TABLE 2

TDI kinetic parameters for dataset 1 (TAO inhibition of CYP3A4)

Data are presented as parameter estimate ± S.E. kprod is the rate constant for metabolite formation, and krev is the rate constant for the reversible component of inactivation.

Numerical Method, MM–Quasi-Irreversible ModelReplot Method (All Data)Replot Method (Linear Region)
KI (μM)0.93 ± 0.1050.31 ± 0.0351.51 ± 0.006
kinact (min−1)0.25 ± 0.0090.062 ± 0.00150.231 ± 0.001
kinact/KI (μM−1 min−1)0.27 ± 0.030.20 ± 0.02
kprod (min−1)67.23 ± 0.94
krev (min−1)0.031 ± 0.0023