Table 1

Potency of bile acids for binding to FXR as determined in the cell-free ligand-sensing assay (25). The indicated values for CDCA and its conjugates are EC50's derived from dose response analysis as described in Fig. 3B. The indicated values for other bile acids and their conjugates are half-maximal inhibitory concentrations (IC50's) derived from dose response analysis as described in Fig. 3C.

Bile acidFree acid Glycine conjugateTaurine conjugate
CDCA4.5 μM10 μM10 μM
CA>1000 μM >1000 μM>1000 μM
LCA3.8 μM4.7 μM3.8 μM
DCA100 μM≥500 μM≥500 μM
MCA >1000 μMNot tested≥500 μM