Skip to main content
. 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 9.

Functional mGlu5 activity and binding affinity in the aryl amide series

graphic file with name nihms-291053-t0008.jpg

Entry R1 R2 R3 mGlu5 IC50 (nM) mGlu5 Ki (nM)
136 Cl H H 1870 1730
137 CN H H 490 330
138 CN H F 22 66
141 3-pyridyl H F not tested 702
142 CN Ph H 14 9.8
143 H Ph H not tested 7000
144 CN 3-fluorophenyl H 25 22
145 CN 4-fluorophenyl H 4.6 134
146 CN 1-naphthyl H 640 72
147 CN 3-pyridyl H >1000 2040