PMID

Data

Article Title

Organization

Non-kinase targets of protein kinase inhibitors.

The University of Sydney

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

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

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Merck Research Laboratories

p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.

Glaxosmithkline

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

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

Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.

Korea University

The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.

TBA

A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.

Nerviano Medical Sciences Oncology

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.

Pfizer

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Bristol-Myers Squibb Research and Development

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford

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

Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.

Pfizer

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.

RhôNe-Poulenc Rorer

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.

Pfizer

3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.

Roche Palo Alto

Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.

Korea Institute of Science and Technology

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Vertex Pharmaceuticals

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

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Specificity and mechanism of action of some commonly used protein kinase inhibitors.

University of Dundee

Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.

Daiichi Sankyo

Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.

Pfizer

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

Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.

Roche Palo Alto

Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Amgen

Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles.

Scios

Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.

The University of Texas At Austin

Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Amgen

3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Amgen

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

Glaxosmithkline

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.

Glaxosmithkline

Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.

Merck Research Laboratories

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

Design, Synthesis, and Biological Characterization of Inhaled p38?/? MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.

Chiesi Farmaceutici

High-Throughput Screening Platform in Postnatal Heart Cells and Chemical Probe Toolbox to Assess Cardiomyocyte Proliferation.

Christian-Albrechts University of Kiel

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

Rapid computational identification of the targets of protein kinase inhibitors.

University of Iowa

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Bristol-Myers Squibb

Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.

Johann Wolfgang Goethe University

Discovery of New Imidazo[2,1-

National Research Centre (Nrc)

SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.

Merck Research Laboratories

Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.

Sichuan University/Collaborative Innovation Center of Biotherapy

From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.

Sichuan University

The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38? MAP kinase inhibitors.

Astrazeneca

Selective targeting of the ?C and DFG-out pocket in p38 MAPK.

Johann Wolfgang Goethe University

Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.

Bayer Research Center

Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.

China Pharmaceutical University

Identification of 6-amino-1

University of Dundee

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.

Bayer Research Center

SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.

Novartis Pharma

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

Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.

Shanghai Jiao-Tong University School of Medicine

Discovery of 4

TBA

Pyrroles and other heterocycles as inhibitors of p38 kinase.

Merck Research Laboratory

Discovery of potent p38? MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.

University of Perugia

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

Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors.

Johann Wolfgang Goethe-University

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

Bristol-Myers Squibb Pharmaceutical Research Institute

A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.

Northwestern University

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals