Table 12.
| |||||||
---|---|---|---|---|---|---|---|
Compd | R | fpKia | Solubility (μg/mL) | Compd | R | fpKi | Solubility (μg/mL) |
121(hit) | 5.6 | 113 | 127 | 7.1 | 3 | ||
122 | 7.3 | 22 | 128 | 8.0 | 0 | ||
123 | 6.8 | 4 | 129 | 8.3 | 0 | ||
124 | 7.7 | 4 | 130 | 8.2 | 7 | ||
125 | 6.5 | nt | 131 | 6.5 | 70 | ||
126 | 5.2 | nt | (±)132 | 7.9 | 8 |
Functional activity against human Y2 receptors using [35S]GTPγS binding assay.