Table 1.
Compounds Ability to Inhibit (Ki) Testosterone Metabolism by CYP3A4. The number of paraphrases is the error in the last digit from at least three measurements.
| Series | Cmpd | Structure | Ki +/− SD (μM) | Series | Cmpd | Structure | Ki +/− SD (μM) |
|---|---|---|---|---|---|---|---|
| 1 | 1 |  |
3.9 (7) | 6 | 16 |  |
0.31 (5) |
| 1 | 2 |  |
>100 | 6 | 17 |  |
N.D.1 |
| 1 | 3 |  |
N.D.1 | 6 | 18 |  |
>100 |
| 2 | 4 |  |
45 (7) | 7 | 19 |  |
0.067 (1) |
| 2 | 5 |  |
N.D.1 | 7 | 20 |  |
7 (2) |
| 2 | 6 |  |
N.D.1 | 8 | 21 |  |
1.0 (2) |
| 3 | 7 |  |
0.076 (3) | 8 | 22 |  |
16 (5) |
| 3 | 8 |  |
0.41 (6) | 9 | 23 |  |
0.24 (4) |
| 3 | 9 |  |
95 (21) | 9 | 24 |  |
2.3 (7) |
| 4 | 10 |  |
0.16 (4) | 9 | 25 |  |
1.5 (3) |
| 4 | 11 |  |
0.52 (4) | 26 |  |
N.D.1 | |
| 4 | 12 |  |
1.2 (4) | ||||
| 5 | 13 |  |
0.7 (2) | ||||
| 5 | 14 |  |
0.98 (9) | ||||
| 5 | 15 |  |
14 (3) |
1
ND, not determined do to solubility or very low affinity.