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Description: BMS-986169 is a novel and potent negative allosteric modulator of GluN2B which is a N-methyl-d-aspartate receptor subtype. BMS-986169 has potential to be used in major depressive disorder. BMS-986169 exhibited high binding affinity for the GluN2B allosteric site (Ki = 4.0 nM) and selective inhibition of GluN2B receptor function (IC50 = 24 nM) in cells. BMS-986169 has demonstrated an acceptable safety and toxicology profile and was selected as a preclinical candidate for further evaluation in major depressive disorder.
References: ACS Med Chem Lett. 2018 Apr 13; 9(5):472-477.
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