Table 1.
Compound | hV1a Ki (nM) | hV1b Ki (nM) | hV2 Ki (nM) | cLogP | Pe (10−6 cm s−1) | Predicted CNS penetration |
---|---|---|---|---|---|---|
11a | 1.1 | >1000 | >1000 | 5.62 | 2.2 | CNS± |
11b | 0.61 | 1154 | >10,000 | 4.42 | 5.3 | CNS+ |
11c | 0.63 | 1300 | >10,000 | 4.75 | 4.5 | CNS+ |
Compound | hV1a Ki (nM) | hV1b Ki (nM) | hV2 Ki (nM) | cLogP | Pe (10−6 cm s−1) | Predicted CNS penetration |
---|---|---|---|---|---|---|
11a | 1.1 | >1000 | >1000 | 5.62 | 2.2 | CNS± |
11b | 0.61 | 1154 | >10,000 | 4.42 | 5.3 | CNS+ |
11c | 0.63 | 1300 | >10,000 | 4.75 | 4.5 | CNS+ |