Table 4.

Second generation aryl SAR

Compd	R	mGlu1 pIC50a (±SEM)	mGlu1 IC50 (nM)	% Glu maxa,b (±SEM)
15		6.79 ± 0.15	161	2.5 ± 0.5
48		6.59 ± 0.11	255	2.0 ± 0.4
49		6.38 ± 0.07	414	1.3 ± 0.9
50		6.15 ± 0.05	712	2.4 ± 0.7
46		6.58 ± 0.06	264	2.1 ± 0.3
51		6.46 ± 0.14	344	3.3 ± 1.0
52		5.86 ± 0.04	1400	−0.8 ± 3.3
53		6.40 ± 0.06	398	0.3 ± 2.2
54		7.01 ± 0.03	99	2.8 ± 0.3

^aCalcium mobilization mGlu₁ 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.