Proteins > Metabotropic glutamate receptor 5
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Metabotropic glutamate receptor 5
A metabotropic glutamate receptor 5 that is encoded in the genome of rat. [OMA:P31424, PRO:DNx]
Synonyms
mGluR5
Research
Bioassay Publications (50)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (4.00) | 18.2507 |
| 2000's | 27 (54.00) | 29.6817 |
| 2010's | 21 (42.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (46)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Rattus norvegicus (Norway rat) | EC50 | 0.6400 | 1 | 2 |
| imetit | Rattus norvegicus (Norway rat) | EC50 | 0.0024 | 1 | 2 |
| d-glutamate | Rattus norvegicus (Norway rat) | EC50 | 4.4000 | 1 | 1 |
| glutamic acid | Rattus norvegicus (Norway rat) | EC50 | 6.4817 | 8 | 10 |
| quisqualic acid | Rattus norvegicus (Norway rat) | EC50 | 0.2333 | 2 | 3 |
| L-2-aminoadipic acid | Rattus norvegicus (Norway rat) | EC50 | 1,000.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Rattus norvegicus (Norway rat) | EC50 | 36.5000 | 2 | 2 |
| alpha-methylhistamine | Rattus norvegicus (Norway rat) | EC50 | 0.0028 | 1 | 2 |
| 2-amino-4-phosphonobutyric acid | Rattus norvegicus (Norway rat) | EC50 | 640.0000 | 4 | 5 |
| l-2-(carboxypropyl)glycine | Rattus norvegicus (Norway rat) | EC50 | 17.0000 | 1 | 2 |
| 2-(2,3-dicarboxycyclopropyl)glycine | Rattus norvegicus (Norway rat) | EC50 | 389.0000 | 1 | 2 |
| 1-aminocyclopentane-1,3,4-tricarboxylic acid | Rattus norvegicus (Norway rat) | EC50 | 1,000.0000 | 1 | 1 |
| ly 341495 | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 1 |
| n-(4-chloro-2-((1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)methyl)phenyl)-2-hydroxybenzamide | Rattus norvegicus (Norway rat) | EC50 | 1.0000 | 1 | 1 |
| 3-cyano-n-(1,3-diphenyl-1h-pyrazol-5-yl)benzamide | Rattus norvegicus (Norway rat) | EC50 | 0.0650 | 3 | 3 |
| adx 47273 | Rattus norvegicus (Norway rat) | EC50 | 0.1125 | 2 | 2 |
| n-(1,3-diphenyl-1h-pyrazolo-5-yl)-4-nitrobenzamide | Rattus norvegicus (Norway rat) | EC50 | 0.0107 | 1 | 1 |
| vu 1545 | Rattus norvegicus (Norway rat) | EC50 | 0.0096 | 1 | 1 |
| vu0092273 | Rattus norvegicus (Norway rat) | EC50 | 0.2700 | 1 | 1 |
| 3,4-dicarboxyphenylglycine | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 2 |
| mk 5046 | Rattus norvegicus (Norway rat) | EC50 | 0.0140 | 1 | 1 |
| n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide | Rattus norvegicus (Norway rat) | EC50 | 0.0275 | 2 | 2 |
| vu0424465 | Rattus norvegicus (Norway rat) | EC50 | 0.3655 | 3 | 5 |
| lsn2463359 | Rattus norvegicus (Norway rat) | EC50 | 0.0240 | 1 | 1 |
Drugs with Other Measurements
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Synthesis and studies on the mGluR agonist activity of FAP4 stereoisomers.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 25, Issue:12, 2015
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
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
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
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
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
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
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
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 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
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
Development of 1ACS medicinal chemistry letters, , Dec-08, Volume: 7, Issue:12, 2016
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 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
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 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
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
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
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
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
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
[no title available]Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 23, Issue:21, 2013
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
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 22, Issue:20, 2012