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. 2017 May 22;60(12):5072–5085. doi: 10.1021/acs.jmedchem.7b00410

Table 1. Initial Picolinamide Core Analogs of 9.

graphic file with name jm-2017-00410d_0008.jpg

no. mGlu5 pIC50 (±SEM)a mGlu5 IC50 (nM)a % Glu maxa,b
9 7.62 ± 0.03 24 1.2 ± 0.1
10 6.70 ± 0.15 200 1.2 ± 0.1
11 7.01 ± 0.09 98 1.3 ± 0.1
12 7.22 ± 0.23 60 1.4 ± 0.1
13 8.01 ± 0.16 10 1.3 ± 0.1
a

Calcium mobilization mGlu5 assay; values are an average of n ≥ 3 independent experiments.

b

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