Table 1. TGR5 and FXR Activities of Natural and Semisynthetic BAs^a6,15.

	TGR5b		FXRc
BA	EC50	efficacyd	EC50	efficacyd
CA (1)	13.6 ± 0.7	101	>100	0
CDCA (2)	6.7 ± 0.3	105	13.0 ± 0.7	62
INT-777 (3)	0.82 ± 0.04	166	>100	18
4	160 ± 8	194	>100	0
5	25 ± 1	148	55 ± 3	132
6	87 ± 4	198	22 ± 1	121
7	0.65 ± 0.03	120	11.5 ± 0.6	210

^aData represent mean values ± SDs of at least three independent experiments.

^bUnits are μM for EC₅₀ and % of 10 μM LCA (EC₅₀: 5 μM) value for efficacy.

^cUnits are μM for EC₅₀ % of 10 μM CDCA (2) value for efficacy.

^dEfficacy values are here used as a measure of fluorescence change.