Table 10. Functional mGlu5 Activity and Binding Affinity in the Quinoline Series.
entry | A | R | mGlu5 IC50 (nM) | mGlu5Ki (nM) |
---|---|---|---|---|
167 | CH | H | 29 | 110 |
159 | CH | phenyl | 1250 | 97 |
160 | CH | 3-pyridyl | 1340 | 730 |
161 | CH | 4-fluorophenyl | 692 | 64 |
164 | N | H | 68 | 100 |
165 | N | Cl | 3310 | >10 000 |
166 | N | phenyl | 81 | 97 |