Table 1. Enzyme Inhibition (IC50), SARS-CoV-2 Antiviral Activity (EC50), and Cellular Toxicity (CC50).
| Compound | IC50a (μM) | EC50b (μM) | CC50c (μM) |
|---|---|---|---|
| 7 | 1.59 | >20 | >100 |
| 6 | 0.28 | 0.5 (0.4–0.6) | >100 |
| 51 | 0.12 | >20 | >100 |
| 35 | 0.10 | 0.82 (0.7–1) | >100 |
| 36 | 0.055 | 1.35 (1.1–1.6) | >100 |
| 37 | 0.043 | 2.4 (2.1–2.6) | >100 |
| 38 | 0.021 | 1.89 (1.0–3.4) | >100 |
| 39 | 0.017 | 5.0 (4.1–5.9) | >100 |
| 40 | 0.016 | 10.2 (7.6–14) | >100 |
| 41 | 0.013 | 6.76 (4.8–9.2) | >100 |
| 42 | 0.012 | 19.3 | >100 |
| 43 | 0.0086 | 0.13 (0.11–0.14) | >100 |
| 44 | 0.0056 | 3.3 (2.9–3.7) | >100 |
| 45 | 0.012 | 0.82 (0.7–0.9) | >100 |
| 3 | 0.026 (lit.10 0.028) | – | – |
| S-217622 | – | 0.23 (0.21–0.26) | – |
a
SARS-CoV-2 recombinant protease enzymatic assay.
b
Cellular antiviral activity assay against SARS-CoV-2 with recombinant SARS-CoV-2-Nluc reporter virus in VeroE6/TMPRSS2 cells. Parentheses denote 95% confidence intervals for EC50 calculations.
c
Cellular cytotoxicity.