BAY-678
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | ELANE: IC50 = 20 nM; Ki = 15 nM |
| Selectivity within target family: > 30-fold | > 30-fold selective over 21 serine proteases (for all IC50 > 30 µM) |
| Selectivity outside target family | Radioligand Binding Assays with 64 receptors and transporters at 10 µM: > 30-fold selective; Bayer in house kinase panel (7) at 20 µM: clean; Clean PDSP scan with the closest hit on HTR3 (pKi = 5.55) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Not applicable (extra cellular protease) |
| Control compound (100 times less potent than the probe) | BAY-677: IC50 > 2000 nM; Clean PDSP scan |