Table 1

Inhibition of CYP3A4 in HLM and Supersomes

CompoundIC50Microsomes/Supersomes IC50 Ratio
MicrosomesSupersomes
μM
Ketoconazole0.070.051.4
1>30.00>30.00Match
23.753.501.1
35.434.001.4
42.291.251.8
56.781.255.4
6>30.006.90>4.3
71.751.751.0
83.400.447.7
97.003.002.3
104.910.2420.5
11>30.00>30.00Match
12>30.00>30.00Match
130.302.000.15
140.800.451.8
158.588.001.1
162.251.721.3
17>30.00>30.00Match
181.860.0726.6
19>30.002.15>14
20>30.00>30.00Match
21>30.00>30.00Match
22>30.002.40>12.5
231.870.1117
248.900.3426.2
253.760.0941.8
269.980.1952.5
2710.004.502.2
28>30.001.25>24
29>30.006.90>4.3
306.000.2030
314.250.2021.3
3215.301.3011.8
33>30.001.10>27
3421.005.304
3519.001.8010.5
3630.001.2524
3730.005.505.5
38>30.00>30.00Match
3910.600.5021.2
40>30.00>30.00Match
41>30.00>30.00Match
42>30.000.55>54.5
43>30.00>30.00Match
441.340.0267
45>30.000.9038.9
46>30.00>30.00Match
47>30.0019.00>1.6
48>30.001.20>25
496.600.2922.7
50>30.004.80>6.3
511.600.275.9
52>30.009.70>3.1
Number of matches25
Percentage of matches48