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ID: ALA1153700
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Authors: Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW.
Abstract: This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.
CiteXplore: 19875287