Table 1. BAR502 is dual FXR and GPBAR1 ligand.

GPBAR1*		FXR**
Affinity(μM)	Efficacy (% vs TLCA)	Affinity (μM)	Efficacy (% vs 6-ECDCA)
0.4 ± 0.1	79.5 ± 11.8	2.0 ± 0.2	325.0 ± 38.1

Data are mean ± SE of 3 experiments in duplicate

* Activity of BAR502 toward GPBAR1 in a reporter assay was assessed in HEK293T cells transfected with a cAMP responsive element (CRE) cloned upstream to the luciferase gene (see Materials and Methods). For calculation of efficacy data, maximal transactivation of CRE caused by BAR502 (10 μM) was compared to maximal transactivation caused by TLCA (10 μM).

** Activity of BAR502 toward FXR in a reporter assay was assessed in HepG2 cells transfected with a FXR responsive element (FRE) cloned upstream to the luciferase gene (see Materials and Methods). For calculation of efficacy data, maximal transactivation of FRE caused by BAR502 (10 μM) was compared to maximal transactivation caused by 6-ECDCA (10 μM).