Table 1.
Enzymatic assay results of protease inhibitors investigated in this study against SARSCoV-2, EV-A71 and EV-D68 proteases.
| SARS-CoV-2 Mpro IC50 (μM) no DTT/with DTT | SARS-CoV-2 PLpro IC50 (μM) no DTT/with DTT | EV-A71 2Apro IC50 (μM) no DTT/with DTT | EV-A71 3Cpro IC50 (μM) no DTT/with DTT | EV-D68 2Apro IC50 (μM) no DTT/with DTT | EV-D68 3Cpro IC50 (μM) no DTT/with DTT | |
|---|---|---|---|---|---|---|
| GC376 | 0.03 ± 0.01/0.03 ± 0.01 | N.T. | N.T. | 0.06 ± 0.02/0.08 ± 0.02 | N.T. | 0.06 ± 0.01/0.05 ± 0.02 |
| Telaprevir | N.T. | N.T. | 1.8 ± 0.9/1.3 ± 0.6 | N.T. | 0.1 ± 0.0/0.2 ± 0.0 | N.T. |
| GRL0617 | N.T. | 1.8 ± 0.2/1.9 ± 0.2 | N.T. | N.T. | N.T. | N.T. |
| Ebselen | 3.7 ± 2.4/>60 0.67 ± 0.09a (reported) |
10.3 ± 8.9/>60 | 5.9 ± 1.1/>60 | 1.2 ± 0.7/>60 | 3.6 ± 1.0/>60 | 0.1 ± 0.0/>60 |
| Disulfiram | 2.1 ± 0.3/>60 9.35 ± 0.18 (reported) |
6.9 ± 4.2/>60 | 11.8 ± 2.1/>60 | 1.0 ± 0.6/>60 | 3.5 ± 0.5/>60 | 0.6 ± 0.1/>60 |
| Tideglusib | 2.1 ± 0.3/>60 1.55 ± 0.30 (reported) |
7.1 ± 1.4/30.4 ± 17.1 | 3.4 ± 2.9/>60 | 1.2 ± 0.1/>60 | 1.3 ± 0.7/>60 | 0.6 ± 0.3/>60 |
| Carmofur | 0.2 ± 0.1/28.2 ± 9.5 1.82 ± 0.06 (reported) |
0.7 ± 0.1/>60 | 12.9 ± 4.5/>60 | 0.4 ± 0.2/>60 | 6.4 ± 1.3/>60 | 0.3 ± 0.0/>60 |
| Shikonin | 1.5 ± 0.3/>60 15.75 ± 8.22 (reported) |
55.3 ± 17.7/28.2 ± 12.5 | 36.0 ± 20.5/>60 | 0.5 ± 0.2/>60 | 37.0 ± 14.2/>60 | 1.2 ± 0.7/>60 |
| PX-12 | 0.9 ± 0.2/>60 21.39 ± 7.06 (reported) |
18.7 ± 2.6/>60 | 16.9 ± 9.2/>60 | 4.1 ± 1.9/>60 | 9.3 ± 4.2>60 | 1.2 ± 0.2>60 |
a
The values shown in bold were reported in reference12