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. 2021 Mar 29;4(2):966–979. doi: 10.1021/acsptsci.1c00041

Table 1. In Vitro Potencies of the Study Compounds FXRA/sEHi DM and sEHi MHa.

graphic file with name pt1c00041_0008.jpg

  FXRA/sEHi (DM) sEHi (MH)
IC50 (sEH) 0.004 μM 0.002 μM
EC50 (FXR) 0.02 μM 1.4 μM
efficacy (FXR) 35% 14%
Kd (FXR LBD) 0.13 μM 1.4 μM
a

Efficacy (FXR) refers to the maximum activation efficacy of the respective compound relative to 1 μM GW4064 which is defined as 100%.