103 articles for thisTarget

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

PMID	Data	Article Title	Organization
12565952	26	p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.	Merck
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.	Merck Research Laboratories
9873730	27	Potent inhibitors of the MAP kinase p38.	R. W. Johnson Pharmaceutical Research Institute
9873686	18	Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.	Smithkline Beecham Pharmaceuticals
26800309	90	Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.	Sygnature Discovery
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).	Icahn School of Medicine At Mount Sinai
26259807	21	Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.	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.	Eli Lilly
25893042	65	Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.	Translational Research Institute
25415535	118	Inhibitors of c-Jun N-terminal kinases: an update.	Eberhard Karls Universit£T T£Bingen
25369539	116	SAR156497, an exquisitely selective inhibitor of aurora kinases.	Sanofi
23442188	4	A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.	Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences
23142618	66	Discovery of a novel series of 4-quinolone JNK inhibitors.	Roche Palo Alto
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.	Sichuan University
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
14593182	34	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.	Pfizer
18359226	50	Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.	Bristol-Myers Squibb Research and Development
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
16876403	85	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
12672248	50	Kinase inhibitors: not just for kinases anymore.	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.	Millennium Pharmaceuticals
11844702	14	Pyridazine based inhibitors of p38 MAPK.	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.	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).	Ansaris
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	RhôNe-Poulenc Rorer
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	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.	Novartis Institute For Biomedical Research
21705217	60	Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.	Bristol-Myers Squibb
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
20637613	4	Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.	Daiichi Sankyo
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.	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.	Amgen
20148563	42	BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.	The Institute of Cancer Research
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	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.	Amgen
19327989	40	Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.	Pfizer
19035792	85	Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.	Glaxosmithkline
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.	Bristol-Myers Squibb
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.	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.	Astrazeneca
16216497	67	Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.	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.	Takeda Pharmaceutical
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
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.	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.	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).	Bristol-Myers Squibb Pharmaceutical Research Institute
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12565927	24	Imidazopyrimidines, potent inhibitors of p38 MAP kinase.	Johnson & Johnson Pharmaceutical Research and Development
12540232	53	Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.	Merck Research Laboratories
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
11549467	85	Substituted imidazoles as glucagon receptor antagonists.	Merck Research Laboratories
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
30792101	3	Design and molecular modeling of novel P38? MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.	National Research Centre
26914744	24	Chemical Space of DNA-Encoded Libraries.	University of Utah
30755337	95	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
31550662	109	Progress in the development of more effective and safer analgesics for pain management.	University of Catania
30817889	11	Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.	Shanghai Jiao-Tong University School of Medicine
31693351	473	Discovery of 4	TBA
9873604	72	Pyrroles and other heterocycles as inhibitors of p38 kinase.	Merck Research Laboratory
30384048	365	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
31526603	379	Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.	Takeda Pharmaceutical
31188592	39	Why Some Targets Benefit from beyond Rule of Five Drugs.	Boston University
28291685	12	Synthesis and molecular docking studies of new furochromone derivatives as p38? MAPK inhibitors targeting human breast cancer MCF-7 cells.	Cairo University
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.	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.	Abbvie Bioresearch Center
23941661	5	KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.	Vu University Amsterdam
24332487	46	Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.	The Scripps Research Institute
23746475	93	The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode.	Bristol-Myers Squibb Pharmaceutical Research Institute
30978288	113	A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.	Northwestern University
18157122	1	High-content single-cell drug screening with phosphospecific flow cytometry.	Stanford University
17095218	3	Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.	Paradigm Therapeutics
17411025	12	Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.	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.	Merck Research Laboratories
16750367	2	The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.	Procter and Gamble Pharmaceuticals
15139749	35	Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.	Procter and Gamble Pharmaceuticals
12852754	143	Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.	Eberhard-Karls-University T£Bingen
12061876	53	From imidazoles to pyrimidines: new inhibitors of cytokine release.	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.	Aventis Pharma
11585447	16	Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.	Vertex Pharmaceuticals
30082069	359	ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.	Vertex Pharmaceuticals
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals
29291937	40	Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.	Takeda Pharmaceutical
29107542	35	Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.	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.	University of Zagreb
21985426	27	Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.	Ondokuz Mayis University
9933142	67	Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.	Eli Lilly