Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype

Autor:	Anette Graven Sams, Gitte Mikkelsen, Andreas Ritzen, Xiaosui Pu, Robbin Brodbeck
Rok vydání:	2011
Předmět:	Allosteric modulator Stereochemistry Receptor Metabotropic Glutamate 5 animal diseases Clinical Biochemistry Allosteric regulation Pharmaceutical Science Ligands Receptors Metabotropic Glutamate Biochemistry Small Molecule Libraries Inhibitory Concentration 50 Structure-Activity Relationship Allosteric Regulation mental disorders Drug Discovery Potency Receptor Molecular Biology Molecular Structure Chemotype Metabotropic glutamate receptor 5 Chemistry Organic Chemistry Glutamate receptor Metabotropic receptor nervous system Drug Design Molecular Medicine Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:3407-3410
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2011.03.103
Popis:	A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the underlying SAR is detailed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8240f41d29dcca0e37700b370af03a93 https://doi.org/10.1016/j.bmcl.2011.03.103 Zobrazit plný text záznamu Full Text from ScienceDirect