Table 1.
Determined enzymatic IC50, cellular EC50, and antiviral EC50 values of MPro inhibitors.
| Compound ID | Enzymatic IC50 (nM) | Cellular EC50 (μM) | Antiviral EC50 (μM) | PDB Entry | Compound ID | Enzymatic IC50 (nM) | Cellular EC50 (μM) | Antiviral EC50 (μM) | CC50 (μM) | PDB Entry |
|---|---|---|---|---|---|---|---|---|---|---|
| Boceprevir | 4200 ± 600 [16]/8000 ± 1500 [15] | >10 | MPI39 | 26 ± 1 | >10 | |||||
| MPI29 | 9.3 ± 0.8 | >5 | 7S6W | MPI40 | 180 ± 20 | 7.4 ± 0.9 | n.d.a/n.d.b/n.d.c | |||
| MPI30 | 40 ± 4 | >10 | 7S6X | MPI41 | 150 ± 20 | 7.7 ± 1.5 | ||||
| MPI31 | 360 ± 50 | >10 | MPI42 | 22 ± 4 | 2.6 ± 0.5 | 7S75 | ||||
| MPI32 | 620 ± 170 | >10 | 7S6Y | MPI43 | 45 ± 5 | 0.37 ± 0.04 | 0.61a/0.36b/1.00c | 34.2 | ||
| MPI33 | 75 ± 9 | >10 | 7S6Z | MPI44 | 59 ± 7 | 0.31 ± 0.03 | 2.94a/0.86b/1.04c | 143.7 | ||
| MPI34 | 370 ± 30 | >10 | 7S70 | MPI45 | 97 ± 11 | 0.74 ± 0.11 | ||||
| MPI35 | 720 ± 80 | >5 | 7S71 | MPI46 | 120 ± 10 | 0.14 ± 0.02 | 1.08a/2.28b/0.75c | 163.4 | ||
| MPI36 | 102 ± 2 | >10 | 7S72 | MPI47 | 720 ± 90 | >10 | ||||
| MPI37 | 23 ± 1 | >10 | 7S73 | PF-07321332 | 66 ± 12 | 3.4 ± 0.8 | 1.30 | |||
| MPI38 | 17 ± 2 | >5 | 7S74 |
n.d.: no detectable value.
a
Antiviral EC50 value for the USA-WA1/2020 strain.
b
Antiviral EC50 value for the Beta strain.
c
Antiviral EC50 value for the Delta strain.