Table 4. Substituted Heteroaryl Amide SAR.

Cpd	A	R	mGlu5 pIC50a (± SEM)	mGlu5 IC50 (nM)	% Glu Maxa,b (± SEM)
65	N		<4.5	>30,000	—
66	N		<4.5	>30,000	—
67	N		6.72 ± 0.22	193	2.1 ± 0.8
68	N		7.20 ± 0.06	62.4	1.6 ± 0.1
69	N		7.00 ± 0.29	100	2.3 ± 0.6
70	CF		6.00 ± 0.04	990	1.1 ± 0.75
71	CF		<5.0c	>10,000	20 ± 10
72	CF		5.33 ± 0.17	4640	19 ± 6
73	CF		<4.5	>30,000	—
74	CF		<4.5	>30,000	—
75	CF		6.51 ± 0.15	311	1.7 ± 0.4
76	CF		6.95 ± 0.29	111	2.0 ± 0.3

^aCalcium mobilization mGlu5 assay; values are average of n ≥ 3

^bAmplitude of response in the presence of 30 μM test compound as a percentage of maximal response (100 μM glutamate); average of n ≥ 3

^cCRC does not plateau