Table 1 Potency and physicochemical characterization of initial leads.

From: Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development

 

1

2

AKT IC50 (µM)

 AKT1

2.5

0.1

 AKT2

3.3

0.4

 AKT3

6.1

5.6

PC3, pGSK3β ELISA IC50 (µM)

3.0

0.1

Kinetic solubility pH7.4 (µM)

206

191

MW/clogP

371/3.8

385/3.3

AKT1 ligand efficiency (LE)

0.28

0.34

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