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BI-1935

2D structure
Target EPHX2 
Targeted domain catalytic domain
Mode of action Inhibitor
Control BI-2049
Recommended cellular usage concentration < 1 nM
In vivo use Yes
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) Inhibition of human EPHX2 and rat EPHX2: IC50 = 7 nM
Selectivity within target family: > 30-fold Internal screen against h CYP2J2/ CYP2C9/ CYP2C19 and IL2: > 100-fold selectivity achieved (> 1 μM for all)
Selectivity outside target family Off Target Screen - Panlabs panel: 61/67 < 20% Inhibition @ 10 μM, 5/67 < 80% Inhibition @ 10 μM, TBXAS1 96% inhibition @ 10 μM (IC50 = 0.132 μM); Clean PDSP scan with the closest hit on SLC6A3 (pKi = 5.3)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Cellular EPHX2 assay (DHET, h EPHX2): IC50 < 1 nM
Control compound (100 times less potent than the probe) BI-2049: IC50 > 3 μM (h EPHX2)
Clean PDSP scan.