Antiviral activity and cytotoxicity assay of novel non-covalent SARS-CoV-2 Mpro inhibitors by propagation in Vero E6 cells.
Comp. ID | Cytotoxicity IC50 (µM ± SEa) | Antiviral assay (qPCR) | SIb | |||
---|---|---|---|---|---|---|
Inhibition % | EC50 and EC90 (µM ± SEa) | |||||
1 µM | 10 µM | EC50 | EC90 | |||
17 | >200 | 22.25 | 42.51 | 22.1 ± 1.012 | 36.13 ± 2.31 | 9 |
21 | 48.8 ± 3.72 | 83.49 | 95.92 | 0.0138 ± 0.00198 | 3.60 ± 0.42 | 3544 |
22 | 193.0 ± 14.7 | 88.16 | 94.10 | 0.1093 ± 0.01105 | 1.738 ± 0.54 | 1766 |
23 | 47.6 ± 3.62 | 78.96 | 92.92 | 0.0216 ± 0.00656 | 3.11 ± 1.61 | 2201 |
24 | 21.6 ± 1.64 | 94.01 | 96.22 | 0.0762 ± 0.00973 | 3.437 ± 0.55 | 283.3 |
25 | 121.0 ± 9.21 | 92.48 | 97.08 | 0.1066 ± 0.00115 | 2.50 ± 0.841 | 1135 |
26 | 87.3 ± 6.65 | 87.61 | 94.05 | 0.0376 ± 0.00423 | 3.801 ± 0.041 | 2323 |
27 | 64.4 ± 4.91 | 94.36 | 96.52 | 0.1035 ± 0.00344 | 2.601 ± 1.02 | 622.2 |
28 | 139.0 ± 10.6 | 92.71 | 95.60 | 0.108 ± 0.00304 | 1.41 ± 0.91 | 1278 |
29 | 151.0 ± 11.5 | 94.10 | 96.39 | 0.0519 ± 0.00512 | 8.953 ± 2.01 | 2909 |
Remdesivir | 43.1 ± 3.28 | 94.23 | 97.58 | 0.0099 ± 0.00175 | 0.0835 ± 1.88 | 7195 |
SE represents standard error from triplicate readings.
Selectivity index (SI) was calculated by dividing of IC50 value for Vero cell cytotoxicity by the EC50 of the antiviral assay.