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. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Sep 10;23(21):10.1016/j.bmcl.2013.09.001. doi: 10.1016/j.bmcl.2013.09.001

Table 2.

Initial Amide SAR

graphic file with name nihms524282u2.jpg
cpd R mGlu5 pIC50 (± SEM)a mGlu5 IC50 (nM) % Glu Max (± SEM)a,b
17 graphic file with name nihms524282t12.jpg < 5.0c > 10,000 14.4 ± 6.7
18 graphic file with name nihms524282t13.jpg 6.11 ± 0.12 772 1.7 ± 0.2
19 graphic file with name nihms524282t14.jpg < 4.5 > 30,000 3
20 graphic file with name nihms524282t15.jpg < 4.5 > 30,000 3
21 graphic file with name nihms524282t16.jpg < 4.5 > 30,000 3
22 graphic file with name nihms524282t17.jpg < 4.5 > 30,000 3
a

Calcium mobilization mGlu5 assay; values are average of n ≥ 3

b

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

c

CRC does not plateau