Table 1.

SRE.L Activity of 5-Aryl-1,3,4-Oxadiazole-2-thiopropionic acids

Cmpd	R1	R2	R3	R4	SRE.L IC50 (nM)a, b
8a	H	H	H	H	3,500
8b	H	H	Cl	H	340
8c	H	H	Me	H	34
8d	H	H	OMe	H	160
8e	H	Cl	H	H	1,500
1	H	Me	H	H	180
8f	H	OMe	H	H	3,600
8g	Cl	H	H	H	25
8h	Me	H	H	H	6,300
8i	OMe	H	H	H	3,100
8j	Cl	H	Cl	H	4 (2c)
8k	Cl	H	Me	H	1.5
8l	Cl	H	OMe	H	2.6
8m	Cl	Me	Me	H	0.02c
8n	Cl	H	Me	Me	0.23c
8o	Cl	H	Cl	Me	0.32c

^aInhibition of Gα12-stimulated SRE.L activity (mean of n = 3, SEM < 10%) in PC3 cells unless otherwise noted.

^bCell viability and proliferation assay with WST-1 < 5% inhibition up to 100 μM inhibitor (mean of n = 3, SEM < 10%).

^cSRE.L assay performed in HEK293T cells (mean of n = 3, SEM < 10%).