Table 6 Selectivity of the bispecific inhibitor against different human proteases
From: An orally available Mpro/TMPRSS2 bispecific inhibitor with potent anti-coronavirus efficacy in vivo
Host protease | Inhibition (%) | STD (%) | Concentration (μM) | Type | SI for Mpro | SI for TMPRSS2 |
|---|---|---|---|---|---|---|
Calpain 1 | 4.89 | 8.63 | 100 | Cys | 323 | >78 |
Caspase-2 | 21.67 | 5.64 | 100 | Cys | 323 | >78 |
Chymotrypsin | -14.65 | 22.65 | 50 | Ser | 161 | >39 |
Cathepsin L | 19.89 | 2.69 | 100 | Cys | 323 | >78 |
Cathepsin D | 0.66 | 2.03 | 100 | Aps | 323 | >78 |
Neutrophil Elastase | 6.37 | 1.14 | 100 | Ser | 323 | >78 |
Thrombin | 30.86 | 2.12 | 100 | Ser | 323 | >78 |
