JNJ-40411813

Description: JNJ-40411813 (formerly known as ADX71149) is a novel positive allosteric modulator of the mGlu2R receptor (metabotropic Glutamate 2 receptor) with EC50 of 147 nM. Full in vitro and in vivo profiles indicate that JNJ-40411813 displayed an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity. JNJ-40411813 has been investigated in the clinic for schizophrenia and anxious depression disorders. A different exploration from the lead compound that led to the discovery of a novel subseries of phenylpiperidine-substituted pyridones. The optimization strategy involved the introduction of different spacers between the pyridone core and the phenyl ring of the lead compound.

References: J Med Chem. 2014 Aug 14; 57(15):6495-512.