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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 3.

Phenyl Ring SAR

graphic file with name nihms524282u3.jpg
cpd Series R mGlu5 pIC50 (± SEM)a mGlu5 IC50 (nM) % Glu Max (± SEM)a,b
23 I H 6.69 ± 0.25 205 1.7 ± 0.3
24 I F 7.62 ± 0.03 24 1.2 ± 0.1
25 I Cl 7.94 ± 0.19 11 1.4 ± 0.2
26 I CF3 6.55 ± 0.10 283 1.7 ± 0.2
27 II F 6.52 ± 0.07 305 1.3 ± 0.3
28 II Cl 7.49 ± 0.02 33 1.2 ± 0.2
29 II CH3 7.72 ± 0.06 19 0.8 ± 0.2
30 II CF3 5.26 ± 0.01 5530 3.2 ± 0.3
31 II CN 6.50 ± 0.08 318 1.1 ± 0.4
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