Table 7.
Cmpd | Measured IC50 (μM) | Literature IC50 (μM) | MW | cLogP | LE | Relative LE cf. 7b | %F (rat) |
---|---|---|---|---|---|---|---|
1 | 0.003 | 0.0006 | 551 | 3.5 | 0.30a/0.32b | 0.9 | 2.4 |
7b | 0.147 | 0.020 | 385 | 2.8 | 0.33a/0.37b | 1 | ndc |
7c | - | 0.007 | 483 | 4.3 | 0.32 | 0.86 | 0.4 |
7d | - | 0.001 | 496 | 3.3 | 0.34 | 0.91 | 8 |
rac-7e | - | 0.141 | 521 | 5.0 | 0.25 | 0.68 | 12 |
(S)-7e | - | 0.048 | 521 | 5.0 | 0.27 | 0.73 | 74 |
27 | 0.059 | - | 341 | 3.8 | 0.39 | 1.18 | 20 |
32 | 0.069 | - | 396 | 3.6 | 0.35 | 1.06 | 58 |
33 | 0.045 | - | 412 | 2.2 | 0.33 | 1.05 | 39 |
Based on measured IC50.
Based on literature IC50.
Not determined.