Table 2

Kinetic analysis of UGTs using UK series of compounds

CompoundUGT IsoformVmaxKm μM (apparent)Vmax/KmGoodness of Fit (r2)
nmol/min/mg ml/min/mg
UK-157,147UGT1A10.14  ± 0.1105  ± 331.340.96
UK-156,037UGT1A10.68  ± 0.05256  ± 542.640.99
UK 157,261UGT1A90.41  ± 0.0245  ± 119.110.98

The errors listed are the standard error as calculated from a nonlinear regression fit of a single kinetic determination for one cell line with one substrate. The goodness of fit parameter is the correlation coefficient of the fit of the experimental data to the Michaelis-Menten equation. Km values for UK-157,147 and UK-156,037 are listed as apparent Km because bothKm and Vmax calculations are based on the sum of products formed. The data could not be processed for each product because it was not detectable at all substrate concentrations.