Table 5.
ADMET profile for active compounds 4a, 4e, 8a, and SOR.
| Comp. | HIA | CaCo2 | MDCK | BBB | CYP3A4 inhibition | PgP inhibition | Carcinogenicity |
|---|---|---|---|---|---|---|---|
| 4a | 91.96 | 0.67 | 0.13 | 0.11 | Non | Inhibitor | Negative |
| 4e | 86.05 | 3.06 | 0.08 | 0.07 | Non | Inhibitor | Negative |
| 8a | 83.30 | 0.44 | 0.13 | 0.07 | Non | Inhibitor | Negative |
| SOR | 93.50 | 22.55 | 0.08 | 1.00 | inhibitor | Inhibitor | Negative |
Notes: HIA: human intestinal absorption (%), CaCo2: permeability through cells derived from human colon adenocarcinoma (nm/s), MDCK: permeability through Maden Darby canine kidney cells (nm/s); tool for rapid permeability, BBB: blood brain barrier penetration, CYP3A4: cytochrome P450 3A4, PgP: P-glycoprotein.