Target Validation Information
TTD ID T62820
Target Name Metabotropic glutamate receptor 2 (mGluR2)
Type of Target
Clinical trial
Drug Potency against Target LY-544344 Drug Info IC50 = 11~38 nM [4]
LY354740 Drug Info IC50 = 11~38 nM [5]
Drug Info Ki = 11000 nM [2]
LY-379268 Drug Info Ki = 14.1 nM [1]
LY-389795 Drug Info Ki = 40.6 nM [1]
[3H]quisqualate Drug Info IC50 = 25 nM [3]
References
REF 1 Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identif... J Med Chem. 2007 Jan 25;50(2):233-40.
REF 2 Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisom... J Med Chem. 2007 Sep 20;50(19):4630-41.
REF 3 Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9.
REF 4 Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
REF 5 Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). Curr Top Med Chem. 2005;5(9):869-84.

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