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. 2011 Apr 15;2(8):411–432. doi: 10.1021/cn2000266

Table 11. Functional mGlu5 Activity in the Nicotinamide Series.

graphic file with name cn-2011-000266_0031.jpg

entry n X A R mGlu5 IC50 (nM)
171 1 H CH Cl 310
172 0 H CH Cl 5400
173 2 H CH Cl 250
174 3 H CH Cl 2300
175 1 H CH H ∼10 000
176 1 H CH F 2300
177 1 H CH Me 2300
178 1 H CH OMe 1800
179 1 H N Me 420
180 1 Cl CH Cl 95
181 1 Cl N Me 87