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BI-1942

2D structure
Target CMA1 
Targeted domain Protease domain
Mode of action Inhibitor
Control
Recommended cellular usage concentration 1 µM
In vivo use No
Donated by Boehringer Ingelheim


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: clean
Clean 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.