1397706-32-9Relevant articles and documents
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors
Hua, Zihao,Huang, Xin,Bregman, Howard,Chakka, Nagasree,Dimauro, Erin F.,Doherty, Elizabeth M.,Goldstein, Jon,Gunaydin, Hakan,Huang, Hongbing,Mercede, Stephanie,Newcomb, John,Patel, Vinod F.,Turci, Susan M.,Yan, Jie,Wilson, Cindy,Martin, Matthew W.
, p. 5392 - 5395 (2012/09/22)
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.
