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75 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
12565952 26 p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.EBI Merck & Co.
12482438 50 p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.EBI Merck Research Laboratories
9873730 27 Potent inhibitors of the MAP kinase p38.EBI R. W. Johnson Pharmaceutical Research Institute
9873686 18 Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.EBI SmithKline Beecham Pharmaceuticals Ltd
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
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
26259807 21 Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.EBI Sejong University
25965804 80 Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.EBI Eli Lilly and Company
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
25369539 116 SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI Sanofi
22521646 38 Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.EBI Rhône-Poulenc Rorer
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
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
22795331 51 Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI Janssen Pharmaceutical Companies of Johnson & Johnson L.L.C.
24900346 90 Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI TBA
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Inc
18359226 50 Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI Bristol-Myers Squibb Research and Development
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
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
12672248 50 Kinase inhibitors: not just for kinases anymore.EBI Northwestern University
12166950 208 Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI Millennium Pharmaceuticals Inc
11844702 14 Pyridazine based inhibitors of p38 MAPK.EBI Merck Research Laboratories
11591521 39 Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.EBI Bayer Research Center
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
21705217 60 Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb Co.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20637613 4 Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.EBI Daiichi Sankyo Co., Ltd
20346655 117 Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI Abbott Laboratories
20218619 44 Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
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
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Inc
18313298 40 The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.EBI Bristol-Myers Squibb Co.
16789733 41 Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16516473 444 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 AstraZeneca
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
16162000 42 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.EBI Takeda Pharmaceutical Co., Ltd
15615512 21 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15317463 16 Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
14592495 60 Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc
12565927 24 Imidazopyrimidines, potent inhibitors of p38 MAP kinase.EBI Johnson & Johnson Pharmaceutical Research and Development LLC
12540232 53 Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.EBI Merck Research Laboratories
11934592 24 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11549467 85 Substituted imidazoles as glucagon receptor antagonists.EBI Merck Research Laboratories
10866395 33 SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI Novartis Pharma AG
9873604 72 Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI Merck Research Laboratory
28291685 12 Synthesis and molecular docking studies of new furochromone derivatives as p38? MAPK inhibitors targeting human breast cancer MCF-7 cells.EBI Cairo University
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
23941661 5 KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.EBI VU University Amsterdam
24332487 46 Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.EBI The Scripps Research Institute
23746475 93 The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
18157122 1 High-content single-cell drug screening with phosphospecific flow cytometry.EBI Stanford University
17095218 3 Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.EBI Paradigm Therapeutics Ltd
17411025 12 Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.EBI Eberhard-Karls-University T£bingen
16945534 7 p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.EBI Merck Research Laboratories
16750367 2 The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.EBI Procter and Gamble Pharmaceuticals
15139749 35 Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.EBI Procter and Gamble Pharmaceuticals
12852754 143 Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.EBI Eberhard-Karls-University T£bingen
12061876 53 From imidazoles to pyrimidines: new inhibitors of cytokine release.EBI Eberhard-Karls-University T£bingen
12014955 19 An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.EBI Aventis Pharma S.A.
11585447 16 Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.EBI Vertex Pharmaceuticals Inc
30480444 85 Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.EBI Sichuan University/Collaborative Innovation Center of Biotherapy
30082069 359 ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI Vertex Pharmaceuticals Inc
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals, Inc
29291937 40 Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.EBI Takeda Pharmaceutical Company Limited
29107542 35 Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.EBI Novartis Institutes for Biomedical Research
29133046 18 Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.EBI University of Zagreb