257 articles for thisTarget
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Article Title
Organization
Geminally substituted cyanoethylpyrazolo pyridones as Janus kinase inhibitors
Merck Sharp & Dohme
6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives
Hoffmann-La Roche
Substituted benzylindazoles for use as Bub1 kinase inhibitors in the treatment of hyperproliferative diseases
Bayer Intellectual Property
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof
Pfizer
N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system
Chronos Therapeutics
Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
Incyte
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
Array Biopharm
Assays for screening for or identifying an agent or molecule that can block or inhibit AVB3 integrin from forming a complex with KRAS
University of California
Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
Exonhit Therapeutics
Positive allosteric modulators of the muscarinic acetylcholine receptor M4
Vanderbilt University
Substituted 5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine compounds as PDE2 inhibitors
Dart Neuroscience (Cayman)
N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of NR2B
Cadent Therapeutics
C5-C6-fused tricyclic iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
TBA
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-1-yl) ureas as p38 MAP kinase inhibitors
Respivert
Inhibitors of metallo-beta-lactamase (MBL) comprising a zinc chelating moiety
Universitetet | Oslo
Selective histone deactylase 6 inhibitors
H. Lee Moffitt Cancer Center and Research Institute
Diazine-fused amidines as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Substituted 2-phenyl (AZA)benzofuran compounds for the treatment of hepatitis C
Bristol-Myers Squibb
Xanthine derivatives, their use as a medicament, and pharmaceutical preparations comprising the same
Max-DelbrÜCk-Centrum FÜR Molekulare Medizin
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Arena Pharmaceuticals
Oxazolidine-based compound and selective androgen receptor agonist comprising same
Dong-A St
Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
Array Biopharma
Phenyl and pyridinyl substituted piperidines and piperazines as inhibitors of IDH1 mutants and their use in treating cancer
Agios Pharmaceuticals
Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.
The University of Tokyo
Drug design with a new transition state analog of the hydrated carbonyl: silicon-based inhibitors of the HIV protease.
State University of New York
Energetic, structural, and antimicrobial analyses of beta-lactam side chain recognition by beta-lactamases.
Northwestern University
Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production.
Abbott Laboratories
Thioamide Hydroxypyrothiones Supersede Amide Hydroxypyrothiones in Potency against Anthrax Lethal Factor.
Howard Hughes Medical Institute
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
Merck Research Laboratories
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase.
Berlex Biosciences
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.
Bristol-Myers Squibb
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists.
Pharmacopeia Drug Discovery
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.
Institut Claudius Regaud
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
University of Tokyo
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
Institut De Biologie Structurale
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.
Universite Paris 7-Denis Diderot
Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives.
Peking University
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Merck Research Laboratories
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Wyeth Research
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.
Wyeth Research
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.
St. Jude Research Hospital
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
St. Jude Research Hospital
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
University of Mississippi
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Irbm-Mrl
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Irbm-Mrl
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.
The Scripps Research Institute
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.
The Scripps Research Institute
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.
Johnson & Johnson Pharmaceutical
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.
Johnson & Johnson Pharmaceutical
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
Vu University Amsterdam
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.
Friedrich Alexander University Erlangen
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Bristol-Myers Squibb
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors.
University of Liverpool
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
University of Tokyo
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.
Amgen
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species.
Gsk
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.
University Di Perugia
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
University of North Carolina at Chapel Hill
Toward an optimal joint recognition of the S1' subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP).
Cnrs
Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2.
University of Athens
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Universita Degli Studi Di Bari
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Wyeth Research
Structure-activity relationships of C6-uridine derivatives targeting plasmodia orotidine monophosphate decarboxylase.
Toronto General Research Institute
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
University of Arizona Tucson
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.
Abbott Laboratories
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
Wyeth Research
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
University of Arizona Tucson
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
Vernalis (R&D)
Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes.
Bristol-Myers Squibb
Orally active purine-based inhibitors of the heat shock protein 90.
Conforma Therapeutics
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Amgen
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Amgen
Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.
Gsk
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Abbott Laboratories
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Abbott Laboratories
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.
Abbott Laboratories
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Gsk
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.
Bristol-Myers Squibb
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
Karo Bio
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor.
Karo Bio
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.
Karo Bio
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1).
Duquesne University
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
Ligand Pharmaceuticals
Isofagomine- and 2,5-anhydro-2,5-imino-D-glucitol-based glucocerebrosidase pharmacological chaperones for Gaucher disease intervention.
The Scripps Research Institute
Alpha-1-C-octyl-1-deoxynojirimycin as a pharmacological chaperone for Gaucher disease.
Hokuriku University
Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates.
Duquesne University
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Ligand Pharmaceuticals
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Bristol-Myers Squibb
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.
Gsk
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.
Crefsip
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.
Crefsip
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.
Gsk
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.
University of Tennessee At Knoxville
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Pfizer
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.
Novartis Pharmaceuticals
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.
Daiichi Pharmaceutical
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Amgen
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.
Amgen
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.
Amgen
Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme.
Nci-Fcrdc
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
Gsk
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.
Genentech
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
Merck Research Laboratories
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.
Chul
Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa.
Berlex
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Vernalis (R&D)
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
Berlex Biosciences
Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.
Abbott Laboratories
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.
Johnson & Johnson Pharmaceutical
Evaluating scoring functions for docking and designing beta-secretase inhibitors.
Merck Research Laboratories
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.
Merck Research Laboratories
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Pfizer
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.
Vernalis (R&D)
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.
Abbott Laboratories
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain.
University of Copenhagen
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis.
Suny Stony Brook
Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.
Sunesis
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.
Purdue University
Strong solute-solute dispersive interactions in a protein-ligand complex.
University of Leeds
Thermodynamic penalty arising from burial of a ligand polar group within a hydrophobic pocket of a protein receptor.
University of Leeds
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.
University of North Carolina