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Updated: Jul 19, 2026

Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
Identification of novel, selective and potent Chk2 inhibitors
Gary Larson1, Shunqi Yan, Huanming Chen
1Drug Discovery, Valeant Pharmaceutical Research and Development 3300 Hyland Avenue, Costa Mesa, CA 92626, USA.
Abstract:
A series of isothiazole carboxamidine compounds were synthesized and discovered as novel and selective inhibitors for Chk2. They are not active against the related Chk1 kinase. The structure-activity relationship studies were performed on the scaffold, and enzymatic kinetic analysis showed they are simple ATP competitive inhibitors with K(i) values as low as 11 nM for Chk2. Computer modeling studies were employed to comprehend the mechanism of action and SAR of these compounds.
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M cyclin...