Table 2.
Anti‐SARS‐CoV‐2 RdRp/ExoN activities (along with the respective ratios) of the six target drugs in HEK293T cells. Remdesivir and molnupiravir were used as the positive control/reference drugs, and DMSO as the negative control/placebo drug.
|
Classification |
Compound |
EC50 [μM][a] |
EC50 Ratio |
|||
|---|---|---|---|---|---|---|
|
|
|
Nsp12 |
Nsp12+ Nsp14 |
Nsp12+ Nsp14mutant |
(Nsp12+ Nsp14)/Nsp12 |
(Nsp12+ Nsp14mutant)/Nsp12 |
|
Repurposed NAs |
Riboprine |
0.22±0.03 |
0.33±0.04 |
0.27±0.03 |
1.50 |
1.23 |
|
Forodesine |
0.25±0.03 |
0.35±0.04 |
0.30±0.04 |
1.40 |
1.20 |
|
|
Nelarabine |
0.69±0.05 |
1.25 ± 0.07 |
1.15 ± 0.06 |
1.81 |
1.67 |
|
|
Tecadenoson |
1.05±0.06 |
1.42 ± 0.08 |
1.34 ± 0.08 |
1.35 |
1.28 |
|
|
Maribavir |
1.11±0.06 |
1.95 ± 0.09 |
1.56 ± 0.07 |
1.76 |
1.41 |
|
|
Vidarabine |
1.15±0.07 |
2.10 ± 0.09 |
1.59 ± 0.08 |
1.83 |
1.38 |
|
|
Reference Drugs |
Remdesivir |
1.20 ± 0.08 |
2.19 ± 0.10 |
1.64 ± 0.08 |
1.83 |
1.37 |
|
Molnupiravir |
0.29±0.04 |
0.50±0.05 |
0.39±0.05 |
1.72 |
1.35 |
|
|
Placebo Solvent |
DMSO |
>100 |
>100 |
>100 |
N.A.[b] |
N.A. |
[a] Test compound concentration required for 50 % decrease in SARS‐CoV‐2 RdRp activity in vitro; Nsp12 refers to nsp12/7/8 complex, Nsp14 refers to nsp14/10 complex, and Nsp14mutant refers to nsp14mutant/10 complex. [b] N.A.: not available (i. e., not determined).