|
Compound(s)
|
IC50(μM)1,a
|
Ki(μM)1,a
|
IC50(μM)2,b
|
Ki(μM)2,b
|
IC50(μM)3,b
|
|---|
|
Ketoconazole (KC)
|
0.6 (0.0)c
|
0.04 – low [S]
|
0.3 (0.1)c
|
0.2
|
0.4c
|
| | |
0.2 – high [S]
| | | |
|
Nonylphenol (NP)
|
5.2 (1.1)
|
3.5
|
160 (40)
|
Not analysed
|
35
|
|
Ethynylestradiol
|
20 (1.2)
|
5.4 – low [S]
|
40 (7.1)
|
54 – low [S]
|
50
|
| | |
10.3 – high [S]
| |
95 – high [S]
| |
|
KC:NP (1:5)
|
1.3 (0.2):6.2 (1.0)
|
Not analysed
|
5.3 (1.1):25.0 (5.3)
|
Not analysed
|
Not analysed
|
- 1 Hepatic Microsomal CYP1A activity; 2 Hepatic Microsomal CYP3A activity; 3 cDNA Expressed Human CYP3A4; a Substrate [S] = 7-Ethoxyresorufin; b [S] = 7-Benzyloxy-4-[trifluoromethyl]-coumarin; c Published in [22]. Each IC50 value represents the mean from 2–4 separate assays, followed by the SD, in brackets. The Ki values are estimated from one representative Dixon plot.
