| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T62820 | ||||
| Target Name | Metabotropic glutamate receptor 2 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | QUISQUALATE | Drug Info | IC50 = 25 nM | [534590] | |
| LY-544344 | Drug Info | IC50 = 11~38 nM | [536272] | ||
| LY354740 | Drug Info | IC50 = 11~38 nM | [552548] | ||
| LY-379268 | Drug Info | Ki = 14.1 nM | [528620] | ||
| LY-389795 | Drug Info | Ki = 40.6 nM | [528620] | ||
| GLUTAMATE | Drug Info | Ki = 11000 nM | [529001] | ||
| References | |||||
| Ref 534590 | J Med Chem. 1998 Mar 12;41(6):930-9.Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid. | ||||
| Ref 536272 | Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84. | ||||
| Ref 552548 | Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). Curr Top Med Chem. 2005;5(9):869-84. | ||||
| Ref 528620 | J Med Chem. 2007 Jan 25;50(2):233-40.Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors. | ||||
| Ref 528620 | J Med Chem. 2007 Jan 25;50(2):233-40.Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors. | ||||
| Ref 529001 | J Med Chem. 2007 Sep 20;50(19):4630-41. Epub 2007 Aug 29.Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs. | ||||
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