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113 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
27055065 92 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
27089211 38 Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI Zhejiang University
26762835 342 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
26431428 36 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 Co., Ltd.
25893042 65 Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.EBI Translational Research Institute
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25341110 66 Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.EBI Genentech
24938496 32 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 Co., Ltd
25393557 83 Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.EBI Translational Research Institute
23498914 32 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
23434140 35 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
23416002 126 Amino acid derived quinazolines as Rock/PKA inhibitors.EBI Translational Research Institute
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline
17194588 92 N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI GlaxoSmithKline
22621397 39 Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI Covalution Pharma BV
23142618 66 Discovery of a novel series of 4-quinolone JNK inhibitors.EBI Roche Palo Alto
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
23116168 42 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
22905713 9 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 Inc
22257213 98 Discovery and development of spleen tyrosine kinase (SYK) inhibitors.EBI Rigel, Inc.
22746295 91 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 Ltd.
23002419 30 From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.EBI TBA
22858099 52 Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.EBI Korea University
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc
19751974 81 Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.EBI Pfizer Inc
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
17850214 99 The selectivity of protein kinase inhibitors: a further update.EBI University of Dundee
18578517 93 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
18313930 30 Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2).EBI Takeda Pharmaceutical Co., Ltd
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18278858 93 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 Amgen Inc
18313304 50 Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).EBI Takeda Pharmaceutical Co., Ltd
16876403 85 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
15999997 85 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
15177483 33 SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.EBI Novartis Institutes for BioMedical Research
11844702 14 Pyridazine based inhibitors of p38 MAPK.EBI Merck Research Laboratories
22244937 44 Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.EBI Celgene Corporation
22226655 88 Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.EBI Celgene Corporation
22014550 337 Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI Ansaris
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Rhône-Poulenc Rorer
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21936542 143 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
21813278 95 Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.EBI Elan Pharmaceuticals
20594847 62 In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.EBI Novartis Institutes for BioMedical Research
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer Inc
21570836 78 Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.EBI Elan Pharmaceuticals
21515047 24 3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.EBI Roche Palo Alto
21489792 26 Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.EBI Korea Institute of Science and Technology
21458276 82 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
21375264 77 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 LLC
21316234 133 Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.EBI Elan Pharmaceuticals, Inc.
21112785 151 Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.EBI Elan Pharmaceuticals
21071223 190 Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.EBI Elan Pharmaceuticals
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
20655210 3 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
20395140 42 Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.EBI Pfizer Inc
20146479 31 Small molecule JNK (c-Jun N-terminal kinase) inhibitors.EBI Merck Research Laboratories
19950901 23 Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.EBI Roche Palo Alto
20060294 21 Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI Novartis Institutes for BioMedical Research
20045647 35 Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI Institute for Medical Research
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19928858 77 Displacement assay for the detection of stabilizers of inactive kinase conformations.EBI Chemical Genomics Centre of the Max Planck Society
19591487 38 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.EBI Eberhard-Karls University
19361991 80 Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI Vertex Pharmaceuticals Inc
19574047 42 Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc
19356929 17 Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI Boehringer Ingelheim Pharmaceuticals Inc
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Inc
18817365 73 Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.EBI Amgen Inc
18539026 5 Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.EBI Cardiff University
18482836 14 IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.EBI UCB Pharma SA
17166835 12 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 "P. Angeletti
18207396 10 Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.EBI Eberhard-Karls University
17658737 2 Discovery and optimization of p38 inhibitors via computer-assisted drug design.EBI Boehringer Ingelheim Pharmaceuticals Inc
17570666 64 Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Pfizer Inc
17560108 5 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 Inc
17459703 111 Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI UCB Pharma SA
17289388 8 Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.EBI Tibotec BVBA
17055723 17 Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.EBI Abbott Laboratories
17010605 2 Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc
16971120 104 Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.EBI Abbott Laboratories
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc
16249085 26 Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.EBI Novartis Institutes for BioMedical Research
15943486 8 Rapid computational identification of the targets of protein kinase inhibitors.EBI University of Iowa
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
15615541 2 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
15177482 90 Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI Novartis Institutes for BioMedical Research
12086485 10 Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.EBI Boehringer Ingelheim Pharmaceuticals Inc
11597418 47 Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI GlaxoSmithKline
10866395 33 SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI Novartis Pharma AG
10377223 57 Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.EBI Merck Research Laboratories
9873604 72 Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI Merck Research Laboratory
26505898 123 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
26509640 234 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
23664880 47 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
29969256 21 Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI Centre Hospitalier Universitaire Vaudois (CHUV) and University of Lausanne (UNIL)
30199249 92 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
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals, Inc
28929759 83 Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.EBI WuXi AppTec Co., Ltd.
27996267 22 Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.EBI University of Pittsburgh
21381887 3 Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.BDB Aristotle University of Thessaloniki
27616456 21 Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as a-glucosidase inhibitors.BDB Jishou University
9650799 159 [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB Novartis Pharma AG
2905002 8 Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity.BDB Schering-Plough Corporation