Target Validation Information
Target ID T27137
Target Name Metabotropicglutamate receptor 1
Target Type
Research
Drug Potency against Target QUISQUALATE Drug Info IC50 = 25 nM [534590]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine Drug Info IC50 = 398 nM [530473]
N-(3-bromophenyl)-6-chloroquinazolin-4-amine Drug Info IC50 = 955 nM [530473]
(3,4-dimethylphenyl)(4-phenoxyphenyl)methanone Drug Info IC50 = 15300 nM [530245]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine Drug Info IC50 = 713 nM [530473]
N-(2-methyl-2-phenylpropyl)pyrazine-2-carboxamide Drug Info Ki = 6550 nM [528497]
PF-1913539 Drug Info Ki = 0.6 nM [552328]
N-phenethylquinoxaline-2-carboxamide Drug Info Ki = 69 nM [528497]
N-(2-phenylpropyl)quinoxaline-2-carboxamide Drug Info Ki = 22 nM [528497]
GLUTAMATE Drug Info Ki = 250 nM [529001]
Quinoxaline-2-carboxylic acid adamantan-1-ylamide Drug Info IC50 = 5 nM [529241]
N-(2,3-dihydro-1H-inden-2-yl)quinazolin-4-amine Drug Info Ki = 34 nM [530023]
N-cyclohexylquinolin-4-amine Drug Info Ki = 6160 nM [530023]
N-cyclohexylquinazolin-4-amine Drug Info Ki = 27 nM [530023]
Quinoline-3-carboxylic acid adamantan-1-ylamide Drug Info IC50 = 52 nM [529241]
4-(cyclohexyloxy)quinazoline Drug Info Ki = 694 nM [530023]
N-(2,3-dihydro-1H-inden-2-yl)isoquinolin-1-amine Drug Info Ki = 1650 nM [530023]
Quinoline-2-carboxylic acid adamantan-1-ylamide Drug Info IC50 = 440 nM [529241]
Pyrazine-2-carboxylic acid adamantan-1-ylamide Drug Info IC50 = 7000 nM [529241]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone Drug Info Ki = 21 nM [530245]
(E)-4,4-Dimethyl-1-quinolin-3-yl-pent-1-en-3-one Drug Info Ki = 5230 nM [530245]
VU0080241 Drug Info IC50 = 2600 nM [529695]
2-methyl-6-(phenylethynyl)pyridine Drug Info Ki = 36 nM [531019]
Action against Disease Model AZD-9272 AZD 9272, a metabotropic glutamate receptor (mGLUR) antagonist, had IC50 values ranging from 0.02 to 2 mcM in vivo. Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Reduction of mGluR1 moderately decreased Fmr1 KO activity. Reduction of mGluR5 caused an analgesic response in the Fmr1 KO and decreased active social behavior. Modulation of either mGluR1 or mGluR5 did not significantly alter audiogenic seizures, anxiety- and perseverative-related responses, sensorimotor gating, memory, or motor responses. [534590]
References
Ref 534590J 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 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530245Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. Epub 2009 Jun 23.Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 528497Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. Epub 2006 Oct 11.Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Ref 552328Pharmacology of adenosine A2A receptors and therapeutic applications. Curr Top Med Chem. 2003;3(4):413-26.
Ref 528497Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. Epub 2006 Oct 11.Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Ref 528497Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. Epub 2006 Oct 11.Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Ref 529001J 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.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 530023Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Ref 530023Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Ref 530023Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 530023Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Ref 530023Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 529241J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors.
Ref 530245Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. Epub 2009 Jun 23.Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
Ref 530245Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. Epub 2009 Jun 23.Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
Ref 529695Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. Epub 2008 Aug 29.Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.
Ref 531019Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. Epub 2010 Jun 17.Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.

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