TABLE 4

Comparison of estimates of KI,u and kinact by post hoc and concurrent methods

fumicaCompoundPost Hoc (KI . fumic)ConcurrentKI,u1 Fold Differencekinact Fold Difference
KI,ukinactAICcKI,ukinactAICc
µMminµMmin
0.24PAR1.11 ± 0.210.006 ± 0.002−7270.61 ± 0.090.005 ± 0.001−7620.560.83
0.009ITZ model 1bKI,u1 = 0.0008 ± 0.0001KI,u2 = 0.03 ± 0.0090.005 ± 0.003−951KI,u1 = 0.024 ± 0.006KI,u2 = 0.037 ± 0.0160.0042 ± 0.004−97231.440.84
0.009ITZ model 2bDNCDNCNAKI,u1 = 0.015 ± 0.0005KI,u2 = 0.062 (fixed)NAc−973NANA
  • DNC, did not converge; NA, not applicable.

  • a fumic at 1 mg/ml.

  • b KI,u1 used for calculation of kinact/KI,u.

  • c The metabolite did not reach saturation (“V/K” range).