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. 2017 Apr 27;9(5):41. doi: 10.3390/cancers9050041

Table 1.

Potent and specific small molecule inhibitors of ATR and CHK1.

CHK1 Inhibitors
Name Structure IC50/Ki Specificity
AZD7762 graphic file with name cancers-09-00041-i001.jpg CHK1 IC50 = 5 nM Equally potent: CHK1/CHK2
V158411 graphic file with name cancers-09-00041-i002.jpg 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 graphic file with name cancers-09-00041-i003.jpg CHK1 Ki = 4.9 nM 100-fold CHK1 vs. CHK2
MK8776/SCH900776 graphic file with name cancers-09-00041-i004.jpg CHK1 IC50 = 3 nM 500-fold CHK1 vs. CHK2
CCT244747 graphic file with name cancers-09-00041-i005.jpg CHK1 IC50 = 8 nM >1000-fold CHK1 vs. CHK2
CCT245737 graphic file with name cancers-09-00041-i006.jpg CHK1 IC50 = 1.3 nM >1500-fold CHK1 vs. CHK2
LY2603618 graphic file with name cancers-09-00041-i007.jpg CHK1 IC50 = 7 nM >1500-fold CHK1 vs. CHK2
ATR Inhibitors
Name Structure IC50/Ki Specificity
NU6027 graphic file with name cancers-09-00041-i008.jpg ATR IC50 = 1 nM ATR, CDK1 (Ki = 2.5 µM), CDK2 (Ki = 1.3 µM)
ETP-46464 graphic file with name cancers-09-00041-i009.jpg ATR IC50 = 25 nM ATR
VE-821 graphic file with name cancers-09-00041-i010.jpg ATR IC50 = 26 nM >100-fold ATR vs. ATM/DNA-PK
VE-822/VX-970 graphic file with name cancers-09-00041-i011.jpg ATR IC50 = 0.2 nM >100-fold ATR vs. ATM/DNA-PK
AZ20 graphic file with name cancers-09-00041-i012.jpg ATR IC50 = 5 nM >600-fold ATR vs. ATM/DNA-PK/PI-3K
AZD6738 graphic file with name cancers-09-00041-i013.jpg ATR IC50 = 1 nM ATR