Table 1.

Investigations of central hydrophobic contacts

Compound										IC50 (μM)a
2b	Ac-	GR	P	R	-H	-H	V	F	-Bn	28±8
3	Ac-	GR	P	R	-CH3	-H	V	F	-Bn	50±10
4	Ac-	GR	P	R	-Ph	-H	V	F	-Bn	>500
5	Ac-	GR	P	R	-H	-Ph	V	F	-Bn	16±5
6	Ac-	GR	P	R	-H	-Nap	V	F	-Bn	78±14
7			Ac-	R	-Ph	-H	V	F	-Bn	288±100
8			Ac-	R	-H	-Ph	V	F	-Bn	173±31
9 b			Ac-	R	-H	-H	V	F	-Bn	119±36

^aReported values are an average of three independent-binding curves utilizing an IMAP® Akt Assay Kit (Molecular Devices). Reactions were conducted in wells with 20.0 μL of 10 mM Tris–HCl (pH 7.2), 10 mM MgCl₂, 0.1% BSA, 0.05% NaN₃, 1 mM DTT, 100 nM 5FAM-GRPRTSSFAEG-COOH, 5 μM ATP, Akt1, and inhibitor (DMSO stock solution). Reaction mixtures were incubated for 1 h at room temperature and then quenched with 60 μL of the IMAP-binding solution. The reactions were equilibrated for 1 h at room temperature then data points were collected and analyzed.

^bPreviously reported inhibitors.³⁵