TABLE 4

Kinetic parameters of M28 and M31 formation

Incubation time = 60 min. Protein concentration for incubation with SCH 534128 = 0.8 mg/ml. Protein concentration for incubation with SCH 534129 = 0.4 mg/ml.

Kinetic Parameters of M28 and M31 Formation from Boceprevir with Human Liver Cytosol (1.6 mg protein/ml)aKinetic Parameters of M28 and M31 Formation from SCH 534128 and SCH 534129 with Human Liver Cytosolb
ParametersM28M31ParametersM28 from SCH 534128M31 from SCH 534129
Km (μM)13.0 ± 4.712.5 ± 3.2Km (μM)35.5 ± 9.527.4 ± 4.6
Vmax (pmol/mg per min)28.6 ± 5.234.9 ± 4.5Vmax (nmol/mg per min)0.361 ± 0.040.846 ± 0.06
Vmax/Km (μl/mg per min)2.22.8Vmax/Km (μl/mg per min)10.230.9
  • a Samples were analyzed by LC-MS/MS.

  • b Samples were analyzed by HPLC-FSA.