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. 2022 Sep 22;12(41):26895–26907. doi: 10.1039/d2ra04015h

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
a

SE represents standard error from triplicate readings.

b

Selectivity index (SI) was calculated by dividing of IC50 value for Vero cell cytotoxicity by the EC50 of the antiviral assay.