PMID

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Article Title

Organization

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

RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency.

Aventis Pharma

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

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

Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.

RhôNe-Poulenc Rorer

Discovery of a novel series of 4-quinolone JNK inhibitors.

Roche Palo Alto

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

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

Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.

Janssen Pharmaceutical Companies of Johnson & Johnson

Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.

TBA

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

Pfizer

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

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

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

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

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

Ambit Biosciences

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

Daiichi Sankyo

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

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

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

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

Amgen

Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Pfizer

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 p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.

Chiesi Farmaceutici

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

Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr

East China Normal University

Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.

East China Normal University

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

The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors.

Astrazeneca

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

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

China Pharmaceutical University

Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Merck

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

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

Novartis Pharma

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

Shanghai Jiao-Tong University School of Medicine

Discovery of 4

TBA

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

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

Docking, synthesis and pharmacological activity of novel urea-derivatives designed as p38 MAPK inhibitors.

Universidade Federal Do Rio De Janeiro

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

Aventis Pharma

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.

Sichuan University/Collaborative Innovation Center of Biotherapy

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

Heteroaryl inhibitors of PDE4

Tetra Discovery Partners

Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors.

Medical University of Lodz