TABLE 1

Azole Kd and IC50 determinations versus A. fumigatus CYP51 (AfCYP51) enzymes

Test agentParameter value (μM)a
AfCYP51AAfCYP51B
KdIC50Kd1Kd2IC50
PC9450.500.2319,2980.320.22
Posaconazole0.960.160.012NA0.17
  • a Kd determinations used 4 μM purified AfCYP51A and 4 μM AfCYP51B. IC50 determinations used 0.5 μM AfCYP51A and 0.5 μM AfCYP51B, recovered from the membrane fraction of E. coli expression clones. NA, not applicable.