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162 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review

Article Title
Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.EBI
Eberhard Karls Universit£T T£Bingen
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).EBI
Icahn School Of Medicine At Mount Sinai
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).EBI
Wuxi Apptec
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI
Sichuan University
Tetra-substituted pyridinylimidazoles as dual inhibitors of p38a mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases.EBI
Eberhard Karls Universit£T T£Bingen
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies.EBI
Kakatiya University
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI
Astellas Pharma
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.EBI
Translational Research Institute
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI
Sichuan University
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.EBI
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.EBI
Translational Research Institute
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI
Vertex Pharmaceuticals
Inhibitors of c-Jun N-terminal kinases: an update.EBI
Eberhard Karls Universit£T T£Bingen
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.EBI
Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.EBI
Aska Pharmaceutical
Unfolded Protein Response in Cancer: IRE1a Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability.EBI
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.EBI
Translational Research Institute
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects.EBI
Hanyang University
Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.EBI
The Scripps Research Institute
3D-QSAR studies of 1,2-diaryl-1H-benzimidazole derivatives as JNK3 inhibitors with protective effects in neuronal cells.EBI
Hanyang University
Amino acid derived quinazolines as Rock/PKA inhibitors.EBI
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).EBI
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI
Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI
Covalution Pharma
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.EBI
Korea University
Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI
Vertex Pharmaceuticals
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI
Hanyang University
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI
Vertex Pharmaceuticals
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.EBI
Translational Research Institute
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
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.EBI
Kinase array design, back to front: biaryl amides.EBI
Latifolians A and B, novel JNK3 kinase inhibitors from the Papua New Guinean plant Gnetum latifolium.EBI
Griffith University
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2).EBI
Takeda Pharmaceutical
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI
Osi Pharmaceuticals
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).EBI
Takeda Pharmaceutical
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
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
Serono Pharmaceutical Research Institute
Fragment-based drug discovery.EBI
Sunesis Pharmaceuticals
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.EBI
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.EBI
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.EBI
The Scripps Research Institute
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI
Novartis Institute For Biomedical Research
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.EBI
Elan Pharmaceuticals
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.EBI
Elan Pharmaceuticals
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.EBI
Roche Palo Alto
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.EBI
Korea Institute Of Science And Technology
Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.EBI
The Scripps Research Institute
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 inhibitorsEBI
Roche Palo Alto
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.EBI
The Scripps Research Institute
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.EBI
Elan Pharmaceuticals
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.EBI
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.EBI
Elan Pharmaceuticals
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.EBI
Daiichi Sankyo
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.EBI
Roche Palo Alto
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.EBI
The Scripps Research Institute
Small molecule JNK (c-Jun N-terminal kinase) inhibitors.EBI
Merck Research Laboratories
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.EBI
Roche Palo Alto
Selectively nonselective kinase inhibition: striking the right balance.EBI
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.EBI
Translational Research Institute And Department Of Molecular Therapeutics
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.EBI
Eberhard-Karls-University Of T£Bingen
3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.EBI
Eberhard-Karls University
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
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.EBI
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.EBI
The Scripps Research Institute-Florida
Chroman-3-amides as potent Rho kinase inhibitors.EBI
The Scripps Research Institute
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.EBI
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.EBI
Ucb Pharma
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.EBI
Eberhard-Karls University
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.EBI
Scripps Florida
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Ucb Pharma
Assessing potency of c-Jun N-terminal kinase 3 (JNK3) inhibitors using 2D molecular descriptors and binary QSAR methodology.EBI
Aureus Pharma
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.EBI
Eberhard-Karls-University TüBingen
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.EBI
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.EBI
Abbott Laboratories
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.EBI
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.EBI
Hefei University Of Technology
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.EBI
Astrazeneca R&D SöDertäLje
Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.EBI
National Clinical Research Center For Geriatrics
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.EBI
University College London
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.EBI
Astrazeneca R&D SöDertäLje
Kinase Inhibitors as Underexplored Antiviral Agents.EBI
Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)
Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors.EBI
University Of Sharjah
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.EBI
Central South University
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.EBI
Rapt Therapeutics
A small molecule-kinase interaction map for clinical kinase inhibitors.EBI
Ambit Biosciences
Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.EBI
Serono Pharmaceutical Research Institute
Selective Macrocyclic Inhibitors of DYRK1A/B.EBI
Dana-Farber Cancer Institute
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.EBI
-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.EBI
Reaction Biology
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.EBI
Korea Institute Of Science And Technology
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.EBI
Aventis Pharmaceuticals
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.EBI
Peking University
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.EBI
Sichuan University
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.EBI
Dana-Farber Cancer Institute
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI
Merck Research Laboratories
Advances in the Development of Phosphodiesterase-4 Inhibitors.EBI
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.EBI
Reaction Biology
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.EBI
China Pharmaceutical University
Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series.EBI
University Of North Carolina
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.EBI
Vertex Pharmaceuticals
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
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.EBI
Japan Tobacco
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.EBI
Gachon University
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.EBI
Glaxosmithkline R&D
Discovery of 4EBI
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.EBI
Peking University
Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy.EBI
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
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.EBI
Montana State University
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.EBI
Eppley Institute For Research In Cancer And Allied Diseases
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI
Novartis Institutes For Biomedical Research
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.EBI
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.EBI
Shanghai Pharmaceuticals Holding
A novel necroptosis inhibitor-necrostatin-21 and its SAR study.EBI
Chinese Academy Of Sciences
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.EBI
Roche Palo Alto
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.EBI
Northwestern University
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI
Universitaire Vaudois
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 NEBI
The Institute Of Cancer Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.EBI
Temple University
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.EBI
Wuxi Apptec
The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen.EBI
Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.EBI
University Of Pittsburgh
Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.BDB
Aristotle University Of Thessaloniki
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives.BDB
Warsaw University Of Technology
Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors.BDB
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.BDB
The Scripps Research Institute
1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.BDB
The Oregon Health Sciences University