Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594549 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zihao Hua, Xin Huang, Howard Bregman, Nagasree Chakka, Erin F. DiMauro, Elizabeth M. Doherty, Jon Goldstein, Hakan Gunaydin, Hongbing Huang, Stephanie Mercede, John Newcomb, Vinod F. Patel, Susan M. Turci, Jie Yan, Cindy Wilson, Matthew W. Martin,