Table 3. ADME Values for Selected Compoundsa.
microsomal stability | plasma stability | PAMPA | |
---|---|---|---|
compd | % remaining (1 h) | % remaining (3 h) | log Papp |
4hh | 7.9 ± 6.3 | ≥100 | –7.33 |
4t | 0.1 ± 0.1 | ≥100 | N/A |
4y | 1.8 ± 2.1 | 97.9 ± 5.7 | –7.12 |
4ee | 1.8 ± 0.4 | 98.8 ± 3.7 | –7.54 |
4ff | 4.7 ± 1.7 | ≥100 | –7.46 |
4jj | 12.9 ± 1.6 | ≥100 | –10.20 |
Compounds with highest relative potency were analyzed for stability in mouse microsomes and plasma, as well as for BBB permeability.