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. Author manuscript; available in PMC: 2012 Aug 17.
Published in final edited form as: ACS Chem Neurosci. 2011 Aug 17;2(8):411–432. doi: 10.1021/cn2000266

Table 10.

Functional mGlu5 activity and binding affinity in the quinoline series

graphic file with name nihms-291053-t0009.jpg

Entry A R mGlu5 IC50 (nM) mGlu5 Ki (nM)
167 CH H 29 110
151 CH phenyl 1250 97
152 CH 3-pyridyl 1340 730
153 CH 4-fluorophenyl 692 64
164 N H 68 100
165 N Cl 3310 > 10,000
166 N phenyl 81 97