Extended Data Fig. 3: Small molecule and peptide-based inhibitors disable dasTMPRSS2 activity at varying potencies.
From: Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation
a IC50 plot of the small molecule benzamidine inhibitor, measuring residual dasTMPRSS2 peptidase activity in the presence of 100 µM Boc-QAR-AMC substrate. b IC50 plot of the bicyclic, 14 amino acid peptide inhibitor, sunflower trypsin inhibitor-1 (SFTI-1), measuring residual dasTMPRSS2 peptidase activity in the presence of 10 µM Boc-QAR-AMC. Synthesis and purification of this compound is available in Methods. c IC50 plot of the nafamostat leaving group, 6-amidino-2-napthol, measuring residual dasTMPRSS2 peptidase activity in the presence of 100 µM Boc-QAR-AMC. All plots have data shown as mean + /- SD for n = 3 technical replicates and curve fit for absolute IC50 in GraphPad. Consistent IC50 plots were obtained for n = 2 independent biological experiments.
