2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors.

Bioorg Med Chem Lett

Authors	Zihao Hua Xin Huang Howard Bregman Nagasree Chakka Erin DiMauro Elizabeth Doherty Jon Goldstein Hakan Gunaydin Hongbing Huang Stephanie Mercede John Newcomb Vinod Patel Susan Turci Jie Yan Cindy Wilson Matthew Martin
Keywords	Animals Humans Mice Binding Sites Rats Models, Molecular Protein Isoforms Structure-Activity Relationship Protein Kinase Inhibitors Benzimidazoles beta Catenin Casein Kinase I
Abstract	Screening of the Amgen compound library led to the identification of 2-phenylamino-6-cyano-1H-benzimidazole 1a as a potent CK1 gamma inhibitor with excellent kinase selectivity and unprecedented CK1 isoform selectivity. Further structure-based optimization of this series resulted in the discovery of 1h which possessed good enzymatic and cellular potency, excellent CK1 isoform and kinase selectivity, and acceptable pharmacokinetic properties.
Year of Publication	2012
Journal	Bioorg Med Chem Lett
Volume	22
Issue	17
Pages	5392-5
Date Published	2012 Sep 01
ISSN	1464-3405
DOI	10.1016/j.bmcl.2012.07.046
PubMed ID	22877629
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