Table 1. Core SAR.

Cpd	Core	mGlu5 pIC50a (± SEM)	mGlu5 IC50 (nM)	% Glu Maxa,b(± SEM)
1		6.55 ± 0.19	284	1.3 ± 0.2
10		6.00 ± 0.21	994	1.8 ± 0.7
11		5.43 ± 0.26	3700	−4.9 ± 4.7
12		6.44 ± 0.19	359	2.0 ± 0.7
13		5.53 ± 0.23	2930	1.1 ± 0.5
20		6.39 ± 0.07	403	1.1 ± 0.4
21		6.89 ± 0.04	129	1.0 ± 0.3
22		<5.0c	>10,000	44 ± 8

^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

^cConcentration response curve (CRC) does not plateau