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. 2010 Aug;78(2):319–324. doi: 10.1124/mol.110.064261

TABLE 1.

Comparison of kinetic parameters and inhibition potency data between CID 16725315 and CID 23631927

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