Table 2. Benzamide SAR.

Cpd	A	R	mGlu5pIC50a (± SEM)	mGlu5 IC50 (nM)	% Glu Maxa,b (± SEM)
29	N	3-Cl	6.94 ± 0.10	116	1.2 ± 0.0
30	N	H	<5.0c	>10,000	12 ± 11
31	N	3-F	5.29 ± 0.17	5140	1.5 ± 2.7
32	N	3-Me	6.67 ± 0.16	212	1.5 ± 0.5
33	N	3-CN	6.15 ± 0.17	709	1.5 ± 0.2
34	N	3-OMe	5.39 ± 0.15	4110	−4.3 ± 2.7
35	CF	3-Cl	6.93 ± 0.10	118	2.0 ± 0.3
36	CF	H	5.06 ± 0.09	8650	−9.4 ± 2.3
37	CF	3-F	5.42 ± 0.09	3820	−0.4 ± 1.7
38	CF	3-Me	6.70 ± 0.18	199	2.1 ± 0.4
39	CF	3-CN	6.18 ± 0.16	662	1.2 ± 0.3
40	CF	3-OMe	5.36 ± 0.17	4400	−5.6 ± 5.1
41	CF	3-NMe2	<5.0c	>10,000	52 ± 11
42	CF	2-F, 3-Cl	<4.5	>30,000	—
43	CF	3-Cl, 4-F	5.34 ± 0.15	4590	−2.8 ± 6.2
44	CF	3-Cl, 5-F	<5.0c	>10,000	48 ± 10
45	CF	2-F, 5-Cl	6.05 ± 0.13	894	1.0 ± 0.8
46	CF	3,5-di-F	<4.5	>30,000	—
47	CF	3,5-di-Cl	<4.5	>30,000	—
48	CF	3,5-di-Me	5.18 ± 0.18	6600	6.6 ± 2.0
49	CF	3,5-di-OMe	<4.5	>30,000	—
50	CF	3-CN, 5-F	<4.5	>30,000	—

^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