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. Author manuscript; available in PMC: 2012 Aug 17.
Published in final edited form as: ACS Chem Neurosci. 2011 Aug 17;2(8):411–432. doi: 10.1021/cn2000266

Table 16.

mGlu5 potency in the quinazoline series

graphic file with name nihms-291053-t0014.jpg

Entry R1 R2 mGlu5 IC50 (nM)
219 Br Cl 256
220 Br H >10,000
221 Br F 1970
222 Br Br 174
223 Br Me 246
224 Br OMe >10,000
225 Cl Cl 130
226 F Cl 311
227 NO2 Cl 274
228 OMe Cl 1510
229 Cl Br 124
230 F Br 96
231 F Me 1350
232 F CF3 >10,000
233 F CN 1370
234 F OMe >10,000