PMID

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Article Title

Organization

Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

Abbvie Bioresearch Center

Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors.

University of North Carolina At Chapel Hill

An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.

Chinese Academy of Sciences

AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.

University of Edinburgh

Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.

Chinese Academy of Sciences (Cas)

Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.

Chinese Academy of Sciences

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

(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.

Genomics Institute of The Novartis Research Foundation

Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.

Shanghai Institute of Materia Medica

Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.

Chinese Academy of Sciences

UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

University of North Carolina At Chapel Hill

Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.

Eshelman School of Pharmacy�Department of Pharmacology�Lineberger Compreh

Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.

University of North Carolina At Chapel Hill

Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.

Chinese Academy of Sciences

Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.

Chinese Academy of Sciences

Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.

Institut Curie

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents.

Beijing Institute of Pharmacology & Toxicology

Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.

Chinese Academy of Sciences

Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

TBA

Pyrazine-based Syk kinase inhibitors.

RhôNe-Poulenc Rorer

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Harvard Medical School

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Ambit Biosciences

Novel 8-arylated purines as inhibitors of glycogen synthase kinase.

Institut Curie

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

Glaxosmithkline

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.

Bristol-Myers Squibb

Development of [

Monash University

Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6

Sichuan University

Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.

Chinese Academy of Sciences

UNC5293, a potent, orally available and highly MERTK-selective inhibitor.

University of North Carolina At Chapel Hill

Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-

The Genomics Institute of The Novartis Research Foundation

Design and Development of a Chemical Probe for Pseudokinase Ca

Goethe University Frankfurt Am Main

Optimization of an Imidazo[1,2-

Astrazeneca

Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.

Chinese Academy of Sciences

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

Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.

Astrazeneca

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

Beijing Normal University

Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.

Vertex Pharmaceuticals

Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors.

College of Pharmacy of Liaoning University

Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.

China Pharmaceutical University

Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.

Shenyang Pharmaceutical University

Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.

Biocon Bristol Myers Squibb Research Center

Efficacy and Tolerability of Pyrazolo[1,5-

The Genomics Institute of The Novartis Research Foundation

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

Merck

4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.

Chinese Academy of Sciences

Discovery of 4

TBA

Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.

Central China Normal University

Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.

Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital

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

Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors.

Korea University

Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical

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

Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

Unc Eshelman School of Pharmacy

Design, synthesis, biological evaluation and cellular imaging of imidazo[4,5-b]pyridine derivatives as potent and selective TAM inhibitors.

Psl Research 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

Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.

University of Edinburgh

Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.

University of Chinese Academy of Sciences