BI-1942
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | IC50 = 0.4 nM |
| Selectivity within target family: > 30-fold | Eurofins protease panel (35 at 10 µM): Only off-target is CTSG (cathepsin G, IC50 = 110 nM, > 100-fold selective) |
| Selectivity outside target family | Eurofins SafetyScreen (44) at 10 µM: cleanClean PDSP scan with one off-target: HTR1D (Ki = 1130.61 nM) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Angiotensin II formation by CMA1 in human plasma IC50 = 198 nM |
| Control compound (100 times less potent than the probe) | No control; Note: BI-1829, a closely related structural analog, shows 1000-fold less activity, but is only suitable for use as an in vitro control, due to potential hydrolysis of the methyl-ester and no data on the Chymase inhibitory potency of the free acid form of BI-1829. |