PMID

Data

Article Title

Organization

p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.

Merck & Co.

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

Potent inhibitors of the MAP kinase p38.

R. W. Johnson Pharmaceutical Research Institute

Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.

SmithKline Beecham Pharmaceuticals Ltd

Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.

Sejong University

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 and Company

Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.

Translational Research Institute

Inhibitors of c-Jun N-terminal kinases: an update.

Eberhard Karls Universit£t T£bingen

SAR156497, an exquisitely selective inhibitor of aurora kinases.

Sanofi

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals Inc

Pyridazine based inhibitors of p38 MAPK.

Merck Research Laboratories

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

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

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

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

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

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

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals Inc

Imidazopyrimidines, potent inhibitors of p38 MAP kinase.

Johnson & Johnson Pharmaceutical Research and Development LLC

Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.

Merck Research Laboratories

Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp

Takeda Research in California

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Merck Research Laboratories

Substituted imidazoles as glucagon receptor antagonists.

Merck Research Laboratories

Design and molecular modeling of novel P38? MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.

National Research Centre

Chemical Space of DNA-Encoded Libraries.

University of Utah

Progress in the development of more effective and safer analgesics for pain management.

University of Catania

Pyrroles and other heterocycles as inhibitors of p38 kinase.

Merck Research Laboratory

Why Some Targets Benefit from beyond Rule of Five Drugs.

Boston University

Synthesis and molecular docking studies of new furochromone derivatives as p38? MAPK inhibitors targeting human breast cancer MCF-7 cells.

Cairo University

KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.

VU University Amsterdam

Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.

The Scripps Research Institute

The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode.

Bristol-Myers Squibb Pharmaceutical Research Institute

High-content single-cell drug screening with phosphospecific flow cytometry.

Stanford University

Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.

Paradigm Therapeutics Ltd

Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.

Eberhard-Karls-University T£bingen

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

The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.

Procter and Gamble Pharmaceuticals

Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.

Procter and Gamble Pharmaceuticals

Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.

Eberhard-Karls-University T£bingen

From imidazoles to pyrimidines: new inhibitors of cytokine release.

Eberhard-Karls-University T£bingen

An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.

Aventis Pharma S.A.

Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.

Vertex Pharmaceuticals Inc

Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.

Takeda Pharmaceutical Company Limited

Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

Novartis Institutes for Biomedical Research

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