Table 1. GPBAR1 and LXRs efficacy of compounds 4–30.

Compound	GPBAR1*		LXRα**		LXRβ
	Efficacy		Efficacy		Efficacy
	(% vs TLCA)	(% vs HDCA)	(% vs GW3965)	(% vs HDCA)	(% vs GW3965)
HDCA	26		15, 5		NA***
4	26, 3	101, 0	49, 3	317, 1	NA
5	14, 9	57, 5	72, 8	468, 1	NA
6	65, 0	249, 8	32, 6	209, 7	NA
7	26, 3	101, 2	28, 0	180, 1	NA
8	25, 5	98, 0	42, 9	276, 3	NA
9	27, 0	103, 9	54, 1	348, 3	NA
10	26, 0	100, 0	12, 2	78, 5	NA
11	33, 2	127, 7	26, 2	168, 3	NA
12	18, 6	71, 7	63, 1	406, 1	NA
13	52, 6	202, 4	36, 1	232, 0	NA
14	55, 1	211, 9	109, 3	703, 3	NA
15	68, 7	264, 0	NA	—	NA
16	53, 7	206, 6	23, 8	153, 0	NA
17	53, 1	204, 3	17, 3	111, 7	NA
18	22, 8	87, 6	NA	—	NA
19	75, 1	288, 7	NA	—	NA
20	74, 0	284, 6	20, 0	128, 6	NA
21	73, 0	280, 7	NA	—	NA
22	77, 1	296, 5	NA	—	NA
23	59, 6	229, 1	NA	—	NA
24	92, 9	357, 1	NA	—	NA
25	58, 1	223, 2	NA	—	NA
26	50, 9	195, 8	NA	—	NA
27	64, 4	247, 7	NA	—	NA
28	54, 9	211, 1	NA	—	NA
29	96, 0	368, 8	15, 0	96, 7	NA
30	58, 1	223, 5	NA	—	NA

^*Activity toward GPBAR1 in a reporter assay was assessed in HEK-293T cells transfected with a cAMP responsive element (CRE) cloned upstream to the luciferase gene. For calculation of efficacy data, maximal transactivation of CRE caused by each compound (10 μM) was compared to maximal transactivation caused by TLCA (10 μM) and by HDCA (10 μM).

^**Activity toward LXRα in a reporter assay was assessed in HepG2 cells transfected with an LXRα responsive element (LRE) cloned upstream to the luciferase gene. For calculation of efficacy data, maximal transactivation of LRE caused by each compound (10 μM) was compared to maximal transactivation caused by GW3965 (10 μM) and by HDCA (10 μM).

^***NA: no activity at 10 μM.