Table 4. ADME Properties for Compounds 1, 2, 3, 6, 9, 10, and 11.
| microsomal
stability |
||||||
|---|---|---|---|---|---|---|
| compound | kinetic solubility (μM) | PAMPA (% flux) | phase 1 (Clint, μL/min/mg) | glucuronidation in vitro (% remaining) | plasma stability (% remaining) | plasma protein binding (% bound) |
| 1 | 423 | 29.7 | 0.4 | 37.7 | 95.5 | 99.7 |
| 2 | 460 | 36.1 | 31.2 | 73.0 | 79.1 | 99.9 |
| 3 | 436 | 40.9 | 57.8 | 30.7 | 74.2 | 99.7 |
| 6 | 392 | 40.3 | 69.0 | 58.3 | 59.5 | 99.9 |
| 9 | 445 | 37.3 | 77.0 | 54.6 | 97.1 | 99.8 |
| 10 | 421 | 50.5 | 68.0 | 68.9 | 89.5 | 99.3 |
| 11 | 476 | 23.0 | 8.8 | 39.1 | 100 | 98.8 |