TABLE 1

Binding and inhibition of ∆(2–50)CYP46A1 wild type and mutants by the antifungal azoles that were cocrystallized with the P450

The results represent the average of triplicate measurements ± S.D.

DrugKdKi
μM
∆(2–50)CYP46A1 Wild Type
 CLO∼0.0040.017 ± 0.003
 POS0.03 ± 0.010.064 ± 0.005
 VOR0.22 ± 0.020.226 ± 0.006
T306A Mutant
 CLO∼0.005ND
 POS0.51 ± 0.03ND
 VOR0.27 ± 0.02ND
A474V Mutant
 CLO0.09 ± 0.01ND
 POS0.04 ± 0.01ND
 VOR5.4 ± 0.4ND
  • ND, not determined.