Table 1.
CHK1 Inhibitors | |||
Name | Structure | IC50/Ki | Specificity |
AZD7762 | CHK1 IC50 = 5 nM | Equally potent: CHK1/CHK2 | |
V158411 | CHK1 IC50 = 4.4 nM | Equally potent: CHK1/CHK2; 20-fold CHK1 vs. CHK2 in cells (Cellular CHK1 IC50 = 48 nM vs. CHK2 IC50 = 904 nM) | |
PF477736 | CHK1 Ki = 4.9 nM | 100-fold CHK1 vs. CHK2 | |
MK8776/SCH900776 | CHK1 IC50 = 3 nM | 500-fold CHK1 vs. CHK2 | |
CCT244747 | CHK1 IC50 = 8 nM | >1000-fold CHK1 vs. CHK2 | |
CCT245737 | CHK1 IC50 = 1.3 nM | >1500-fold CHK1 vs. CHK2 | |
LY2603618 | CHK1 IC50 = 7 nM | >1500-fold CHK1 vs. CHK2 | |
ATR Inhibitors | |||
Name | Structure | IC50/Ki | Specificity |
NU6027 | ATR IC50 = 1 nM | ATR, CDK1 (Ki = 2.5 µM), CDK2 (Ki = 1.3 µM) | |
ETP-46464 | ATR IC50 = 25 nM | ATR | |
VE-821 | ATR IC50 = 26 nM | >100-fold ATR vs. ATM/DNA-PK | |
VE-822/VX-970 | ATR IC50 = 0.2 nM | >100-fold ATR vs. ATM/DNA-PK | |
AZ20 | ATR IC50 = 5 nM | >600-fold ATR vs. ATM/DNA-PK/PI-3K | |
AZD6738 | ATR IC50 = 1 nM | ATR |