Proteins > Metabotropic glutamate receptor 1
Page last updated: 2024-08-07 16:13:54
Metabotropic glutamate receptor 1
A metabotropic glutamate receptor 1 that is encoded in the genome of rat. [OMA:P23385, PRO:DNx]
Synonyms
mGluR1
Research
Bioassay Publications (27)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (14.81) | 18.2507 |
| 2000's | 15 (55.56) | 29.6817 |
| 2010's | 8 (29.63) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (34)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| melatonin | Rattus norvegicus (Norway rat) | IC50 | 0.0004 | 2 | 2 |
| glutamic acid | Rattus norvegicus (Norway rat) | Ki | 0.3400 | 1 | 1 |
| quisqualic acid | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| 6-methoxy-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-one | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| harmalan | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 2-amino-4-phosphonobutyric acid | Rattus norvegicus (Norway rat) | Ki | 1,000.0000 | 1 | 1 |
| eglumetad | Rattus norvegicus (Norway rat) | IC50 | 458.0000 | 1 | 1 |
| wortmannin | Rattus norvegicus (Norway rat) | IC50 | 0.0085 | 2 | 2 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 3,5-dihydroxyphenylglycine | Rattus norvegicus (Norway rat) | Ki | 0.9000 | 1 | 1 |
| 9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinone | Rattus norvegicus (Norway rat) | IC50 | 0.0095 | 1 | 1 |
| 9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinone | Rattus norvegicus (Norway rat) | Ki | 0.0079 | 1 | 1 |
| 6-methyl-2-(phenylethynyl)pyridine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 2 | 2 |
| n-(n-(phenyl)butyryl-l-prolyl)pyrrolidine | Rattus norvegicus (Norway rat) | IC50 | 0.1300 | 1 | 4 |
| 5-methoxycarbonylamino-n-acetyltryptamine | Rattus norvegicus (Norway rat) | IC50 | 2.5000 | 2 | 2 |
| harmine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 2-(2,3-dicarboxycyclopropyl)glycine | Rattus norvegicus (Norway rat) | IC50 | 389.0000 | 1 | 1 |
| 2-(2,3-dicarboxycyclopropyl)glycine | Rattus norvegicus (Norway rat) | Ki | 77.0000 | 1 | 1 |
| upf 596 | Rattus norvegicus (Norway rat) | IC50 | 25.0000 | 1 | 1 |
| 4-carboxy-3-hydroxyphenylglycine | Rattus norvegicus (Norway rat) | IC50 | 40.0000 | 1 | 1 |
| 1-aminocyclopentane-1,3,4-tricarboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 115.0000 | 1 | 1 |
| 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 2 | 2 |
| ly 341495 | Rattus norvegicus (Norway rat) | IC50 | 8.9900 | 1 | 1 |
| r 214127 | Rattus norvegicus (Norway rat) | IC50 | 0.0060 | 1 | 1 |
| kyp 2047 | Rattus norvegicus (Norway rat) | IC50 | 0.0060 | 1 | 4 |
| jnj16259685 | Rattus norvegicus (Norway rat) | IC50 | 0.0240 | 1 | 2 |
| a 794282 | Rattus norvegicus (Norway rat) | IC50 | 0.0037 | 2 | 3 |
| a-841720 | Rattus norvegicus (Norway rat) | IC50 | 0.0055 | 2 | 2 |
| cep 33779 | Rattus norvegicus (Norway rat) | IC50 | 0.0810 | 1 | 1 |
Drugs with Activation 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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
New probes of the agonist binding site of metabotropic glutamate receptors.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
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
(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
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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
(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
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
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
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
(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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.Journal of medicinal chemistry, , May-06, Volume: 42, Issue:9, 1999
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
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