285 articles for thisTarget
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Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Ambit Biosciences
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Ambit Biosciences
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Ambit Biosciences
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Ambit Biosciences
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Isoindoline compositions and methods for treating neurodegenerative disease
Cognition Therapeutics
Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
Biomarin Pharmaceutical
Method of treatment using substituted imidazo[1,2b]pyridazine compounds
Array Biopharma
Pyrrolopyrimidine compounds for the treatment of cancer
University of North Carolina At Chapel Hill
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
Enanta Pharmaceuticals
Use of agonists of formyl peptide receptor 2 for treating ocular inflammatory diseases
Allergan
2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
Array Biopharma
Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
Bristol-Myers Squibb
Substituted amino triazoles useful as human chitinase inhibitors
Oncoarendi Therapeutics
1-sulfonyl piperidine derivatives as modulators of prokineticin receptors
Takeda Pharmaceutical
Isoindoline compositions and methods for treating neurodegenerative disease
Cognition Therapeutics
Compounds useful for the treatment of degenerative and inflammatory diseases
Galapagos
Compositions and methods of modulating 15-PGDH activity
Case Western Reserve University
Substituted cyclopentanes, tetrahydrofuranes and pyrrolidines as orexin receptor antagonists
Takeda Pharmaceutical
Piperidine and azepine derivatives as prokineticin receptor modulators
Takeda Pharmaceutical
Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
Janssen Pharmaceutica
Lysine demethylase inhibitors for diseases and disorders associated with Flaviviridae
Oryzon Genomics
Compositions and methods of modulating short-chain dehydrogenase activity
Case Western Reserve University
β-D-2′-deoxy-2′-substituted-4′-substituted-2-substituted-N6-substituted-6-aminopurinenucleotides for the treatment of paramyxovirus and orthomyxovirus infections
Atea Pharmaceuticals
3′-substituted methyl or alkynyl nucleosides nucleotides for the treatment of HCV
Idenix Pharmaceuticals
Macrocyclic benzofuran compounds for the treatment of hepatitis C
Bristol-Myers Squibb
Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
Millennium Pharmaceuticals
Fused-ring compounds, pharmaceutical composition and uses thereof
Shanghai De Novo Pharmatech
8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
Boehringer Ingelheim International
3-(1H-benzo[D]imidazol-2-yl)-1H-pyrazolo[3,4-C]pyridine and therapeutic uses thereof
Samumed
Oxazolidin-2-one-pyrimidine derivatives and the use thereof as phosphatidylinositol-3-kinase inhibitors
Novartis
Heterocyclic compounds and methods of use thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Pyranochromenyl phenol derivative, and pharmaceutical composition for treating metabolic syndrome or inflammatory disease
Glaceum
Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
Lycera
2-aminoquinoline-based compounds for potent and selective neuronal nitric oxide synthase inhibition
Northwestern University
Histone deacetylase inhibitors and compositions and methods of use thereof
Chdi Foundation
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
Array Biopharma
N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides
Pfizer
Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors
Phoenix Molecular Design
Substituted oxazole- and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands II
Medifron Dbt
Indole and pyrrole compounds, a process for their preparation and pharmaceutical compositions containing them
Les Laboratoires Servier
Histone deacetylase inhibitors and compositions and methods of use thereof
Chdi Foundation
Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases
University of Washington Through Its Center For Commercialization
2,3-dihydro-isoindole-1-on derivative as BTK kinase suppressant, and pharmaceutical composition including same
Crystalgenomics
3-(indol-3-yl)-pyridine derivatives, pharmaceutical compositions and methods for use
Iteos Therapeutics
Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
Amgen
Glucosylceramide synthase inhibitors and therapeutic methods using the same
The Regents of The University of Michigan
4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE)
Janssen Pharmaceutica
Benzodioxane inhibitors of leukotriene production for combination therapy
Boehringer Ingelheim International
Compounds as inhibitors of diacylglycerol O-acyltransferase type 1 enzyme
Kainos Medicine
Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Vitae Pharmaceuticals
Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.
Max-Planck-Institut Fuer Biochemie
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.
Pfizer
Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase.
Cornell University
The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
University of Leeds
Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).
Universite De Montreal At Succursale Centre-Ville
Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.
Universite De Montreal At Succursale Centre-Ville
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
Merck Research Laboratories
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Merck Research Laboratories
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Merck Research Laboratories
The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity.
Merck Research Laboratories
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
Abbott Laboratories
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Abbott Laboratories
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
Abbott Laboratories
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors.
Abbott Laboratories
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
Aventis Pharma Deutschland
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Aventis Pharma Deutschland
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.
Eli Lilly
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.
Astex
Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
Roche Palo Alto
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.
University of California San Francisco
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
Vertex Pharmaceuticals
New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity.
Sapienza University of Rome
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.
Merck Research Laboratories
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Abbott Laboratories
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Abbott Laboratories
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Eli Lilly
Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.
Pfizer
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.
Vernalis (R&D)
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.
Vernalis (R&D)
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Vernalis (R&D)
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
University of Texas Southwestern Medical Center
Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development.
University of North Carolina At Chapel Hill
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity.
Merck Research Laboratories
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Merck Research Laboratories
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.
Abbott Laboratories
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.
Merck Research Laboratories
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.
Mrc
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
Griffith University
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.
Uk Centre For Cancer Therapeutics
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Merck Research Laboratories
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Merck Research Laboratories
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Abbott Laboratories
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Abbott Laboratories
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Abbott Laboratories
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.
Merck Research Laboratories
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.
Glaxosmithkline
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
Amgen
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
Amgen
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
Boehringer Ingelheim Pharmaceuticals
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.
Boehringer Ingelheim Pharmaceuticals
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.
Abbott Laboratories
Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening.
Astrazeneca
Identification of chemically diverse Chk1 inhibitors by receptor-based virtual screening.
Vernalis (R&D)
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.
Vernalis (R&D)
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.
Plexxikon
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
Pfizer
Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.
Canadian Institutes of Health Research
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Genentech
A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.
Duke University Medical Center
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
University of Leeds
Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
Aventis Pharma
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.
Abbott Laboratories
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Abbott Laboratories
Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors.
Pharmacia
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
Pharmacia
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.
Pharmacia
Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.
Abbott Laboratories
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
Celera
(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
Schering-Plough Research Institute
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Abbott Laboratories
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Abbott Laboratories
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability.
Pfizer
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.
Purdue Pharma
Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase.
University of North Carolina At Chapel Hill
Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.
Celera
Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.
Incyte
Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.
Wyeth Research
Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors.
Wyeth Research
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.
Johnson & Johnson Pharmaceutical
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.
Cephalon
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.
Axys Pharmaceutical
Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Axys Pharmaceutical
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.
Johnson & Johnson Pharmaceutical
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.
University of Queensland
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.
Glaxosmithkline
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Merck Research Laboratories
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.
Abbott Laboratories
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Abbott Laboratories
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.
Abbott Laboratories
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.
Abbott Laboratories
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.
Axys Pharmaceuticals
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S.
Georgia State University
Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.
Johnson & Johnson Pharmaceutical
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.
University of Florida College of Medicine
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease.
University of Queensland