BI-1935
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. |