. The test set.EBI
J Med Chem 47: 6864-74 (2004)
Neurocrine Biosciences
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).EBI
J Med Chem 47: 6854-63 (2004)
The Johns Hopkins University
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.EBI
J Med Chem 47: 6821-30 (2004)
Neurocrine Biosciences
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors.BDB
J Med Chem 47: 6792-803 (2004)
University of Bari
Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors.EBI
J Med Chem 47: 6768-76 (2004)
Washington State University
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.EBI
J Med Chem 47: 6749-59 (2004)
Université
Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.EBI
J Med Chem 47: 6730-9 (2004)
Duquesne University
Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.EBI
J Med Chem 47: 6716-29 (2004)
University of Maryland
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.EBI
J Med Chem 47: 6702-10 (2004)
University of Florida
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.EBI
J Med Chem 47: 6691-701 (2004)
Indian Institute of Technology
Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.EBI
J Med Chem 47: 6681-90 (2004)
The Scripps Research Institute
A novel class of inhibitors of peptide deformylase discovered through high-throughput screening and virtual ligand screening.EBI
J Med Chem 47: 6669-72 (2004)
Stine-Haskell Research Center
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.BDB
J Med Chem 47: 6666-8 (2004)
Wyeth Research
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.EBI
J Med Chem 47: 6662-5 (2004)
Merck Research Laboratories
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI
J Med Chem 47: 6658-61 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.EBI
J Med Chem 47: 6655-7 (2004)
Abbott Laboratories
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.BDB
J Pharmacol Exp Ther 313: 165-75 (2005)
Abbott Laboratories
5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.EBI
Bioorg Med Chem Lett 15: 459-65 (2004)
Pfizer
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.EBI
Bioorg Med Chem Lett 15: 447-51 (2004)
Merck Research Laboratories
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.EBI
Bioorg Med Chem Lett 15: 439-42 (2004)
University of Alberta
Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.EBI
Bioorg Med Chem Lett 15: 431-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D QSAR studies on GSK-3 inhibition by aloisines.EBI
Bioorg Med Chem Lett 15: 395-9 (2005)
Zhejiang University
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.EBI
Bioorg Med Chem Lett 15: 389-93 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.EBI
Bioorg Med Chem Lett 15: 385-8 (2004)
Korea Research Institute of Bioscience and Biotechnology
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.EBI
Bioorg Med Chem Lett 15: 379-83 (2004)
Wyeth Research
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.EBI
Bioorg Med Chem Lett 15: 373-8 (2004)
Merck Sharp & Dohme Research Laboratories
Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX.EBI
Bioorg Med Chem Lett 15: 367-72 (2004)
Harran University
(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.EBI
Bioorg Med Chem Lett 15: 363-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzoyl 2-methyl indoles as selective PPARgamma modulators.EBI
Bioorg Med Chem Lett 15: 357-62 (2004)
Merck Research Laboratories
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.EBI
Bioorg Med Chem Lett 15: 353-6 (2004)
Korea Research Institute of Bioscience and Biotechnology
(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.EBI
Bioorg Med Chem Lett 15: 349-51 (2004)
Eli Lilly
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.EBI
Bioorg Med Chem Lett 15: 331-5 (2005)
Nagoya City University
QSAR studies on structurally similar 2-(4-methanesulfonylphenyl)pyran-4-ones as selective COX-2 inhibitors: a Hansch approach.EBI
Bioorg Med Chem Lett 15: 313-20 (2004)
Devi Ahilya Vishwavidyalaya
Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.EBI
Bioorg Med Chem Lett 15: 283-6 (2004)
Korea Institute of Science & Technology
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.EBI
Bioorg Med Chem Lett 15: 277-81 (2004)
Athersys
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.EBI
Bioorg Med Chem Lett 15: 271-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.EBI
Bioorg Med Chem Lett 15: 251-4 (2004)
Fujisawa Pharmaceutical
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.BDB
Bioorg Med Chem 13: 425-32 (2005)
Mitsubishi Pharma
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.BDB
J Pharmacol Exp Ther 313: 410-21 (2005)
I.G.B.M.C.
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.EBI
J Med Chem 47: 6645-8 (2004)
University of Bath
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.EBI
J Med Chem 47: 6616-24 (2004)
Università
Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database.EBI
J Med Chem 47: 6609-15 (2004)
University of Mississippi
Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors.EBI
J Med Chem 47: 6603-8 (2004)
Wyeth Research
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.EBI
J Med Chem 47: 6595-602 (2004)
G£Teborg University
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.EBI
J Med Chem 47: 6584-94 (2004)
Boehringer Ingelheim (Canada)
Structure-activity relationship of 6-methylidene penems bearing tricyclic heterocycles as broad-spectrum beta-lactamase inhibitors: crystallographic structures show unexpected binding of 1,4-thiazepine intermediates.EBI
J Med Chem 47: 6556-68 (2004)
Wyeth Research
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.EBI
J Med Chem 47: 6541-6 (2004)
University of Cagliary
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.EBI
J Med Chem 47: 6529-40 (2004)
Leiden/Amsterdam Center For Drug Research
Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer cells.EBI
J Med Chem 47: 6509-18 (2004)
University of Colorado
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.EBI
J Med Chem 47: 6490-8 (2004)
University of Bologna
Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase.EBI
J Med Chem 47: 6485-9 (2004)
Harvard Medical School
Catecholic flavonoids acting as telomerase inhibitors.EBI
J Med Chem 47: 6466-75 (2004)
Bu-Nerviano Medical Sciences
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.EBI
J Med Chem 47: 6455-8 (2004)
University of Illinois At Chicago
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).BDB
J Med Chem 47: 6447-50 (2004)
Merck Research Laboratories
The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease.EBI
J Med Chem 47: 6443-6 (2004)
Mrl Rome
2,3-diaminopyridine bradykinin B1 receptor antagonists.EBI
J Med Chem 47: 6439-42 (2004)
Merck Research Laboratories
Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.EBI
J Med Chem 47: 6435-8 (2004)
Wyeth Research
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.BDB
Bioorg Med Chem 13: 257-64 (2005)
University of Alabama At Birmingham
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.BDB
Bioorg Med Chem 13: 69-75 (2005)
Crefsip
The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors.BDB
Bioorg Med Chem 13: 59-68 (2005)
Pfizer
Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives.EBI
Bioorg Med Chem Lett 15: 235-8 (2004)
University of North Carolina
2,3-Diphenylpropionic acids as potent VLA-4 antagonists.EBI
Bioorg Med Chem Lett 15: 217-20 (2004)
Kaken Pharmaceutical
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.EBI
Bioorg Med Chem Lett 15: 211-5 (2004)
Kyoto Pharmaceutical University
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.EBI
Bioorg Med Chem Lett 15: 195-201 (2004)
Abbott Laboratories
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.EBI
Bioorg Med Chem Lett 15: 185-9 (2004)
Central Pharmaceutical Research Institute
N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.EBI
Bioorg Med Chem Lett 15: 181-3 (2004)
Sejong University
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.EBI
Bioorg Med Chem Lett 15: 171-5 (2004)
Merck Research Laboratories
Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.EBI
Bioorg Med Chem Lett 15: 159-62 (2004)
National Institute of Health Sciences
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.EBI
Bioorg Med Chem Lett 15: 153-8 (2004)
Abbott Laboratories
Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2.EBI
Bioorg Med Chem Lett 15: 145-8 (2004)
Polo Scientifico Università
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.EBI
Bioorg Med Chem Lett 15: 135-8 (2004)
University of The Mediterranean
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.EBI
Bioorg Med Chem Lett 15: 125-8 (2004)
Abbott Laboratories
Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain.EBI
Bioorg Med Chem Lett 15: 121-3 (2004)
University of California San Francisco
Aminothiazole inhibitors of HCV RNA polymerase.EBI
Bioorg Med Chem Lett 15: 115-9 (2004)
Neogenesis Pharmaceuticals
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.EBI
Bioorg Med Chem Lett 15: 107-13 (2004)
Merck Research Laboratories
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.EBI
Bioorg Med Chem Lett 15: 103-6 (2004)
The Scripps Research Institute
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.EBI
Bioorg Med Chem Lett 15: 93-8 (2004)
Abbott Laboratories
Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters.EBI
Bioorg Med Chem Lett 15: 85-7 (2004)
Xenoport
Optimization of pyrrolidinone based HIV protease inhibitors.BDB
Bioorg Med Chem Lett 15: 81-4 (2005)
Glaxosmithkline
2,3-Ethylene- and 2,3-trimethylene-bridged analogues of the group III metabotropic glutamate receptor ligand 2-amino-4-phosphonobutanoic acid.EBI
Bioorg Med Chem Lett 15: 57-60 (2004)
University of Minnesota
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.EBI
Bioorg Med Chem Lett 15: 51-5 (2004)
Eli Lilly
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.EBI
Bioorg Med Chem Lett 15: 41-5 (2004)
Daiichi Pharmaceutical
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.BDB
Bioorg Med Chem Lett 15: 29-35 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.EBI
Bioorg Med Chem Lett 15: 25-8 (2004)
Astrazeneca
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).BDB
Bioorg Med Chem Lett 15: 15-20 (2005)
University of Illinois At Chicago
Structural basis for the activity of drugs that inhibit phosphodiesterases.BDB
Structure 12: 2233-47 (2004)
Plexxikon
Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors.EBI
J Nat Prod 67: 1882-5 (2004)
Instituto De Qu£Mica Da Universidade Estadual Paulista
Isolation of cytochrome P450 inhibitors from strawberry fruit, Fragaria ananassa.EBI
J Nat Prod 67: 1839-41 (2004)
Kanazawa University
Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens.EBI
J Nat Prod 67: 1829-32 (2004)
Ghent University
Mechanism-based inactivation of COX-1 by red wine m-hydroquinones: a structure-activity relationship study.EBI
J Nat Prod 67: 1777-82 (2004)
University of Pennsylvania School of Medicine
Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.EBI
Eur J Pharm Biopharm 59: 17-24 (2004)
Biozentrum of The Martin-Luther-University Halle-Wittenberg
Discovery of novel phenolic antioxidants as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases.EBI
J Med Chem 47: 6420-32 (2004)
Atherogenics
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.EBI
J Med Chem 47: 6401-9 (2004)
Research Triangle Institute
New constrained"molecular tongs" designed to dissociate HIV-1 protease dimer.EBI
J Med Chem 47: 6392-400 (2004)
Paris-Sud University
Synthesis of tropeines and allosteric modulation of ionotropic glycine receptors.EBI
J Med Chem 47: 6384-91 (2004)
Hungarian Academy of Sciences
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.BDB
J Med Chem 47: 6363-72 (2004)
Merck Research Laboratories
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.EBI
J Med Chem 47: 6326-37 (2004)
RhôNe-Poulenc Rorer
Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.EBI
J Med Chem 47: 6311-25 (2004)
Eberhard-Karls-University TüBingen
An in silico approach to discovering novel inhibitors of human sirtuin type 2.EBI
J Med Chem 47: 6292-8 (2004)
University of Kuopio
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI
J Med Chem 47: 6283-91 (2004)
Bristol-Myers Squibb
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.EBI
J Med Chem 47: 6255-69 (2004)
Wyeth Research
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.EBI
J Med Chem 47: 6248-54 (2004)
Leopold-Franzens University of Innsbruck
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.EBI
J Med Chem 47: 6239-47 (2004)
Università
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.EBI
J Med Chem 47: 6218-29 (2004)
Biogen Idec
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.EBI
J Med Chem 47: 6195-206 (2004)
Université
Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.EBI
J Med Chem 47: 6187-94 (2004)
Ghent University
alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.EBI
J Med Chem 47: 6160-73 (2004)
Universit£
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.EBI
J Med Chem 47: 6128-36 (2004)
National Institute On Drug Abuse
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.EBI
J Med Chem 47: 6124-7 (2004)
Roche Palo Alto
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.BDB
J Med Chem 47: 6117-9 (2004)
Merck Research Laboratories
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.BDB
J Am Chem Soc 126: 15405-11 (2004)
Weizmann Institute of Science
Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim.BDB
Antimicrob Agents Chemother 48: 4643-9 (2004)
Oklahoma State University At Stillwater
Pharmacological inhibitors of glycogen synthase kinase 3.EBI
Trends Pharmacol Sci 25: 471-80 (2004)
The Rockefeller University
Synthesis and urease enzyme inhibitory effects of some dicoumarols.BDB
J Enzyme Inhib Med Chem 19: 367-71 (2004)
University of Karachi
Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.EBI
Bioorg Med Chem Lett 14: 6113-6 (2004)
Eli Lilly
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.EBI
Bioorg Med Chem Lett 14: 6107-11 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.BDB
Bioorg Med Chem Lett 14: 6095-9 (2004)
Avenida De La Industria
QSAR modelling of HIV-1 reverse transcriptase inhibition by benzoxazinones using a combination of P_VSA and pharmacophore feature descriptors.EBI
Bioorg Med Chem Lett 14: 6089-94 (2004)
S.G.S.I.T.S.
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.EBI
Bioorg Med Chem Lett 14: 6083-7 (2004)
University of Newcastle
Novel diarylsulfonylurea derivatives as potent antimitotic agents.EBI
Bioorg Med Chem Lett 14: 6075-8 (2004)
Lg Life Sciences
Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors.EBI
Bioorg Med Chem Lett 14: 6071-4 (2004)
Department of Life Science and National Research Laboratory of Proteolysis
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.EBI
Bioorg Med Chem Lett 14: 6061-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.EBI
Bioorg Med Chem Lett 14: 6053-6 (2004)
Aventis Pharmaceuticals
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.EBI
Bioorg Med Chem Lett 14: 6049-52 (2004)
Nitromed
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.EBI
Bioorg Med Chem Lett 14: 6045-8 (2004)
Merck Research Laboratories
Antiviral compounds from traditional Chinese medicines Galla Chinese as inhibitors of HCV NS3 protease.EBI
Bioorg Med Chem Lett 14: 6041-4 (2004)
Peking University
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.EBI
Bioorg Med Chem Lett 14: 6017-21 (2004)
Cv Therapeutics
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.EBI
Bioorg Med Chem Lett 14: 6011-6 (2004)
Eli Lilly
Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters.EBI
Bioorg Med Chem Lett 14: 6007-10 (2004)
Organix
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.EBI
Bioorg Med Chem Lett 14: 6001-6 (2004)
Pennsylvania State University
Alpha-1-C-alkyl-1-deoxynojirimycin derivatives as potent and selective inhibitors of intestinal isomaltase: remarkable effect of the alkyl chain length on glycosidase inhibitory profile.EBI
Bioorg Med Chem Lett 14: 5991-5 (2004)
Universit£
Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.EBI
Bioorg Med Chem Lett 14: 5975-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.EBI
Bioorg Med Chem Lett 14: 5963-6 (2004)
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.EBI
Bioorg Med Chem Lett 14: 5959-62 (2004)
Dainippon Pharmaceutical
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.EBI
J Med Chem 47: 6108-11 (2004)
University of Alberta
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.EBI
J Med Chem 47: 6070-81 (2004)
Universit£
Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.EBI
J Med Chem 47: 6034-41 (2004)
Virginia Commonwealth University
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.EBI
J Med Chem 47: 6025-33 (2004)
University of Florida
AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.EBI
J Med Chem 47: 6009-19 (2004)
Uppsala University
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.EBI
J Med Chem 47: 5995-6008 (2004)
Uppsala University
Building predictive models for protein tyrosine phosphatase 1B inhibitors based on discriminating structural features by reassembling medicinal chemistry building blocks.EBI
J Med Chem 47: 5984-94 (2004)
Leadscope
5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials.EBI
J Med Chem 47: 5972-83 (2004)
Université
Tetrahydrobiopterin binding to aromatic amino acid hydroxylases. Ligand recognition and specificity.EBI
J Med Chem 47: 5962-71 (2004)
University of Bergen
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.EBI
J Med Chem 47: 5953-61 (2004)
Uppsala University
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.BDB
J Med Chem 47: 5945-52 (2004)
University of Bologna
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.BDB
J Med Chem 47: 5912-22 (2004)
University of Oxford
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.BDB
J Med Chem 47: 5894-911 (2004)
Bristol-Myers Squibb
Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase.EBI
J Med Chem 47: 5860-71 (2004)
Universit£T M£Nster
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.EBI
J Med Chem 47: 5833-6 (2004)
Novartis Institutes For Biomedical Research
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.EBI
J Med Chem 47: 5829-32 (2004)
Merck Sharp & Dohme Research Laboratories
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.EBI
J Med Chem 47: 5825-8 (2004)
Merck Research Laboratories
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.EBI
J Med Chem 47: 5821-4 (2004)
Acenta Discovery
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.BDB
Biochemistry 43: 14500-7 (2004)
Glaxosmithkline
Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors.BDB
Bioorg Chem 32: 494-503 (2004)
BiomolÉCules Et Cibles Cellulaires Tumorales
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).BDB
J Mol Biol 344: 527-47 (2004)
Celera
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.BDB
Bioorg Med Chem 12: 6171-82 (2004)
Yamanouchi Pharmaceutical
The core structures of roseophilin and the prodigiosin alkaloids define a new class of protein tyrosine phosphatase inhibitors.BDB
Chembiochem 5: 1575-9 (2004)
Max-Planck-Institut FÜR Kohlenforschung
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.BDB
J Pharmacol Exp Ther 312: 1114-23 (2005)
Section of Pharmacology
Efficient evaluation of binding free energy using continuum electrostatics solvation.EBI
J Med Chem 47: 5791-7 (2004)
University of ZüRich
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.EBI
J Med Chem 47: 5783-90 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.EBI
J Med Chem 47: 5690-9 (2004)
University of Colorado
Structural characterization and pharmacology of a potent (Cys101-Cys119, Cys110-Cys117) bicyclic agouti-related protein (AGRP) melanocortin receptor antagonist.EBI
J Med Chem 47: 5662-73 (2004)
University of Florida
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.EBI
J Med Chem 47: 5620-9 (2004)
Budapest University of Technology and Economics
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.EBI
J Med Chem 47: 5612-5 (2004)
Trinity College Dublin
A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors.EBI
J Med Chem 47: 5605-7 (2004)
University of Kuopio
NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs.EBI
J Med Chem 47: 5597-600 (2004)
Universit£
Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.EBI
J Med Chem 47: 5593-6 (2004)
X-Ceptor Therapeutics
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.BDB
J Am Chem Soc 126: 14224-33 (2004)
Nagoya Institute of Technology
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.EBI
Bioorg Med Chem Lett 14: 5937-41 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.EBI
Bioorg Med Chem Lett 14: 5925-9 (2004)
Kyoto Pharmaceutical University
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.EBI
Bioorg Med Chem Lett 14: 5907-11 (2004)
Merck Research Laboratories
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.EBI
Bioorg Med Chem Lett 14: 5899-902 (2004)
Schering-Plough Research Institute
Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.EBI
Bioorg Med Chem Lett 14: 5881-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.EBI
Bioorg Med Chem Lett 14: 5867-72 (2004)
Merck Research Laboratories
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.EBI
Bioorg Med Chem Lett 14: 5863-6 (2004)
Polish Academy of Sciences
Evaluation of by disubstituted acridone derivatives as telomerase inhibitors: the importance of G-quadruplex binding.EBI
Bioorg Med Chem Lett 14: 5845-9 (2004)
University of London
Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers.EBI
Bioorg Med Chem Lett 14: 5827-30 (2004)
Università
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI
Bioorg Med Chem Lett 14: 5817-22 (2004)
Merck
Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands.EBI
Bioorg Med Chem Lett 14: 5813-6 (2004)
University of Michigan
Synthesis of small molecule CDC25 phosphatases inhibitors.EBI
Bioorg Med Chem Lett 14: 5809-12 (2004)
Institut Henri Beaufour
Inactivation of human S-adenosylhomocysteine hydrolase by covalent labeling of cysteine 195 with thionucleoside derivatives.EBI
Bioorg Med Chem Lett 14: 5803-7 (2004)
Umr 6519
Inactivation of S-adenosylhomocysteine hydrolase with haloethyl and dihalocyclopropyl esters derived from homoadenosine-6'-carboxylic acid.EBI
Bioorg Med Chem Lett 14: 5799-802 (2004)
Umr 6519
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.EBI
Bioorg Med Chem Lett 14: 5793-7 (2004)
Novartis Institutes For Biomedical Research
Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties.EBI
Bioorg Med Chem Lett 14: 5781-6 (2004)
Universit£
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide.EBI
Bioorg Med Chem Lett 14: 5775-80 (2004)
Universit£
Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.EBI
Bioorg Med Chem Lett 14: 5769-73 (2004)
Universit£
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.EBI
Bioorg Med Chem Lett 14: 5763-7 (2004)
Università
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.BDB
Bioorg Med Chem Lett 14: 5751-5 (2004)
Schering-Plough Research Institute
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors.EBI
Bioorg Med Chem Lett 14: 5739-42 (2004)
Florida A&M University
Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.BDB
J Enzyme Inhib Med Chem 19: 269-73 (2004)
UniversitÀ Degli Studi Di Firenze
DNA polymerase beta lyase inhibitors from Maytenus putterlickoides.EBI
J Nat Prod 67: 1744-7 (2004)
University of Virginia
Marine sesquiterpenoids that inhibit the lyase activity of DNA polymerase beta.EBI
J Nat Prod 67: 1716-8 (2004)
Virginia Polytechnic Institute and State University
Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.EBI
J Nat Prod 67: 1681-4 (2004)
Merlion Pharmaceuticals
Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A).EBI
Eur J Pharmacol 503: 25-30 (2004)
Kyoto University Hospital
Dihydrexidine--the first full dopamine D1 receptor agonist.BDB
CNS Drug Rev 10: 230-42 (2004)
Karolinska Institutet
Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.BDB
Biochemistry 43: 13380-9 (2004)
University of Alabama At Birmingham
Multicopy suppressors for novel antibacterial compounds reveal targets and drug efflux susceptibility.BDB
Chem Biol 11: 1423-30 (2004)
Mcmaster University
Disruption of protein-membrane binding and identification of small-molecule inhibitors of coagulation factor VIII.BDB
Chem Biol 11: 1413-22 (2004)
University of Washington
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.EBI
Bioorg Med Chem Lett 14: 5709-12 (2004)
Università
Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives.EBI
Bioorg Med Chem Lett 14: 5703-7 (2004)
Università
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.EBI
Bioorg Med Chem Lett 14: 5693-7 (2004)
Adolor
Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.BDB
Bioorg Med Chem Lett 14: 5689-92 (2004)
Glaxosmithkline
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.BDB
Bioorg Med Chem Lett 14: 5685-7 (2004)
Glaxosmithkline
Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation.EBI
Bioorg Med Chem Lett 14: 5667-72 (2004)
Anadys Pharmaceuticals
Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives.EBI
Bioorg Med Chem Lett 14: 5651-4 (2004)
Cardiff University
Synthesis of 5'-substituted fluoro-neplanocin A analogues: importance of a hydrogen bonding donor at 5'-position for the inhibitory activity of S-adenosylhomocysteine hydrolase.EBI
Bioorg Med Chem Lett 14: 5641-4 (2004)
Pusan National University
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.EBI
Bioorg Med Chem Lett 14: 5635-9 (2004)
Harvard Medical School
Synthesis of 61-bis(1-adamantylcarbamoyl)-1,2-methano[60]fullerene and its antagonistic effect on haloperidol-induced catalepsy in mice.EBI
Bioorg Med Chem Lett 14: 5619-21 (2004)
Kyushu University
QSAR modeling of the MAO inhibitory activity of xanthones derivatives.EBI
Bioorg Med Chem Lett 14: 5611-7 (2004)
Unne
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.EBI
Bioorg Med Chem Lett 14: 5605-9 (2004)
Neurocrine Biosciences
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 14: 5599-603 (2004)
Merck Research Laboratories
Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.EBI
Bioorg Med Chem Lett 14: 5595-8 (2004)
National Cancer Institute-Frederick
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.EBI
Bioorg Med Chem Lett 14: 5591-4 (2004)
Ucb Pharma
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.EBI
Bioorg Med Chem Lett 14: 5573-7 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.BDB
Bioorg Med Chem Lett 14: 5543-6 (2004)
Abbott Laboratories
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.EBI
Bioorg Med Chem Lett 14: 5533-5 (2004)
A.V. Bogatsky Physico-Chemical Institute of The National Academy of Sciences of Ukraine
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.EBI
Bioorg Med Chem Lett 14: 5521-5 (2004)
Pfizer
Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.EBI
Bioorg Med Chem Lett 14: 5513-9 (2004)
Purdue Pharma
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.EBI
Bioorg Med Chem Lett 14: 5509-12 (2004)
Pfizer
A 13C NMR approach to categorizing potential limitations of alpha,beta-unsaturated carbonyl systems in drug-like molecules.EBI
Bioorg Med Chem Lett 14: 5503-7 (2004)
Abbott Bioresearch Center
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.EBI
Bioorg Med Chem Lett 14: 5499-502 (2004)
Wyeth Research
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.EBI
Bioorg Med Chem Lett 14: 5493-8 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.BDB
Bioorg Med Chem Lett 14: 5489-91 (2004)
Dupont Pharmaceuticals
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.EBI
Bioorg Med Chem Lett 14: 5485-8 (2004)
Merck Research Laboratories
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.EBI
Bioorg Med Chem Lett 14: 5481-4 (2004)
Merck Research Laboratories
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.EBI
Bioorg Med Chem Lett 14: 5477-80 (2004)
Merck Research Laboratories
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.EBI
Bioorg Med Chem Lett 14: 5473-6 (2004)
Merck Research Laboratories
Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13).EBI
J Med Chem 47: 5587-90 (2004)
Friedrich-Alexander University
Spectroscopic studies of diketoacids-metal interactions. A probing tool for the pharmacophoric intermetallic distance in the HIV-1 integrase active site.EBI
J Med Chem 47: 5583-6 (2004)
Université
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.EBI
J Med Chem 47: 5555-66 (2004)
Yale University
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.EBI
J Med Chem 47: 5535-40 (2004)
Universit£
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.EBI
J Med Chem 47: 5492-500 (2004)
University of Kansas
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.EBI
J Med Chem 47: 5467-81 (2004)
Pfizer
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.EBI
J Med Chem 47: 5451-66 (2004)
State University of Groningen
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.EBI
J Med Chem 47: 5441-50 (2004)
Leiden University
Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.EBI
J Med Chem 47: 5433-40 (2004)
Universidad De Grenada
A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.EBI
J Med Chem 47: 5418-26 (2004)
Walter Reed Army Institute of Research
Identification and specificity studies of small-molecule ligands for SH3 protein domains.EBI
J Med Chem 47: 5405-17 (2004)
The University of Adelaide
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.EBI
J Med Chem 47: 5393-404 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.EBI
J Med Chem 47: 5381-92 (2004)
Philipps-Universit£T Marburg
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.EBI
J Med Chem 47: 5367-80 (2004)
Eli Lilly
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.EBI
J Med Chem 47: 5356-66 (2004)
Boehringer Ingelheim Pharmaceuticals
Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition.EBI
J Med Chem 47: 5340-6 (2004)
University of Leicester
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.EBI
J Med Chem 47: 5336-9 (2004)
Italy. Vinc
Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.BDB
Br J Pharmacol 143: 649-61 (2004)
Johnson & Johnson Pharmaceutical Research and Development
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.BDB
Cancer Res 64: 7099-109 (2004)
Bayer Pharmaceuticals
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.EBI
J Med Chem 47: 5318-29 (2004)
Instituto De Qu£Mica M£Dica (Csic)
Design and synthesis of novel indole beta-diketo acid derivatives as HIV-1 integrase inhibitors.EBI
J Med Chem 47: 5298-310 (2004)
Università
Synthesis and evaluation of nitrofuranylamides as novel antituberculosis agents.EBI
J Med Chem 47: 5276-83 (2004)
University of Tennessee Health Science Center
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.EBI
J Med Chem 47: 5258-64 (2004)
University of Pennsylvania
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects.EBI
J Med Chem 47: 5251-7 (2004)
Florida International University
Subtype selective substrates for histone deacetylases.EBI
J Med Chem 47: 5235-43 (2004)
Westf£Lische Wilhelms-Universit£T M£Nster
Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library.EBI
J Med Chem 47: 5224-9 (2004)
University of Florence
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].EBI
J Med Chem 47: 5198-203 (2004)
Universit£
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.EBI
J Med Chem 47: 5167-82 (2004)
Daiichi Pharmaceutical
Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization.EBI
J Med Chem 47: 5126-39 (2004)
Purdue University
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.EBI
J Med Chem 47: 5101-13 (2004)
Wayne State University
Identification and characterization of small molecule inhibitors of the calcium-dependent S100B-p53 tumor suppressor interaction.EBI
J Med Chem 47: 5085-93 (2004)
University of Maryland
Soft docking and multiple receptor conformations in virtual screening.EBI
J Med Chem 47: 5076-84 (2004)
University of California San Francisco
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.EBI
J Med Chem 47: 5069-75 (2004)
University of Bath
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.EBI
J Med Chem 47: 5057-68 (2004)
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.EBI
J Med Chem 47: 5049-56 (2004)
Glaxosmithkline
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.EBI
J Med Chem 47: 5021-40 (2004)
Wyeth Research
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.EBI
J Med Chem 47: 5009-20 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.EBI
J Med Chem 47: 4998-5008 (2004)
Università
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.EBI
J Med Chem 47: 4985-8 (2004)
The Pennsylvania State University
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 14: 5445-8 (2004)
Glaxosmithkline
Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions.EBI
Bioorg Med Chem Lett 14: 5435-9 (2004)
Universit£
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.EBI
Bioorg Med Chem Lett 14: 5427-33 (2004)
Universit£
Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.EBI
Bioorg Med Chem Lett 14: 5413-6 (2004)
Deltagen Research Laboratories
Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives.EBI
Bioorg Med Chem Lett 14: 5407-11 (2004)
Institute For Bio-Medical Research
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.EBI
Bioorg Med Chem Lett 14: 5389-94 (2004)
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.EBI
Bioorg Med Chem Lett 14: 5383-7 (2004)
Astrazeneca
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.EBI
Bioorg Med Chem Lett 14: 5377-81 (2004)
Research Triangle Institute
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 14: 5371-6 (2004)
Abbott Laboratories
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 14: 5367-70 (2004)
Abbott Laboratories
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.EBI
Bioorg Med Chem Lett 14: 5343-6 (2004)
Crest Research Project
Three new compounds from the plant Lippia alva as inhibitors of chemokine receptor 5 (CCR5).EBI
Bioorg Med Chem Lett 14: 5339-42 (2004)
Schering-Plough Research Institute
HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY.EBI
Bioorg Med Chem Lett 14: 5333-7 (2004)
Virochem Pharma
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.EBI
Bioorg Med Chem Lett 14: 5329-32 (2004)
Merck Research Laboratories
Substrate analogs for the investigation of deoxyxylulose 5-phosphate reductoisomerase inhibition: synthesis and evaluation.EBI
Bioorg Med Chem Lett 14: 5309-12 (2004)
Oregon State University
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.EBI
Bioorg Med Chem Lett 14: 5301-4 (2004)
University of Pennsylvania
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.EBI
Bioorg Med Chem Lett 14: 5295-300 (2004)
Maxim Pharmaceuticals
Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands.EBI
Bioorg Med Chem Lett 14: 5285-8 (2004)
The University of Michigan Medical School
Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity.EBI
Bioorg Med Chem Lett 14: 5281-4 (2004)
Wyeth Research
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.EBI
Bioorg Med Chem Lett 14: 5275-9 (2004)
Purdue Pharma
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.BDB
Bioorg Med Chem Lett 14: 5269-73 (2004)
Bristol-Myers Squibb
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.BDB
Bioorg Med Chem Lett 14: 5263-7 (2004)
Bristol-Myers Squibb
Synthesis and enzymatic evaluation of xanthine oxidase-activated prodrugs based on inhibitors of thymidine phosphorylase.EBI
Bioorg Med Chem Lett 14: 5247-50 (2004)
University of Manchester
Design and synthesis of indole and tetrahydroisoquinoline hydantoin derivatives as human chymase inhibitors.BDB
J Enzyme Inhib Med Chem 19: 137-43 (2004)
UniversitÉ
Biscoumarin derivatives from Edgeworthia gardneri that inhibit the lyase activity of DNA polymerase beta.EBI
J Nat Prod 67: 1608-10 (2004)
University of Virginia
BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.EBI
J Nat Prod 67: 1528-31 (2004)
Boehringer Ingelheim Pharma Gmbh And
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.EBI
Biopharm Drug Dispos 25: 283-9 (2004)
Tufts University School of Medicine
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.BDB
J Pharmacol Exp Ther 312: 220-30 (2005)
Temple University
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.EBI
Bioorg Med Chem Lett 14: 5227-32 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.EBI
Bioorg Med Chem Lett 14: 5223-6 (2004)
Abbott Laboratories
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors.EBI
Bioorg Med Chem Lett 14: 5219-22 (2004)
Purdue University
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.EBI
Bioorg Med Chem Lett 14: 5215-8 (2004)
Upres Ea 1085 BiomoléCules Et Cibles Cellulaires Tumorales
Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.EBI
Bioorg Med Chem Lett 14: 5205-9 (2004)
University of Mainz
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.EBI
Bioorg Med Chem Lett 14: 5199-203 (2004)
University of California San Francisco
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.EBI
Bioorg Med Chem Lett 14: 5193-8 (2004)
Daiichi Pharmaceutical
Synthesis of 5a-carba-hexopyranoses and hexopyranosylamines, as well as 5a,5a'-dicarbadisaccharides, from 3,8-dioxatricyclo[4.2.1.0(2,4)]nonan-9-ol: glycosidase inhibitory activity of N-substituted 5a-carba-beta-gluco- and beta-galactopyranosylamines, and derivatives thereof.EBI
Bioorg Med Chem Lett 14: 5183-8 (2004)
Keio University
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.EBI
Bioorg Med Chem Lett 14: 5171-4 (2004)
Central Pharmaceutical Research Institute
N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.EBI
Bioorg Med Chem Lett 14: 5157-60 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.EBI
Bioorg Med Chem Lett 14: 5151-5 (2004)
Merck
Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors.EBI
Bioorg Med Chem Lett 14: 5121-5 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).EBI
Bioorg Med Chem Lett 14: 5113-6 (2004)
University of Southern California
Benzothiophene and naphthalene derived constrained SERMs.EBI
Bioorg Med Chem Lett 14: 5103-6 (2004)
Eli Lilly
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.EBI
Bioorg Med Chem Lett 14: 5095-8 (2004)
Abbott Laboratories
Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.EBI
Bioorg Med Chem Lett 14: 5085-8 (2004)
Mrl Rome
Development of a polyvalent assay system for lead identification.EBI
Bioorg Med Chem Lett 14: 5081-3 (2004)
Wyeth Research
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.EBI
Bioorg Med Chem Lett 14: 5075-80 (2004)
7Tm Pharma
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.EBI
Bioorg Med Chem Lett 14: 5067-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.EBI
Bioorg Med Chem Lett 14: 5057-62 (2004)
Abbott Laboratories
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.EBI
Bioorg Med Chem Lett 14: 5045-50 (2004)
Purdue Pharma
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.BDB
Biochemistry 43: 12141-51 (2004)
University of Florida College of Medicine
Molecular design of cholesterols as inhibitors of DNA polymerase alpha.EBI
J Med Chem 47: 4971-4 (2004)
Frontier Research Center For Genome & Drug Discovery
A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.EBI
J Med Chem 47: 4950-7 (2004)
Novartis Institutes For Biomedical Research and Novartis Pharma Development
Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.EBI
J Med Chem 47: 4941-9 (2004)
The Ohio State University
Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.EBI
J Med Chem 47: 4881-90 (2004)
Università
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints.EBI
J Med Chem 47: 4875-80 (2004)
Telik
Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).EBI
J Med Chem 47: 4858-64 (2004)
National Cancer Institute-Frederick
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.EBI
J Med Chem 47: 4829-37 (2004)
Merck Research Laboratories
Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.EBI
J Med Chem 47: 4799-801 (2004)
Johnson & Johnson Pharmaceutical Research and Development
Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group.BDB
Chembiochem 5: 1270-4 (2004)
Laboratorium FÜR Organische Chemie
Inhibition of Golgi mannosidase II with mannostatin A analogues: synthesis, biological evaluation, and structure-activity relationship studies.BDB
Chembiochem 5: 1220-7 (2004)
University of Georgia
Transport characteristics of fexofenadine in the Caco-2 cell model.EBI
Pharm Res 21: 1398-404 (2004)
Uppsala University
Non-peptide oxytocin agonists.EBI
Bioorg Med Chem Lett 14: 4585-9 (2004)
Ferring Research
SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.EBI
Bioorg Med Chem Lett 14: 4575-9 (2004)
Merck Research Laboratories
Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors.EBI
Bioorg Med Chem Lett 14: 4569-73 (2004)
Virginia Commonwealth University
Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the methanoarchaeon Methanobacterium thermoautotrophicum (Cab) with anions.EBI
Bioorg Med Chem Lett 14: 4563-7 (2004)
Universit£
Discovery of new chemical leads for prostaglandin D2 receptor antagonists.EBI
Bioorg Med Chem Lett 14: 4557-62 (2004)
Minase Research Institute
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.EBI
Bioorg Med Chem Lett 14: 4553-5 (2004)
3-Dimensional Pharmaceuticals
Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.EBI
Bioorg Med Chem Lett 14: 4549-51 (2004)
Guilford Pharmaceuticals
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.EBI
Bioorg Med Chem Lett 14: 4539-44 (2004)
Merck Research Laboratory
AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey.EBI
Bioorg Med Chem Lett 14: 4525-8 (2004)
Alcon Research
Substituted 6-phenyl-pyridin-2-ylamines: selective and potent inhibitors of neuronal nitric oxide synthase.EBI
Bioorg Med Chem Lett 14: 4511-4 (2004)
Pfizer
Isoindolinone ureas: a novel class of KDR kinase inhibitors.BDB
Bioorg Med Chem Lett 14: 4505-9 (2004)
Abbott Laboratories
The purine transferase from Trypanosoma cruzi as a potential target for bisphosphonate-based chemotherapeutic compounds.EBI
Bioorg Med Chem Lett 14: 4501-4 (2004)
Universidad De Buenos Aires
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.EBI
Bioorg Med Chem Lett 14: 4467-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.EBI
Bioorg Med Chem Lett 14: 4461-5 (2004)
Korea Research Institute of Chemical Technology
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.EBI
Bioorg Med Chem Lett 14: 4453-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.EBI
Bioorg Med Chem Lett 14: 4449-52 (2004)
Biovitrum
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.EBI
Bioorg Med Chem Lett 14: 4445-8 (2004)
Biovitrum
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.EBI
Bioorg Med Chem Lett 14: 4417-23 (2004)
Neurocrine Biosciences
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.EBI
Bioorg Med Chem Lett 14: 4411-5 (2004)
Merck Research Laboratories
Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.EBI
Bioorg Med Chem Lett 14: 4395-8 (2004)
Conjuchem
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.EBI
Bioorg Med Chem Lett 14: 4379-82 (2004)
Brigham & Women'S Hospital
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.EBI
Bioorg Med Chem Lett 14: 4375-8 (2004)
Glaxosmithkline
Heterologous expression of human {alpha}6{beta}4{beta}3{alpha}5 nicotinic acetylcholine receptors: binding properties consistent with their natural expression require quaternary subunit assembly including the {alpha}5 subunit.BDB
J Pharmacol Exp Ther 312: 619-26 (2005)
Targacept
Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.BDB
J Pharmacol Exp Ther 312: 561-70 (2005)
University of Piemonte Orientale
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.BDB
J Biol Chem 279: 50555-65 (2004)
The Scripps Research Institute
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI
Bioorg Med Chem Lett 14: 5007-11 (2004)
Eli Lilly
Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase.EBI
Bioorg Med Chem Lett 14: 4999-5002 (2004)
Novartis Institutes For Biomedical Research Gdc
Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate.EBI
Bioorg Med Chem Lett 14: 4979-82 (2004)
University of Kentucky
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.EBI
Bioorg Med Chem Lett 14: 4967-73 (2004)
Neurocrine Biosciences
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.EBI
Bioorg Med Chem Lett 14: 4945-8 (2004)
Procter and Gamble Pharmaceuticals
Synthesis and evaluation of novel oxazoline MMP inhibitors.EBI
Bioorg Med Chem Lett 14: 4935-9 (2004)
North Dakota State University
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.EBI
Bioorg Med Chem Lett 14: 4925-9 (2004)
Wyeth Research
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.EBI
Bioorg Med Chem Lett 14: 4915-8 (2004)
Athersys
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.EBI
Bioorg Med Chem Lett 14: 4911-4 (2004)
University of Alberta
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.EBI
Bioorg Med Chem Lett 14: 4903-6 (2004)
University of Virginia
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.EBI
Bioorg Med Chem Lett 14: 4897-902 (2004)
Glaxosmithkline
Discovery of orally active prostaglandin D2 receptor antagonists.EBI
Bioorg Med Chem Lett 14: 4891-5 (2004)
Minase Research Institute
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.EBI
Bioorg Med Chem Lett 14: 4883-6 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.EBI
Bioorg Med Chem Lett 14: 4879-82 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.EBI
Bioorg Med Chem Lett 14: 4873-7 (2004)
Abbott Laboratories
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.EBI
Bioorg Med Chem Lett 14: 4867-72 (2004)
In Vivo Sciences Millennium Pharmaceuticals
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.EBI
Bioorg Med Chem Lett 14: 4861-6 (2004)
Merck Research Laboratories
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.EBI
Bioorg Med Chem Lett 14: 4851-4 (2004)
Ewha Womans University
N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.EBI
Bioorg Med Chem Lett 14: 4847-50 (2004)
Nps Pharmaceuticals
Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.EBI
Bioorg Med Chem Lett 14: 4843-6 (2004)
Johnson & Johnson Pharmaceutical Research and Development
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.EBI
Bioorg Med Chem Lett 14: 4839-42 (2004)
University of Cincinnati
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.EBI
Bioorg Med Chem Lett 14: 4835-8 (2004)
Biogen Idec
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.EBI
Bioorg Med Chem Lett 14: 4831-4 (2004)
Biogen Idec
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.EBI
Bioorg Med Chem Lett 14: 4819-23 (2004)
Aventis Pharmaceuticals
Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides.EBI
Bioorg Med Chem Lett 14: 4815-7 (2004)
University of Georgia
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.EBI
J Med Chem 47: 4787-98 (2004)
Neurocrine Biosciences
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).EBI
J Med Chem 47: 4774-86 (2004)
Wyeth Research
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.EBI
J Med Chem 47: 4766-73 (2004)
Cv Therapeutics
Dipeptidomimetic ketomethylene isosteres as pro-moieties for drug transport via the human intestinal di-/tripeptide transporter hPEPT1: design, synthesis, stability, and biological investigations.EBI
J Med Chem 47: 4755-65 (2004)
University of Tromsø
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.EBI
J Med Chem 47: 4741-54 (2004)
Pharmaceutical Research Institute
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.BDB
J Med Chem 47: 4716-30 (2004)
Glaxosmithkline
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.EBI
J Med Chem 47: 4684-92 (2004)
Merck
Indolebutylamines as selective 5-HT(1A) agonists.EBI
J Med Chem 47: 4677-83 (2004)
Merck
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.EBI
J Med Chem 47: 4645-8 (2004)
TBA
Potent and orally bioavailable non-peptide antagonists at the human bradykinin B(1) receptor based on a 2-alkylamino-5-sulfamoylbenzamide core.EBI
J Med Chem 47: 4642-4 (2004)
TBA
Virulence regulation and quorum sensing in staphylococcal infections: competitive AgrC antagonists as quorum sensing inhibitors.EBI
J Med Chem 47: 4633-41 (2004)
University of Nottingham
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.EBI
J Nat Prod 67: 1291-4 (2004)
Griffith University
An analysis of phakellin and oroidin structures stimulated by further study of an Agelas sponge.EBI
J Nat Prod 67: 1256-61 (2004)
University of California
Intrinsic and acquired forms of resistance against the anticancer ruthenium compound KP1019 [indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A).EBI
J Pharmacol Exp Ther 312: 281-9 (2004)
Institute of Cancer Research
Design and synthesis of substituted N-methylbenzamide analogues derived from SR 48,968 as neurokinin-2 receptor antagonists.EBI
Bioorg Med Chem Lett 14: 4779-82 (2004)
St. John'S University
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.EBI
Bioorg Med Chem Lett 14: 4771-7 (2004)
China Pharmaceutical University
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.EBI
Bioorg Med Chem Lett 14: 4763-6 (2004)
Merck
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.EBI
Bioorg Med Chem Lett 14: 4759-62 (2004)
Merck
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 14: 4741-5 (2004)
Roche Palo Alto
A novel cyclic enkephalin analogue with potent opioid antagonist activity.EBI
Bioorg Med Chem Lett 14: 4731-3 (2004)
Clinical Research Institute of Montreal
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.EBI
Bioorg Med Chem Lett 14: 4727-30 (2004)
Pfizer
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.EBI
Bioorg Med Chem Lett 14: 4705-10 (2004)
Novartis Horsham Research Centre
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.EBI
Bioorg Med Chem Lett 14: 4697-9 (2004)
Virginia Commonwealth University
Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA:cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size.EBI
Bioorg Med Chem Lett 14: 4677-81 (2004)
National Research Laboratory of Lipid Metabolism and Atherosclerosis
Exploring QSAR with E-state index: selectivity requirements for COX-2 versus COX-1 binding of terphenyl methyl sulfones and sulfonamides.EBI
Bioorg Med Chem Lett 14: 4665-70 (2004)
Jadavpur University
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.EBI
Bioorg Med Chem Lett 14: 4659-63 (2004)
Universit£T Regensburg
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.BDB
Bioorg Med Chem Lett 14: 4651-4 (2004)
Merck Research Laboratories
Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.BDB
Bioorg Med Chem Lett 14: 4639-42 (2004)
Shanghai Institute of Materia Medica
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.EBI
Bioorg Med Chem Lett 14: 4627-31 (2004)
Pfizer
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.EBI
Bioorg Med Chem Lett 14: 4623-6 (2004)
Pfizer
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.EBI
Bioorg Med Chem Lett 14: 4607-13 (2004)
Pfizer
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 14: 4603-6 (2004)
Abbott Laboratories
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 370: 114-23 (2004)
Vernalis Research
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".EBI
J Med Chem 47: 4613-26 (2004)
Uppsala University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.EBI
J Med Chem 47: 4588-94 (2004)
Research Triangle Institute
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.EBI
J Med Chem 47: 4570-87 (2004)
Taisho Pharmaceutical
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.EBI
J Med Chem 47: 4559-69 (2004)
Universit£
High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor.EBI
J Med Chem 47: 4530-7 (2004)
Monash University (Parkville Campus)
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI
J Med Chem 47: 4517-29 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.EBI
J Med Chem 47: 4494-506 (2004)
Glaxosmithkline
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity toward the alpha2-adrenoceptor.EBI
J Med Chem 47: 4483-93 (2004)
University of Kansas
Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis.EBI
J Med Chem 47: 4471-82 (2004)
Universitat De Barcelona
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.BDB
J Med Chem 47: 4417-26 (2004)
Abbott Laboratories
Molecular recognition in purinergic receptors. 2. Diastereoselectivity of the h-P2Y1-receptor.EBI
J Med Chem 47: 4405-16 (2004)
Bar-Ilan University
Determinants of retinoid X receptor transcriptional antagonism.EBI
J Med Chem 47: 4360-72 (2004)
Institute
Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions.EBI
Cancer Res 64: 5804-11 (2004)
The Netherlands Cancer Institute
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.BDB
Br J Pharmacol 143: 81-90 (2004)
Abbott Laboratories
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.EBI
J Med Chem 47: 4300-15 (2004)
Umr Cnrs/Ulp 7081
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.EBI
J Med Chem 47: 4291-9 (2004)
Biogen Idec
Identification of structurally diverse growth hormone secretagogue agonists by virtual screening and structure-activity relationship analysis of 2-formylaminoacetamide derivatives.EBI
J Med Chem 47: 4286-90 (2004)
Institute For Life Science Research
2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase.EBI
J Med Chem 47: 4268-76 (2004)
Novartis Institute For Biomedical Research Vienna
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.EBI
J Med Chem 47: 4258-67 (2004)
Università
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.EBI
J Med Chem 47: 4247-57 (2004)
National Health Research Institutes
Design, synthesis, and biological evaluation of new cyclic disulfide decapeptides that inhibit the binding of AP-1 to DNA.EBI
J Med Chem 47: 4239-46 (2004)
Toyama Chemical
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.EBI
J Med Chem 47: 4213-30 (2004)
Abbott Laboratories
Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.EBI
J Med Chem 47: 4202-12 (2004)
Universit£
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.BDB
J Med Chem 47: 4163-5 (2004)
Virginia Commonwealth University
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.EBI
J Med Chem 47: 4155-8 (2004)
Friedrich-Schiller-UniversitäT Jena
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI
J Med Chem 47: 4151-4 (2004)
Fujisawa Pharmaceutical
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.BDB
J Med Chem 47: 4147-50 (2004)
University of Michigan
Prospects for inhibitors of protein tyrosine phosphatase 1B as antidiabetic drugs.EBI
J Med Chem 47: 4142-6 (2004)
Serono Pharmaceutical Research Institute
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.EBI
J Med Chem 47: 4135-41 (2004)
Merck Research Laboratories
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.EBI
J Med Chem 47: 4118-27 (2004)
Glaxosmithkline
New crinine-type alkaloids with inhibitory effect on induction of inducible nitric oxide synthase from Crinum yemense.EBI
J Nat Prod 67: 1119-24 (2004)
Mansoura University
Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.EBI
J Nat Prod 67: 1079-83 (2004)
Toyama Medical and Pharmaceutical University
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.EBI
J Med Chem 47: 4083-8 (2004)
Neurocrine Biosciences
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.EBI
J Med Chem 47: 4066-71 (2004)
University of Cagliary
Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase.EBI
J Med Chem 47: 4060-5 (2004)
University of California
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.EBI
J Med Chem 47: 4054-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute