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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 17.

mGlu5 potency in the N,N'-(1,3-phenylene)diamide series

graphic file with name nihms-291053-t0015.jpg

Entry R1 R2 mGlu5 IC50 (nM)
240 2-OMe 3-chlorophenyl 880
241 2-OMe 2-chlorophenyl >30,000
242 2-OMe 4-chlorophenyl >30,000
243 2-OMe 3-fluorophenyl 6480
244 2-OMe 3-methylphenyl 1350
245 2-OMe 3-(CF3)phenyl 10,600
246 2-OMe 3-cyanophenyl 1800
247 2-OMe benzyl >30,000
248 3-Cl 2-chlorophenyl 2620
249 3-Cl 3-chlorophenyl >30,000
250 3-C1 2-furyl 4510
251 3-Cl cyclopentyl >30,000
252 3-Cl cyclobutyl 5270
253 3-Cl cyclopropyl 2230
254 3-Cl isonicotinamide PAM
255 3-Cl nicotinamide PAM