Table 2.
Name | Structure | IC50 (μM)a | Kis (μM)b |
---|---|---|---|
6TG | 13.7 ± 1.7 | 21.1 ± 1.1 | |
6MP | 58.1 ± 5.7 | – | |
Hypoxanthine | NDc | – | |
2-amino-6-methyl-mercaptopurine | NDc | – | |
Mycophenolic acid | >200 | – | |
Disulfiram | >100 | – | |
GRL0617 | >100 | – |
The DUB activity assay was used for the measurement of IC50 (Eq. (1)).
Proteolytic activity at various concentrations of SARS-CoV-derived peptidyl substrate and 6TG was measured (Fig. S6 and Fig. 3) and the apparent Kis was determined from the best global fit of the data to a noncompetitive inhibition model (Eq. (2)). Rsqr was 0.964.
ND: IC50 was not determined due to lack of inhibition at a compound concentration of 200 μM.