TABLE 1.
Thiocarbazate CID 16725315 | Oxocarbazate CID 23631927 | |
---|---|---|
k1 | 3.09 × 106 M−1·s−1 | 2.27 × 106 M−1·s−1 |
k−1 | 0.32 s−1 | 0.29 s−1 |
kcat | 4.31 s−1 | 3.78 s−1 |
kon | 3.27 × 104 M−1·s−1 | 1.53 × 105 M−1·s−1 |
koff | 3.75 × 10−5 s−1 | 4.40 × 10−5 s−1 |
Ki = koff/kon | 1.15 nM | 0.29 nM |
Human Cat L. IC50 | ||
0 h | 56 ± 4 nM | 6.9 ± 1.0 nM |
4 h | 1.0 ± 0.5 nM | 0.4 ± 0.1 nM |
SARS IC50 | 273 ± 49 nM | |
Ebola IC50 | 193 ± 39 nM | |
Inhibition of intracellular Cat L. | 2% | 38% |
Cat L/B Selectivity | 40–50 | 735 |