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.

Drug	Kd	Ki
	μM
∆(2–50)CYP46A1 Wild Type
CLO	∼0.004	0.017 ± 0.003
POS	0.03 ± 0.01	0.064 ± 0.005
VOR	0.22 ± 0.02	0.226 ± 0.006
T306A Mutant
CLO	∼0.005	ND
POS	0.51 ± 0.03	ND
VOR	0.27 ± 0.02	ND
A474V Mutant
CLO	0.09 ± 0.01	ND
POS	0.04 ± 0.01	ND
VOR	5.4 ± 0.4	ND

ND, not determined.