Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T27137 | ||||
Target Name | Metabotropic glutamate receptor 1 (mGluR1) | ||||
Type of Target |
Discontinued |
||||
Drug Potency against Target | PF-1913539 | Drug Info | Ki = 0.6 nM | [10] | |
Drug Info | Ki = 250 nM | [2] | |||
(3,4-dimethylphenyl)(4-phenoxyphenyl)methanone | Drug Info | IC50 = 15300 nM | [6] | ||
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone | Drug Info | Ki = 21 nM | [6] | ||
(E)-4,4-Dimethyl-1-quinolin-3-yl-pent-1-en-3-one | Drug Info | Ki = 5230 nM | [6] | ||
2-methyl-6-(phenylethynyl)pyridine | Drug Info | Ki = 36 nM | [8] | ||
4-(cyclohexyloxy)quinazoline | Drug Info | Ki = 694 nM | [5] | ||
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | IC50 = 398 nM | [7] | ||
N-(2,3-dihydro-1H-inden-2-yl)isoquinolin-1-amine | Drug Info | Ki = 1650 nM | [5] | ||
N-(2,3-dihydro-1H-inden-2-yl)quinazolin-4-amine | Drug Info | Ki = 34 nM | [5] | ||
N-(2-methyl-2-phenylpropyl)pyrazine-2-carboxamide | Drug Info | Ki = 6550 nM | [1] | ||
N-(2-phenylpropyl)quinoxaline-2-carboxamide | Drug Info | Ki = 22 nM | [1] | ||
N-(3-bromophenyl)-6-chloroquinazolin-4-amine | Drug Info | IC50 = 955 nM | [7] | ||
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine | Drug Info | IC50 = 713 nM | [7] | ||
N-cyclohexylquinazolin-4-amine | Drug Info | Ki = 27 nM | [5] | ||
N-cyclohexylquinolin-4-amine | Drug Info | Ki = 6160 nM | [5] | ||
N-phenethylquinoxaline-2-carboxamide | Drug Info | Ki = 69 nM | [1] | ||
NPS-2390 | Drug Info | IC50 = 5 nM | [3] | ||
Pyrazine-2-carboxylic acid adamantan-1-ylamide | Drug Info | IC50 = 7000 nM | [3] | ||
Quinoline-2-carboxylic acid adamantan-1-ylamide | Drug Info | IC50 = 440 nM | [3] | ||
Quinoline-3-carboxylic acid adamantan-1-ylamide | Drug Info | IC50 = 52 nM | [3] | ||
VU0080241 | Drug Info | IC50 = 2600 nM | [4] | ||
[3H]quisqualate | Drug Info | IC50 = 25 nM | [9] | ||
Action against Disease Model | AZD-9272 | Drug Info | AZD 9272, a metabotropic glutamate receptor (mGLUR) antagonist, had IC50 values ranging from 0.02 to 2 mcM in vivo. | ||
References | |||||
REF 1 | Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. | ||||
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 | Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47. | ||||
REF 4 | Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel ... Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. | ||||
REF 5 | In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. | ||||
REF 6 | Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate recepto... Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. | ||||
REF 7 | Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. | ||||
REF 8 | Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. | ||||
REF 9 | 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 10 | Pharmacology of adenosine A2A receptors and therapeutic applications. Curr Top Med Chem. 2003;3(4):413-26. | ||||
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