Table 2 Inhibitory activity (Ki) of synthesized TMPRSS2 inhibitors 1–8 against TMPRSS2, matriptase, thrombin, and factor Xa.
From: Peptidomimetic inhibitors of TMPRSS2 block SARS-CoV-2 infection in cell culture
Ki [nM] | Selectivity indices | ||||||
|---|---|---|---|---|---|---|---|
Compound | TMPRSS2 | Matriptase | Thrombin | Factor Xa | Matriptase | Thrombin | Factor Xa |
1 | 86.7 | 1.7 | 2077 | 4.1 | 0.02 | 24 | 0.05 |
2 | 3.8 | 3.3 | 599 | 106.7 | 0.9 | 158 | 28.1 |
3 | 9.1 | 14.0 | 4088 | 271.3 | 1.5 | 449 | 29.8 |
4 | 8.5 | 11.5 | 7217 | 331 | 1.4 | 849 | 38.9 |
5 | 2.5 | 5.2 | 1046 | 41.1 | 2.1 | 418 | 16.4 |
6 | 71.5 | 75.6 | >50,000 | 472.4 | 1.1 | >699 | 6.6 |
7 | 57.7 | 30 | >50,000 | 94.1 | 0.5 | >867 | 1.6 |
8 | 215.9 | 159.8 | >50,000 | 965.5 | 0.7 | 232 | 4.5 |
CM | 0.4 | 0.6 | >50,000 | 1785.5 | 1.5 | >12,500 | 4,464 |
FOY-251 | 9.7 | 173.4 | >50,000 | 697 | 17.9 | >5155 | 71.9 |
