Table 5.

Selectivity of compounds for CaCYP51 (Ca) over Δ60HsCYP51 (Hs) based on K _d and IC₅₀.

Cmpd	K d [nM]		Selectivity	IC50 [μM]		Selectivity
	Ca	Hs	Hs/Ca (fold)	Ca	Hs	Hs/Ca (fold)
5 d	17±5	45±13	2.6	0.39	3.37	8.6
5 f	62±17	74±13	1.2	0.46	3.73	8.1
12 c	43±18	923±509	21.5	0.33	152	461
fluconazole	41±13	38 460±4840	938	0.31	∼1327	4281
posaconazole	43±11	204±63	4.7	0.218	123[a]	615
voriconazole	10±221	2 290±12021	229	0.218	78[a]	390
itraconazole	19±521	92±721	4.8	0.421	7021	175
ketoconazole	12±321	42±1621	3.5	0.521	4.521	9

Mean K _d values of three replicates are shown along with associated standard deviations. For IC₅₀ determinations CYP51 assays contained 1 μM CaCYP51 (all azoles) or 0.25 μM Δ60HsCYP51 (5 d, 5 f, 12 c and fluconazole) or 0.4 μM Δ60HsCYP51 (posaconazole, voriconazole, itraconazole and ketoconazole). [a] See Figure S4.