TABLE 1.
IC50 valuesa of 1, analogs, and controls for enzyme activity against cysteine and serine proteases
| Structure | Compound ID | MPro IC50, nM |
CatB IC50, nM |
CatL IC50, nM |
Thrombin IC50, nM |
|---|---|---|---|---|---|
|
1 | 230 ± 18 | 18,000 ± 9,100 | >32,000 | >32,000 |
|
18 | 11 ± 0.7 | 24 ± 7.5 | 1.8 | >10,000 |
|
GC-376 | 18 ± 1.5 | 37 ± 15 | 0.05 | >10,000 |
|
19 | 620 ± 48 | 13,000 ± 3,600 | >32,000 | > 32,000 |
|
20 | 580 ± 40 | 1,800 ± 260 | 23,058 | > 32,000 |
|
21 | 3,100 ± 770 | 27,000 ± 11,000 | >32,000 | >32,000 |
a
Enzyme assay. Values were calculated from at least 10-point dose-response curves performed in duplicate.