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. 2023 Feb 7;66(4):2622–2645. doi: 10.1021/acs.jmedchem.2c01591

Table 2. In Vitro Inhibition of HSET and Ligand Efficiencies of 13 and 1932.

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a

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

b

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

c

Lipophilic ligand efficacy was determined using the equation LLE = −Log(IC50 [M]) – cLogP, where cLogP was calculated using MoKa from Molecular Discovery.

d

From a single determination.