Table 8. ADME Profile, Including Aqueous Solubility, Plasma Protein Binding, and Metabolic Stability, of ortho-Methylated Quinoline Analogs.
| ID | aq sola (μM) | human PPBb (%) | HLMc Clintd (μL/min/mg protein) |
|---|---|---|---|
| 3(8,9) | 44 | 87 | 180 |
| 8a(10) | < 0.02 | 97 | 130 |
| 8b | 670 | 82 | 260 |
| 8c | 790 | 84 | 300 |
| 8d | 480 | 88 | 300 |
| 8e | 1000 | 70 | 13 |
| 9a(10) | 5.0 | 97 | 120 |
| 9b | 860 | 82 | 120 |
| 9c | 580 | 88 | 160 |
| 9d | 450 | 94 | 300 |
| 9e | 465 | 76 | 41 |
a
aq sol = aqueous solubility.
b
PPB = plasma protein binding.
c
HLM = human liver microsomes.
d
Clint = intrinsic clearance.