Table 2.
Kinetic parameters of a series of pyridinyl analogue inhibitors of HAV 3Cpro and SARS 3CLpro and half-life of pyridinyl analogues in buffer
| Compound | Structure | IC50 (nM) | Km (nM) | kcat (s−1) × 10−5 | kcat/Km (M−1s−1) × 103 | Half-life (s−1) × 10−3 |
|---|---|---|---|---|---|---|
| HAV 3Cpro | ||||||
| 20 |  |
338 ± 2 | 240 ± 30 | 110 ± 6 | 4.6 ± 0.6 | 1.2 ± 0.2 |
| 37 |  |
140 ± 20 | 180 ± 30 | 25 ± 8 | 1.4 ± 0.5 | 4.9 ± 0.6 |
| 24 |  |
53 ± 2 | 120 ± 20 | 119 ± 8 | 10 ± 2 | 1.1 ± 0.3 |
| 45 |  |
470 ± 60 | ND | ND | ND | ND |
| 36 |  |
1200 ± 130 | ND | ND | ND | ND |
| 44 |  |
250 ± 50 | ND | ND | ND | ND |
| SARS 3CLpro | ||||||
| 24 | ND | 26 ± 7 | 17 ± 6 | 7 ± 3 | ||
ND, not determined.