Table 1. Purified Mpro dose response and kinetic data.
FC = IC50 fold-change vs the parental protease. Nir = nirmatrelvir; Ens = ensitrelvir. Higher VMAX values for O/A206T and O/A206T/T198I are due to a higher enzyme concentration.
| Mpro | FC Nir |
FC Ens |
VMAX [μM*min-1] |
KM [μM] |
kcat [min-1] |
kcat/KM [μM-1*min-1] |
Mpro conc. [μM] |
|---|---|---|---|---|---|---|---|
| wild type (WT) | 1 | 1 | 74.4 | 329.8 | 37.2 | 0.1128 | 2 |
| L57F | 1.6 | 4.0 | 76.5 | 528.1 | 38.2 | 0.0724 | 2 |
| L167F/P168S | 8.3 | 8.6 | 32.8 | 410.1 | 16.4 | 0.0400 | 2 |
| L167F/P168S/L57F | 20.4 | 57.7 | 24 | 648.7 | 12 | 0.0185 | 2 |
| Omicron | 1 | 1 | 426.6 | 356.8 | 213.3 | 0.5978 | 2 |
| O/A206T | 2 | 1.2 | 2526 | 2467 | 252.6 | 0.1024 | 10 |
| O/A206T/T198I | 2.3 | 1.8 | 1966 | 1885 | 196.6 | 0.1043 | 10 |