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. 2011 Apr 15;2(8):411–432. doi: 10.1021/cn2000266

Table 14. mGlu5 Potency in Tetrahydroazolopyridines and Tetrahydroazoloazepines.

graphic file with name cn-2011-000266_0036.jpg

entry n X Y Z R mGlu5 IC50 (nM)
201 1 O C N H 60
202 1 N C O H 290
203 1 O C N F 28
204 1 N C O F 54
205 1 N C NH F 34% at 10 μM
206 1 N C S F 52% at 10 μM
207 1 C N N F 153
208 1 N N N F 346
209 2 O C N H 65
210 2 O C N F 16