Table 2.

In vitro biological activity of 13–15. 11 for comparison.

ID	Structure	EC50(FXR)[a] (efficacy)	IC50(LTA4H)[b] (max. inhib.)
11		0.0010±0.0003 μM (35±1 %)	0.55±0.06 μM (98.2±0.1 %)
13		antagonist	0.28±0.02 μM (90.8±0.3 %)
14		0.017±0.006 μM (21±1 %)	0.95±0.01 μM (97.9±0.1 %)
15		0.07±0.02 μM (56±1 %)	2.1±0.1 μM (89.6±0.6 %)

[a] FXR modulation was determined in a full‐length FXR reporter gene assay based on the human FXR response element from the BSEP promoter. Efficacy refers to maximum FXR activation relative to the activity of 3 μM GW4064 which was defined as 100 % activation. The activity of 13–15 on FXR has been previously reported^[25]. Data are the mean±S.E.M., n≥3. [b] LTA4H inhibition was determined on recombinant protein using L‐arginine‐7‐amino‐4‐methylcoumarine as fluorogenic substrate. Maximum inhibition (max. inhib.) refers to LTA4H inhibition at the highest tested concentration. Data are the mean±S.E.M., n=3.