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BI-1915

2D structure
Target CTSS 
Mode of action Inhibitor
Control BI-1920
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) CTSS binding (SPR): Kd = 31 nM; CTSS inhibition (luminescent based enzymatic assay): IC50 = 17 nM
Selectivity within target family: > 30-fold IC50 [µM]: CTSK ( > 10) , CTSL ( > 30) , CTSB ( > 10)
Reaction Biology protease panel (43) at 10 µM: clean, except for papain (87 % inhibition)
Selectivity outside target family Eurofins Cerep SafetyScreen44 at 10 µM: clean
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Antigen challenge cell assay (based on the use of B cells to 'present' exogenous antigen (added ovalbumin) via a cathepsin S dependent process to T cells): IC50 = 2.8 nM
Effectively blocks the specific secretion of ovalbumin-induced IL-2 in T-cells.
Control compound (100 times less potent than the probe) BI-1920: CTSS binding (SPR): Kd = 272 nM; CTSS inhibition (luminescent based enzymatic assay): IC50 > 20 µM; Eurofins Cerep SafetyScreen44 at 10 µM: clean