Table 1. In Vitro Inhibition of HSET and Ligand Efficiencies of 1–18.

^aInhibition of recombinant full-length HSET with preformed microtubules and 3 μM ATP measured in ADP-Glo format, mean (±SD) for n ≥ 3.

^bLigand Efficacy was calculated using LE = −1.4Log(IC₅₀ [M])/number of non-hydrogen atoms.

^cLipophilic Ligand Efficacy was determined using the equation LLE = −Log(IC₅₀ [M]) – cLogP, where cLogP was calculated using MoKa from Molecular Discovery.

^dFrom a single determination.

^eInhibition plateaued between 47 and 61%. The mean concentration observed at 50% inhibition was 13 μM.