173 articles for thisTarget
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Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
The Institute Of Cancer Research
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).
Icahn School Of Medicine At Mount Sinai
Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.
Semmelweis University
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Wuxi Apptec
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies.
Kakatiya University
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.
Translational Research Institute
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Genentech
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.
Translational Research Institute
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.
Martin-Luther-University Halle-Wittenberg
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.
Takeda Pharmaceutical
Amino acid derived quinazolines as Rock/PKA inhibitors.
Translational Research Institute
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.
Astrazeneca
Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.
TBA
3D-QSAR and docking studies of aminopyridine carboxamide inhibitors of c-Jun N-terminal kinase-1.
Chinese Academy Of Sciences
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Glaxosmithkline
Irreversible protein kinase inhibitors: balancing the benefits and risks.
Covalution Pharma
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.
Takeda Pharmaceutical
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Takeda Pharmaceutical
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.
Takeda Pharmaceutical
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.
Korea University
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.
Takeda Pharmaceutical
Unbiased binding assays for discovering small-molecule probes and drugs.
Broad Institute Of Harvard And Mit
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.
Hanyang University
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.
Translational Research Institute
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
Glaxosmithkline
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2).
Takeda Pharmaceutical
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).
Takeda Pharmaceutical
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Astrazeneca
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.
Serono Pharmaceutical Research Institute
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Kyowa Hakko Kogyo
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Celgene
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.
The Scripps Research Institute
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Takeda Pharmaceutical
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
Design and characterization of a potent and selective dual ATP- and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor.
Sanford-Burnham Medical Research Institute
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Elan Pharmaceuticals
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.
Elan Pharmaceuticals
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.
Roche Palo Alto
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.
Korea Institute Of Science And Technology
Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.
Sanford-Burnham Medical Research Institute
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors
Roche Palo Alto
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Elan Pharmaceuticals
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Elan Pharmaceuticals
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Roche Palo Alto
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Novartis Institutes For Biomedical Research
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
Institute For Medical Research
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Takeda Pharmaceutical
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.
Vertex Pharmaceuticals
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Pfizer
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Astrazeneca R&D Boston
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
The Scripps Research Institute-Florida
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Amgen
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Glaxosmithkline
Development of paramagnetic probes for molecular recognition studies in protein kinases.
Institute For Medical Research
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.
Ucb Pharma
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Ucb Pharma
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.
Tibotec
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Abbott Laboratories
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Abbott Laboratories
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University Of Technology
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.
Astrazeneca R&D SöDertäLje
Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.
National Clinical Research Center For Geriatrics
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
Takeda Pharmaceutical
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.
Astrazeneca R&D SöDertäLje
Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors.
University Of Sharjah
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr
East China Normal University
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.
East China Normal University
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Glaxosmithkline
Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity.
Bristol Myers Squibb
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Novartis Institutes For Biomedical Research
-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.
Reaction Biology
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin
Cephalon
Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration.
Eberhard Karls Universit£T
Rational modification, synthesis and biological evaluation of 3,4-dihydroquinoxalin-2(1H)-one derivatives as potent and selective c-Jun N-terminal kinase 3 (JNK3) inhibitors.
Peking University
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.
Dana-Farber Cancer Institute
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.
Reaction Biology
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.
Pharmaceutical Research Institute
Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series.
University Of North Carolina
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Glaxosmithkline
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.
Bayer Research Center
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.
Novartis Pharma
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.
Japan Tobacco
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase I? and ?.
Korea Institute Of Science And Technology
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.
Gachon University
Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.
University Of California
Multistage Screening Reveals 3-Substituted Indolin-2-one Derivatives as Novel and Isoform-Selective c-Jun N-terminal Kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases.
Peking University
Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy.
Celgene
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University Of Florida
Synthesis, biological evaluation, and molecular modeling of 11H-indeno[1,2-b]quinoxalin-11-one derivatives and tryptanthrin-6-oxime as c-Jun N-terminal kinase inhibitors.
Montana State University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.
Shanghai Pharmaceuticals Holding
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.
Roche Palo Alto
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF
Nanjing University
Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.
Montclair State University
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N
The Institute Of Cancer Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.
Glaxosmithkline
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Wuxi Apptec
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.
The Ohio State University
Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.
University Of Pittsburgh
A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases.
The Scripps Research Institute
Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38.
The Scripps Research Institute
Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.
Burnham Institute For Medical Research
Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Gsk
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.
Burnham Institute For Medical Research
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.
Amgen
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