Table 3. In Vitro Profiling for Compounds 25, 27, 28, and 29.
|
in
vitro profiling |
||||||||
|---|---|---|---|---|---|---|---|---|
| ID | mouse plasma t1/2 (h) | human plasma t1/2 (h) | mouse hepatocytes t1/2 (h) | human hepatocytes t1/2 (h) | hERG IC50 (μM) | CYP1A2 IC50 (μM) | CYP2D6 IC50 (μM) | CYP3A4 IC50 (μM) |
| 25 | >1 | >1 | 2.4 | >4 | >30 | >30 | >30 | >30 |
| 27 | >24 | >6 | 1.9 | >4 | >30 | >30 | >30 | >30 |
| 28 | >6 | >6 | 1.7 | >4 | >30 | >30 | >30 | >30 |
| 29 | 3.7 | ND | 1.7 | 2.6 | >30 | >30 | >30 | >30 |