146 articles for thisTarget
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Article Title
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2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
Gilead Sciences
Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
Forma Tm2
Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
Boehringer Ingelheim International
2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
Cancer Research Technology
Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use
Oryzon Genomics
Substituted pyrrolo[2,3-b]pyrazines and substituted pyrazolo[3,4-b]pyridines as ITK and JAK kinase inhibitors
Arrien Pharmaceuticals
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
Vtv Therapeutics
3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1
Vanderbilt University
N-(phenylsulfonyl)benzamides and related compounds as BCL-2 inhibitors
The Regents of The University of Michigan
Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Alkyne compounds for treatment of complement mediated disorders
Achillion Pharmaceuticals
Isoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
Merck Sharpe & Dohme
Amido-substituted imidazopyridazines useful in the treatment of hyper-proliferative and/or angiogenesis disorders
Bayer Pharma Aktiengesellschaft
Substituted benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments
University of Chicago
C-6 spirocarbocyclic iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as anti-tumor agents
Duquesne University of The Holy Spirit
Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase.
University of California San Francisco
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Wyeth Research
Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily.
Bristol-Myers Squibb
Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists.
Bristol-Myers Squibb
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.
Gsk
Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.
Abbott Laboratories
Structure-activity relationships of orotidine-5'-monophosphate decarboxylase inhibitors as anticancer agents.
Toronto General Research Institute
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.
University of Tennessee Health Science Center
New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain.
Sapienza University of Rome
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
Vanderbilt University School of Medicine
A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization.
Fujisawa Pharmaceutical
Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo.
Glsynthesis
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.
Astrazeneca
Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases.
Merck Serono
Arginine binding motifs: design and synthesis of galactose-derived arginine tweezers as galectin-3 inhibitors.
Lund University
Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.
Wyeth Research
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Abbott Laboratories
Design, Synthesis, Evaluation, and Crystallographic-Based Structural Studies of HIV-1 Protease Inhibitors with Reduced Response to the V82A Mutation.
Universidad De Santiago De Compostela
Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
Pfizer
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.
Duquesne University
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.
Novartis Pharmaceuticals
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
Eli Lilly
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.
Novartis Pharmaceuticals
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Gnf
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.
Gnf
Identification of a potent and selective non-basic cathepsin K inhibitor.
Merck Frosst Centre For Therapeutic Research
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
Merck Frosst Centre For Therapeutic Research
Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode.
University of California Berkeley
Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method.
University of California Berkeley
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta.
Ghent University
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
University of Illinois At Urbana-Champaign
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
University of Illinois At Chicago
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase.
Pfizer
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
Methylgene
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
Abbott Laboratories
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Abbott Laboratories
Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations.
Cnrs
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
Bristol-Myers Squibb
Probing Binding Requirements of Type I and Type II Isoforms of Inosine Monophosphate Dehydrogenase with Adenine-Modified Nicotinamide Adenine Dinucleotide Analogues.
University of Minnesota At Twin Citiies
Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer.
University of Tennessee Health Science Center
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
Abbott Laboratories
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Merck Research Laboratories
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
Merck Research Laboratories
Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs.
University of Pavia
Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives.
University of Bari
Chlamydocin analogs bearing carbonyl group as possible ligand toward zinc atom in histone deacetylases.
Kyushu Institute of Technology
The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.
University of Southampton
Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
Nagoya City University
Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors.
Wyeth Research
Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity.
Karo Bio
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.
Karo Bio
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
Ligand Pharmaceuticals
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
Ligand Pharmaceuticals
Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.
Ligand Pharmaceuticals
Structure-activity relationships of Bacillus cereus and Bacillus anthracis dihydrofolate reductase: toward the identification of new potent drug leads.
University of Connecticut At Storrs
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis.
Dartmouth College
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
Gsk
Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim.
Oklahoma State University At Stillwater
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region.
University of Prince Edward Island
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
Abbott Laboratories
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Abbott Laboratories
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Gsk
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.
Berlex
Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells.
University of California Davis
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.
Abbott Laboratories
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).
University of Illinois At Chicago
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Bristol-Myers Squibb
Nucleation of an allosteric response via ligand-induced loop folding.
University of Maryland College Park