Table 1.

A summary of the general properties of LY2606368 in biochemical and biologic assays (see Supplementary Data for additional details)

General characteristics of LY2606368
Ki0.9 nmol/L (ATP competitive)
IC50 CHK1 enzyme<1 nmol/L
IC50 CHK2 enzyme8 nmol/L
EC50 HT-29 CHK1 autophosphorylation (S296)1 nmol/L
EC50 HT-29 CHK2 autophosphorylation (S516)<31 nmol/L
EC50 HeLa G2–M checkpoint abrogation9 nmol/L
IC50 proliferation HT-2910 nmol/L
IC50 proliferation HeLa37 nmol/L
IC50 proliferation U-2 OS3 nmol/L
IC50 proliferation Calu-63 nmol/L
IC50 proliferation NCI-H46068 nmol/L
IC50 proliferation HCT 116>1,000 nmol/L
IC50 proliferation Panc-1>1,000 nmol/L

NOTE: All IC50 and EC50 calculations are absolute values.