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

Table 10. Functional mGlu5 Activity and Binding Affinity in the Quinoline Series.

graphic file with name cn-2011-000266_0029.jpg

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