Table 1.
SARS-CoV-2 3CLpro inhibitory activities (μM) of various reported inhibitors. Numbers in parentheses represent relative potencies based on in-house IC50 values, e.g. (1) = most potent.
| Compound | In-house IC50 (μM) | Literature IC50 or Ki (μM) | CoV-1 or CoV-2 3CLpro1 | Literature reference |
|---|---|---|---|---|
| 2i | (8) 0.094 ± 0.006 | 1.7 (IC50) | CoV-1 | 26 |
| 3 | (9) 0.286 ± 0.014 | 0.66 (Ki) | CoV-1 | 19 |
| 11a | (3) 0.014 ± 0.001 | 0.053 ± 0.005 (IC50) | CoV-2 | 20 |
| 0.031 ± 0.003 (IC50) | CoV-2 | 23 | ||
| 11b | (4) 0.023 ± 0.003 | 0.040 ± 0.002 (IC50) | CoV-2 | 20 |
| 17 | (7) 0.065 ± 0.007 | 0.007 (IC50) | CoV-1 | 24 |
| 25c | >10 | 21.0 (IC50) | CoV-1 | 27 |
| Boceprevir | >10 | 4.13 ± 0.61 (IC50) | CoV-2 | 16 |
| 5.40 ± 1.53 (IC50) | CoV-2 | 29 | ||
| Calpeptin | >10 | 10.69 ± 0.28 (IC50) | CoV-2 | 16 |
| 4.81 ± 0.18 (IC50) | CoV-2 | 31 | ||
| GC-373 | (6) 0.042 ± 0.001 | 0.40 ± 0.05 (IC50) | CoV-2 | 21 |
| GC-376 | (5) 0.034 ± 0.001 | 0.030 ± 0.008 (IC50) | CoV-2 | 16 |
| 0.031 ± 0.004 (IC50) | CoV-2 | 23 | ||
| MG-115 | >10 | 3.14 ± 0.97 (IC50) | CoV-2 | 16 |
| MG-132 | >10 | 3.90 ± 1.01 (IC50) | CoV-2 | 16 |
| PF-0835231 | (1) 0.008 ± 0.001 | 0.004 ± 0.0003 (IC50) | CoV-1 | 22 |
| Telaprevir | >10 | 11.47 (IC50) | CoV-2 | 25 |
| TG-0205221 | (2) 0.009 ± 0.001 | 0.053 (Ki) | CoV-1 | 19 |
1Type of protease used in the assay as reported in the literature.