. 2011 Apr 15;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 cn-2011-000266_0026.jpg

entry	R¹	R²	R³	mGlu₅ IC₅₀ (nM)	mGlu₅K_i (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

Table 9. Functional mGlu5 Activity and Binding Affinity in the Aryl Amide Series.