Table 6. In Vitro ADME Parameters for Selected PDE11A4 Inhibitors.
cpd | pH 7.4 PBS solub (μM) | mouse liver microsomal t1/2 (min | human liver microsomal t1/2 (min | IC50 (μM) Hu CYP3A4 | IC50 (μM) Hu CYP2D6 | IC50 (μM) Hu CYP2C9 |
---|---|---|---|---|---|---|
14b | 135 | 2.3 | 3.2 | 10 | 1.4 | 4.4 |
14c | 120 | 1.9 | 4.2 | >10 | >10 | 1.5 |
23b | 42 | 3.6 | 4.3 | 5.8 | >10 | 5.6 |
25 | 39 | 5.2 | 8 | 7.7 | >10 | >10 |