Proteins > Metabotropic glutamate receptor 5
Page last updated: 2024-08-07 16:38:02
Metabotropic glutamate receptor 5
A metabotropic glutamate receptor 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P41594]
Synonyms
mGluR5
Research
Bioassay Publications (65)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (10.77) | 18.2507 |
| 2000's | 28 (43.08) | 29.6817 |
| 2010's | 30 (46.15) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (52)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| alpha-methyl-4-carboxyphenylglycine | Homo sapiens (human) | Ki | 2,000.0000 | 1 | 1 |
| ibotenic acid | Homo sapiens (human) | Ki | 17.0000 | 1 | 1 |
| 1-aminoindan-1,5-dicarboxylic acid | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | Ki | 4.3167 | 3 | 3 |
| quisqualic acid | Homo sapiens (human) | Ki | 0.0550 | 1 | 1 |
| L-2-aminoadipic acid | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Homo sapiens (human) | Ki | 15.0000 | 1 | 1 |
| homocysteic acid | Homo sapiens (human) | Ki | 54.0000 | 1 | 1 |
| 2-amino-4-phosphonobutyric acid | Homo sapiens (human) | Ki | 1,000.0000 | 2 | 2 |
| eglumetad | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 3,5-dihydroxyphenylglycine | Homo sapiens (human) | Ki | 1.9000 | 1 | 1 |
| 9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinone | Homo sapiens (human) | IC50 | 5.3333 | 3 | 3 |
| 6-methyl-2-(phenylethynyl)pyridine | Homo sapiens (human) | IC50 | 0.0199 | 20 | 20 |
| 6-methyl-2-(phenylethynyl)pyridine | Homo sapiens (human) | Ki | 0.0166 | 8 | 8 |
| sib 1757 | Homo sapiens (human) | IC50 | 0.3700 | 1 | 1 |
| sib 1757 | Homo sapiens (human) | Ki | 0.3700 | 1 | 1 |
| l-2-(carboxypropyl)glycine | Homo sapiens (human) | Ki | 3.1000 | 1 | 1 |
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| upf 596 | Homo sapiens (human) | IC50 | 300.0000 | 1 | 1 |
| upf 596 | Homo sapiens (human) | Ki | 103.0000 | 1 | 1 |
| ly-367385 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sib 1893 | Homo sapiens (human) | IC50 | 1.4633 | 3 | 3 |
| sib 1893 | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine | Homo sapiens (human) | IC50 | 0.1128 | 10 | 10 |
| 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine | Homo sapiens (human) | Ki | 0.0327 | 2 | 2 |
| ly 341495 | Homo sapiens (human) | IC50 | 8.2000 | 1 | 1 |
| ly 341495 | Homo sapiens (human) | Ki | 8.2000 | 1 | 1 |
| azd9272 | Homo sapiens (human) | IC50 | 0.0168 | 2 | 2 |
| mavoglurant | Homo sapiens (human) | IC50 | 0.0408 | 2 | 2 |
| mavoglurant | Homo sapiens (human) | Ki | 0.0078 | 2 | 2 |
| n-(4-chloro-2-((1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)methyl)phenyl)-2-hydroxybenzamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ly 389795 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| ly 379268 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 3-(5-pyridin-2-yl-2h-tetrazol-2-yl)benzonitrile | Homo sapiens (human) | IC50 | 0.0715 | 2 | 2 |
| 3-fluoro-5-(5-pyridin-2-yl-2h-tetrazol-2-yl)benzonitrile | Homo sapiens (human) | IC50 | 0.0040 | 2 | 2 |
| 3-cyano-n-(1,3-diphenyl-1h-pyrazol-5-yl)benzamide | Homo sapiens (human) | Ki | 0.2500 | 1 | 1 |
| basimglurant | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| basimglurant | Homo sapiens (human) | Ki | 0.0360 | 1 | 1 |
| a 794282 | Homo sapiens (human) | IC50 | 0.4420 | 2 | 2 |
| a-841720 | Homo sapiens (human) | IC50 | 0.3420 | 1 | 1 |
| ro 4956371 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| ro 4956371 | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| 6-fluoro-2-(4-(pyridin-2-yl)but-3-yn-1-yl)imidazo(1,2-a)pyridine | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| wms 1410 | Homo sapiens (human) | IC50 | 0.5600 | 1 | 1 |
| vu0409106 | Homo sapiens (human) | IC50 | 0.0375 | 2 | 2 |
| vu0409106 | Homo sapiens (human) | Ki | 0.0068 | 1 | 1 |
| ml289 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile | Homo sapiens (human) | IC50 | 0.0006 | 2 | 2 |
| 3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| fenobam | Homo sapiens (human) | IC50 | 0.0851 | 7 | 7 |
| fenobam | Homo sapiens (human) | Ki | 0.0792 | 4 | 5 |
Drugs with Activation Measurements
Drugs with Other Measurements
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGluEuropean journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 25, Issue:16, 2015
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Development of 1ACS medicinal chemistry letters, , Dec-08, Volume: 7, Issue:12, 2016
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Isoxazolo[3,4-d]pyridazinones positively modulate the metabotropic glutamate subtypes 2 and 4.Bioorganic & medicinal chemistry, , 09-15, Volume: 26, Issue:17, 2018
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().ACS medicinal chemistry letters, , Dec-08, Volume: 2, Issue:12, 2011
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glutamate receptor activity | molecular function | Combining with glutamate and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:ai, GOC:signaling] |
| protein tyrosine kinase activator activity | molecular function | Increases the activity of a protein tyrosine kinase, an enzyme which phosphorylates a tyrosyl phenolic group on a protein. [GOC:ai, ISBN:0198506732] |
| A2A adenosine receptor binding | molecular function | Binding to an A2A adenosine receptor. [GOC:mah, GOC:nln] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein tyrosine kinase binding | molecular function | Binding to protein tyrosine kinase. [PMID:25499537] |
| adenylate cyclase inhibiting G protein-coupled glutamate receptor activity | molecular function | Combining with glutamate and transmitting the signal across the membrane by activating the alpha-subunit of an associated heterotrimeric G-protein complex to inhibit downstream adenylate cyclase activity. [GOC:bf, GOC:dph] |
| neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration | molecular function | Any neurotransmitter receptor activity that is involved in regulating the concentration of calcium in the postsynaptic cytosol. [GOC:dos] |
| G protein-coupled receptor activity involved in regulation of postsynaptic membrane potential | molecular function | A G protein-coupled receptor activity occurring in the postsynaptic membrane that is part of a GPCR signaling pathway that positively regulates ion channel activity in the postsynaptic membrane. [GOC:dos] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendritic spine | cellular component | A small, membranous protrusion from a dendrite that forms a postsynaptic compartment, typically receiving input from a single presynapse. They function as partially isolated biochemical and an electrical compartments. Spine morphology is variable:they can be thin, stubby, mushroom, or branched, with a continuum of intermediate morphologies. They typically terminate in a bulb shape, linked to the dendritic shaft by a restriction. Spine remodeling is though to be involved in synaptic plasticity. [GOC:nln] |
| dendritic shaft | cellular component | Cylindric portion of the dendrite, directly stemming from the perikaryon, and carrying the dendritic spines. [GOC:nln] |
| astrocyte projection | cellular component | A prolongation or process extending from the soma of an astrocyte and wrapping around neurons. [NIF_Subcellular:sao1630537580] |
| Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 20 target(s):
| Target | Category | Definition |
|---|
| desensitization of G protein-coupled receptor signaling pathway | biological process | The process that stops, prevents, or reduces the frequency, rate or extent of G protein-coupled receptor signaling pathway after prolonged stimulation with an agonist of the pathway. [PMID:8396717] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| protein kinase C-activating G protein-coupled receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds with activation of protein kinase C (PKC). PKC is activated by second messengers including diacylglycerol (DAG). [GOC:mah, GOC:signaling] |
| phospholipase C-activating G protein-coupled glutamate receptor signaling pathway | biological process | A phospholipase C-activating G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled glutamate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, GOC:signaling, PMID:9131252] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| learning or memory | biological process | The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125] |
| learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
| locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| positive regulation of long-term neuronal synaptic plasticity | biological process | A process that increases long-term neuronal synaptic plasticity, the ability of neuronal synapses to change long-term as circumstances require. Long-term neuronal synaptic plasticity generally involves increase or decrease in actual synapse numbers. [GOC:jid, PMID:11891290] |
| synapse organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a synapse, the junction between a neuron and a target (neuron, muscle, or secretory cell). [GOC:ai, GOC:pr] |
| positive regulation of calcium-mediated signaling | biological process | Any process that activates or increases the frequency, rate or extent of calcium-mediated signaling. [GOC:ai] |
| cognition | biological process | The operation of the mind by which an organism becomes aware of objects of thought or perception; it includes the mental activities associated with thinking, learning, and memory. [ISBN:0721619908] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| regulation of postsynaptic cytosolic calcium ion concentration | biological process | Any process that regulates the concentration of calcium in the postsynaptic cytosol. [GOC:dos] |
| cellular response to amyloid-beta | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
| regulation of synaptic transmission, glutamatergic | biological process | Any process that modulates the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
| trans-synaptic signaling by endocannabinoid, modulating synaptic transmission | biological process | Cell-cell signaling between presynapse and postsynapse, via the release and reception of endocannabinoid ligands, that modulates the synaptic transmission properties of the synapse. [GOC:dos, PMID:21531987] |