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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