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149 articles for thisTarget

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

Article Title
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.EBI
The Institute of Cancer Research
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
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
Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies.EBI
Kakatiya University
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.EBI
Translational Research Institute
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
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.EBI
Translational Research Institute
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
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI
East China University of Science and Technology
Amino acid derived quinazolines as Rock/PKA inhibitors.EBI
Translational Research Institute
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 a novel series of 4-quinolone JNK inhibitors.EBI
Roche Palo Alto
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI
Sichuan University
Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.EBI
Astellas Pharma
Discovery and development of spleen tyrosine kinase (SYK) inhibitors.EBI
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.EBI
Teijin Pharma
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.EBI
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.EBI
Korea University
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.EBI
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
The selectivity of protein kinase inhibitors: a further update.EBI
University of Dundee
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.EBI
Eberhard Karls University Tuebingen
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
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
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.EBI
Novartis Institutes For Biomedical Research
Pyridazine based inhibitors of p38 MAPK.EBI
Merck Research Laboratories
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
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
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.EBI
Novartis Institutes For Biomedical Research
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
Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.EBI
Sanford-Burnham Medical 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
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
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Rational design of inhibitors that bind to inactive kinase conformations.EBI
Novartis Research Foundation
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
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.EBI
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
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI
Novartis Institutes For Biomedical Research
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI
Institute For Medical Research
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Displacement assay for the detection of stabilizers of inactive kinase conformations.EBI
Chemical Genomics Centre of The Max Planck Society
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
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.EBI
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.EBI
Cardiff University
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.EBI
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.EBI
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.EBI
Eberhard-Karls University
Discovery and optimization of p38 inhibitors via computer-assisted drug design.EBI
Boehringer Ingelheim Pharmaceuticals
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Ucb Pharma
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 and design of benzimidazolone based inhibitors of p38 MAP kinase.EBI
Boehringer Ingelheim Pharmaceuticals
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.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
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
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.EBI
Novartis Institutes For Biomedical Research
Kinase Inhibitors as Underexplored Antiviral Agents.EBI
Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)
Rapid computational identification of the targets of protein kinase inhibitors.EBI
University of Iowa
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
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
Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity.EBI
Bristol Myers Squibb
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI
Novartis Institutes For Biomedical Research
Discovery of the c-Jun N-Terminal Kinase Inhibitor EBI
Bristol Myers Squibb
-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.EBI
Reaction Biology
Discovery of EBI
Zhejiang University
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
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.EBI
Dana-Farber Cancer Institute
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
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.EBI
Boehringer Ingelheim Pharmaceuticals
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.EBI
China Pharmaceutical University
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI
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.EBI
Japan Tobacco
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.EBI
Gachon University
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.EBI
Merck Research Laboratories
Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI
Merck Research Laboratory
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
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
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
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
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 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 evaluation and molecular docking studies of novel coumarin-isatin derivatives as a-glucosidase inhibitors.BDB
Jishou University
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB
Novartis Pharma
Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity.BDB