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 |
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University Of Sydney |
| 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 |
| 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. |
Aska Pharmaceutical |
| 25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
| 19772287 |
67 |
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression. |
Glaxosmithkline |
| 22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
| 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. |
Astellas Pharma |
| 22858099 |
52 |
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy. |
Korea University |
| 24900264 |
106 |
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor. |
TBA |
| 18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
| 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 |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 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 |
| 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 |
| 21888439 |
7 |
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. |
Pfizer |
| 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 |
| 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 |
| 21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
| 21515047 |
24 |
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead. |
Roche Palo Alto |
| 21489792 |
26 |
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors. |
Korea Institute Of Science And Technology |
| 21391610 |
139 |
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. |
Vertex Pharmaceuticals |
| 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 inhibitors |
Roche Palo Alto |
| 20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 10998351 |
24 |
Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
University Of Dundee |
| 20637613 |
4 |
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3. |
Daiichi Sankyo |
| 20227876 |
69 |
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase. |
Pfizer |
| 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 |
| 19950901 |
23 |
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. |
Roche Palo Alto |
| 20138761 |
30 |
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase. |
Amgen |
| 20071169 |
9 |
Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles. |
Scios |
| 19822424 |
4 |
Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles. |
The University Of Texas At Austin |
| 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 |
| 18817364 |
41 |
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase. |
Amgen |
| 18614366 |
97 |
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity. |
Glaxosmithkline |
| 18602262 |
56 |
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
Glaxosmithkline |
| 17855341 |
4 |
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation. |
Merck Research Laboratories |
| 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 |
| 15943486 |
8 |
Rapid computational identification of the targets of protein kinase inhibitors. |
University Of Iowa |
| 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 |
| 15566298 |
34 |
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. |
Bristol-Myers Squibb |
| 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 |
| 14592489 |
71 |
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors. |
Merck Research Laboratories |
| 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 |
| 12039561 |
30 |
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
Bayer Research Center |
| 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 |
| 10999468 |
30 |
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. |
Bayer Research Center |
| 10866395 |
33 |
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors. |
Novartis Pharma |
| 9873604 |
72 |
Pyrroles and other heterocycles as inhibitors of p38 kinase. |
Merck Research Laboratory |
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