Table 1.

Summary table showing biochemical potency, selectivity profile, and functional assay metrics of GNE-900

Kinase assaysIC50 (μmol/L)
ChKl0.0011
ChK21.5
Aurora A5.07
Aurora B1.86
CDKl/Cyclin B0.706
CDK2/Cyclin A0.366
PLK1>1
Cellular assays (HT-29)
Checkpoint abrogation EC50 (p-Histone H3)61.8 nmol/L
EC10-fold shift (gemcitabine)12 nmol/L
Combination index (CI)0.06
Single agent Gl508.7 μmol/L