PMID

Data

Article Title

Organization

Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).

Takeda California

Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.

Southeast University

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

Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.

Universit£

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Ansaris

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Bristol-Myers Squibb Research and Development

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.

Pfizer

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

Ambit Biosciences

Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).

University of Zurich

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

Glaxosmithkline

Novel anilinopyrimidine derivatives as potential EGFR

Southeast University

Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.

Zhejiang University

Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.

Promega

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

Beijing Normal University

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

Johann Wolfgang Goethe University

Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3?-carbamoyloxy derivative with antiangiogenetic properties.

University of Parma

Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).

University of North Carolina At Chapel Hill

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

Merck

Discovery of 4

TBA

Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.

Southeast University

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

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

Takeda Pharmaceutical