title: Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5).
abstract: Based on a pharmacophore alignment on known non-competitive mGluR5 inhibitors applying 4SCan technology, a new lead series was identified and further structurally investigated. K(i)'s as low as around 100 nM were achieved.
authors.affiliation: 4SC AG, Martinsried, Germany. stefan.tasler@4sc.com
authors.forename: Stefan
authors.initials: S
authors.lastname: Tasler
authors.forename: Jürgen
authors.initials: J
authors.lastname: Kraus
authors.forename: Stefano
authors.initials: S
authors.lastname: Pegoraro
authors.forename: Andrea
authors.initials: A
authors.lastname: Aschenbrenner
authors.forename: Elena
authors.initials: E
authors.lastname: Poggesi
authors.forename: Rodolfo
authors.initials: R
authors.lastname: Testa
authors.forename: Gianni
authors.initials: G
authors.lastname: Motta
authors.forename: Amedeo
authors.initials: A
authors.lastname: Leonardi
mesh_terms: D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D018691:Excitatory Amino Acid Antagonists; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate