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. 2021 May 24;16(15):2366–2374. doi: 10.1002/cmdc.202100118

Table 3.

In vitro biological activity of 16–20. 8 for comparison.

ID

Structure

EC50(FXR)[a] (efficacy)

IC50(LTA4H)[b] (max. inhib.)

8

graphic file with name CMDC-16-2366-g024.jpg

0.029±0.006 μM (22±1 %)

0.14±0.01 μM (98.8±0.1 %)

16

graphic file with name CMDC-16-2366-g003.jpg

>30 μM

0.20±0.02 μM (98.8±0.1 %)

17

graphic file with name CMDC-16-2366-g005.jpg

>30 μM

1.9±0.1 μM (97.0±0.2 %)

18

graphic file with name CMDC-16-2366-g001.jpg

1.6±0.4 μM (35±2 %)

0.13±0.01 μM (89.5±0.5 %)

19

graphic file with name CMDC-16-2366-g015.jpg

0.46±0.08 μM (21±1 %)

0.45±0.02 μM (98.9±0.1 %)

20

graphic file with name CMDC-16-2366-g014.jpg

11±2 μM (30±1 %)

0,16±0,02 μM (99.7±0.1 %)

[a] FXR modulation has been 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. 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.