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Functional mGlu5 activity and binding affinity in the pyrazolopyrimidine series
| Entry | Series | X | R | Chirality | CHO-K1 mGlu5 IC50 (nM) | Astrocytes mGlu5 IC50 (nM) | mGlu5 Ki (nM) |
|---|---|---|---|---|---|---|---|
| 119 | I | Cl | — | — | 166 | 82 | 247 |
| 120 | I | Br | — | — | 189 | 64 | 281 |
| 121 | II | Cl | Me | (+/−) | 327 | 87 | 275 |
| 122 | II | Br | Me | (+/−) | 223 | 50 | 219 |
| (R)-122 | II | Br | Me | R | 118 | 34 | 74 |
| 123 | II | Cl | Cl | (+/−) | 91 | 22 | 42 |
| 124 | II | Br | Cl | (+/−) | 84 | 23 | 45 |
| (R)-124 | II | Br | Cl | R | 25 | 7.8 | Not Reported |
| 125 | II | Cl | Br | (+/−) | 34 | 17 | 73 |
| 126 | II | Br | Br | (+/−) | 75 | 15 | 55 |
