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BI-3231

2D structure
Target HSD17B13 
Targeted domain Ser172, Tyr185 (catalytical triad)
Mode of action Inhibitor
Control BI-0955
Recommended cellular usage concentration 1 µM
In vivo use Yes
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) hHSD17B13: Ki = 0.7 ± 0.2 nM (Enzymatic assay); DSF (temperature shift): 16.7 K in the presence of NAD+
Selectivity within target family: > 30-fold hHSD17B11: IC50 > 10 µM (enzymatic assay)
Selectivity outside target family Eurofins Safety screen (44 targets) at 10 µM: clean except for PTGS2 (COX2) (49% ctrl)
Clean PDSP scan (43 targets at 10 µM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 IC50 = 11 ± 5 nM (Cellular hHSD17B13 assay, HEK cells)
Control compound (100 times less potent than the probe) BI-0955: Ki = > 10 µM (Enzymatic hHSD17B13 assay); IC50 > 10 µM (Cellular hHSD17B13 assay); Eurofins Safety screen (44 targets): PTGS2 (COX2) (44% ctrl), HTR2B (45 % ctrl)
Clean PDSP scan (43 targets at 10 µM)