Table 4. Mouse PO PK 5 mg/kg and Kinetic Solubility Data of 1 and the Six Shortlisted Compounds.
| compound | t1/2 (h) | tmax (h) | Cmax (ng/mL) | AUC 0 → t (ng/mL·h) | AUC 0 → ∞ (ng/mL·h) | MRT 0 → ∞ (h) | Vd (L/kg) | CL (L/h/kg) | solubility (μM) |
|---|---|---|---|---|---|---|---|---|---|
| 1 (OM-1700)39 | 0.67 | 0.25 | 3203 | 2384 | 2388 | 0.69 | 2.03 | 2.09 | >80 |
| 18b | 1.00 | 0.25 | 285 | 319 | 322 | 1.56 | 22.4 | 15.6 | >80 |
| 22a | 1.17 | 0.25 | 779 | 543 | 547 | 1.39 | 15.5 | 9.14 | 50 |
| 24 (OM-153) | 1.50 | 0.5 | 1967 | 4945 | 5038 | 2.39 | 2.15 | 0.99 | 31 |
| 30b | 0.69 | 0.5 | 6512 | 15 083 | 15 105 | 1.93 | 0.33 | 0.33 | >80 |
| 31a | 0.76 | 0.25 | 2770 | 3401 | 3404 | 1.24 | 1.61 | 1.47 | >80 |
| 31b | 0.59 | 0.25 | 5796 | 5313 | 5316 | 1.47 | 0.80 | 0.94 | 13 |