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Bioorg Med Chem Lett. 2012 Sep 1;22(17):5392-5. doi: 10.1016/j.bmcl.2012.07.046. Epub 2012 Jul 20.

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

Author information

1
Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA. zihao.hua@amgen.com

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.

PMID:
22877629
DOI:
10.1016/j.bmcl.2012.07.046
[Indexed for MEDLINE]

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