AZD-7762是一种强效的 ATP 竞争性检查点激酶 (Chk) 抑制剂，对 Chk1 的 IC50 为 5 nM。

Rabusertib(LY2603618) 是一种高效且选择性的 Chk1 抑制剂，IC50 为 7 nM。

SCH 900776 (MK-8776) is a selective and highly potent CHK1 inhibitor with IC50 value of 3nM, modest to CDK2 and Chk2 with much higher IC50 values of 160nM and 1.5uM, respectively.

CHIR-124 is a potent Chk1 inhibitor with IC50 of 0.3 nM with 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.

PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows ~100-fold selectivity for Chk1 than Chk2.

CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM.

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC (50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G (2) arrest with an IC (50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.

LY2606368 (Prexasertib) is a selective Chk1 inhibitor with IC50 value <1nM, modest to Chk2 and Rsk with IC50 values of 8nM and <10nM.