Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR
J Med Chem. 2013 56 (20): 7976-96

PMID: 24050755 · PMCID: PMC3908770 · DOI:10.1021/jm401028t

MeSH Terms (22)

Acetylene Allosteric Regulation Amides Animals Binding, Competitive Cell Membrane Drug Discovery Excitatory Postsynaptic Potentials HEK293 Cells Hippocampus Humans Male Models, Chemical Models, Molecular Molecular Structure Picolinic Acids Protein Structure, Tertiary Radioligand Assay Rats Rats, Sprague-Dawley Receptor, Metabotropic Glutamate 5 Structure-Activity Relationship

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