Table 1.

In vitro biological activity of 3–12.

ID	Structure	EC50(FXR)[a] (efficacy)	IC50(LTA4H)[b] (max. inhib.)
3		0.026±0.001 μM (34±1 %)	0.54±0.07 μM (97.2±0.4 %)
4		15±3 μM (27±1 %)	1.6±0.2 μM (82.6±0.8 %)
5		inactive (50 μM)	15±2 μM (80±5 %)
6		0.19±0.02 μM (26±1 %)	5.5±0.5 μM (85±2 %)
7		0.014±0.001 μM (29±1 %)	0.37±0.02 μM (97.8±0.1 %)
8		0.029±0.006 μM (22±1 %)	0.14±0.01 μM (98.8±0.1 %)
9		0.15±0.02 μM (56±1 %)	0.61±0.06 μM (96.0±0.2 %)
10		0.009±0.001 μM (20±1 %)	1.1±0.1 μM (94.9±0.2 %)
11		0.0010±0.0003 μM (35±1 %)	0.55±0.06 μM (98.2±0.1 %)
12		0.3±0.1 μM (14±1 %)	5.2±0.6 μM (81.1±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 3–11 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.