Page last updated: 2024-08-07 17:05:01

Metabotropic glutamate receptor 1

A metabotropic glutamate receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13255]

Synonyms

mGluR1

Research

Bioassay Publications (32)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (37.50)18.2507
2000's14 (43.75)29.6817
2010's6 (18.75)24.3611
2020's0 (0.00)2.80

Compounds (49)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
alpha-methyl-4-carboxyphenylglycineHomo sapiens (human)IC50155.000022
alpha-methyl-4-carboxyphenylglycineHomo sapiens (human)Ki295.000022
ibotenic acidHomo sapiens (human)Ki43.000011
4-carboxy-3-hydroxyphenylglycineHomo sapiens (human)IC5040.000011
4-carboxy-3-hydroxyphenylglycineHomo sapiens (human)Ki30.000011
1-aminoindan-1,5-dicarboxylic acidHomo sapiens (human)IC50110.500022
1-aminoindan-1,5-dicarboxylic acidHomo sapiens (human)Ki214.000011
4-carboxyphenylglycineHomo sapiens (human)IC5065.000011
glutamic acidHomo sapiens (human)Ki3.606733
quisqualic acidHomo sapiens (human)Ki1.100011
L-2-aminoadipic acidHomo sapiens (human)Ki1,000.000011
1-amino-1,3-dicarboxycyclopentaneHomo sapiens (human)Ki42.000011
philanthotoxin 343Homo sapiens (human)IC500.023011
homocysteic acidHomo sapiens (human)Ki87.000011
2-amino-4-phosphonobutyric acidHomo sapiens (human)Ki1,000.000022
eglumetadHomo sapiens (human)Ki100.000011
3,5-dihydroxyphenylglycineHomo sapiens (human)Ki6.600011
alpha-methyl-4-carboxyphenylglycineHomo sapiens (human)IC504.300011
9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinoneHomo sapiens (human)IC500.009533
4-bromohomoibotenic acid, (rs)-isomerHomo sapiens (human)Ki329.000011
6-methyl-2-(phenylethynyl)pyridineHomo sapiens (human)IC50100.000011
6-methyl-2-(phenylethynyl)pyridineHomo sapiens (human)Ki15.018022
4-methylglutamic acid, threo-(l)-isomerHomo sapiens (human)Ki10.000011
sib 1757Homo sapiens (human)IC50100.000011
sib 1757Homo sapiens (human)Ki100.000011
l-2-(carboxypropyl)glycineHomo sapiens (human)Ki50.000011
2r,4r-4-aminopyrrolidine-2,4-dicarboxylateHomo sapiens (human)Ki100.000011
upf 596Homo sapiens (human)IC5026.750044
upf 596Homo sapiens (human)Ki25.000011
ly-367385Homo sapiens (human)IC508.400022
sib 1893Homo sapiens (human)IC50100.000011
sib 1893Homo sapiens (human)Ki100.000011
4-carboxy-3-hydroxyphenylglycineHomo sapiens (human)IC5040.000022
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidineHomo sapiens (human)IC50100.000011
ly 341495Homo sapiens (human)IC507.800011
ly 341495Homo sapiens (human)Ki6.800011
bay36-7620Homo sapiens (human)IC500.160011
ly 389795Homo sapiens (human)Ki100.000011
ly 379268Homo sapiens (human)Ki100.000011
r 214127Homo sapiens (human)IC500.014011
jnj16259685Homo sapiens (human)IC500.035923
jnj16259685Homo sapiens (human)Ki0.000311
a 794282Homo sapiens (human)IC500.003033
a-841720Homo sapiens (human)IC500.010011
sp 203Homo sapiens (human)Ki10.000011
fenobamHomo sapiens (human)Ki0.006711

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
aspartic acidHomo sapiens (human)EC501,000.000011
d-glutamateHomo sapiens (human)EC501,000.000011
glutamic acidHomo sapiens (human)EC5045.237544
quisqualic acidHomo sapiens (human)EC500.200011
1-amino-1,3-dicarboxycyclopentane, (trans)-isomerHomo sapiens (human)EC50127.000011
d-aspartic acidHomo sapiens (human)EC501,000.000011
L-2-aminoadipic acidHomo sapiens (human)EC501,000.000011
alpha-aminopimelic acidHomo sapiens (human)EC501,000.000011
1-amino-1,3-dicarboxycyclopentaneHomo sapiens (human)EC5015.433333
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acidHomo sapiens (human)EC501,000.000011
alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acidHomo sapiens (human)EC501,000.000011
eglumetadHomo sapiens (human)EC50100.000011
3,5-dihydroxyphenylglycineHomo sapiens (human)EC506.600011
upf 596Homo sapiens (human)EC50300.000011
1-amino-1,3-dicarboxycyclopentane, cis-(1s,3s)-isomerHomo sapiens (human)EC50300.000022
ampa, (r)-isomerHomo sapiens (human)EC501,000.000011
ly 379268Homo sapiens (human)EC50100.000011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
glutamic acidHomo sapiens (human)Activity1.000011
1-amino-1,3-dicarboxycyclopentaneHomo sapiens (human)Activity42.000011
eglumetadHomo sapiens (human)Activity100.000011
l-2-(carboxypropyl)glycineHomo sapiens (human)Activity23.000011
2-(2,3-dicarboxycyclopropyl)glycineHomo sapiens (human)Activity100.000011
1-aminocyclopentane-1,3,4-tricarboxylic acidHomo sapiens (human)Kb557.500012
mgs 0028Homo sapiens (human)Activity100.000011
ly 379268Homo sapiens (human)Activity100.000011

Enables

This protein enables 7 target(s):

TargetCategoryDefinition
G protein-coupled receptor activitymolecular functionCombining 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 bindingmolecular functionBinding to a protein. [GOC:go_curators]
glutamate receptor activitymolecular functionCombining 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]
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationmolecular functionA G protein-coupled neurotransmitter receptor activity occurring in the postsynaptic membrane, that is involved in regulating the cytosolic concentration of calcium ions in the postsynapse. [GOC:dos]
adenylate cyclase inhibiting G protein-coupled glutamate receptor activitymolecular functionCombining 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 concentrationmolecular functionAny 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 potentialmolecular functionA 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 5 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
dendritecellular componentA 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]
Schaffer collateral - CA1 synapsecellular componentA synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689]
glutamatergic synapsecellular componentA synapse that uses glutamate as a neurotransmitter. [GOC:dos]

Active In

This protein is active in 2 target(s):

TargetCategoryDefinition
postsynaptic density membranecellular componentThe 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 membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Part Of

This protein is part of 2 target(s):

TargetCategoryDefinition
G protein-coupled receptor dimeric complexcellular componentA protein complex that contains two G protein-coupled receptors. [GOC:al, GOC:bf, PMID:10713101]
G protein-coupled receptor homodimeric complexcellular componentA protein complex that contains two G protein-coupled receptors (GPCRs) of the same subtype. Formation of a GPCR homodimer may be important for the transport of newly formed receptors to the cell surface, and the function of the receptor. [GOC:al, GOC:bf, PMID:10713101, PMID:16670762]

Involved In

This protein is involved in 14 target(s):

TargetCategoryDefinition
G protein-coupled receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwaybiological processAn 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]
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwaybiological processA 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]
chemical synaptic transmissionbiological processThe 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]
locomotory behaviorbiological processThe 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]
sensory perception of painbiological processThe series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators]
positive regulation of MAPK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators]
regulation of sensory perception of painbiological processAny process that modulates the frequency, rate or extent of the sensory perception of pain, the series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. [GOC:ai]
regulation of postsynaptic membrane potentialbiological processAny process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef]
cellular response to electrical stimulusbiological processAny 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 an electrical stimulus. [GOC:mah]
L-glutamate import across plasma membranebiological processThe directed movement of L-glutamate from outside of a cell, across the plasma membrane and into the cytosol. [GOC:dos]
regulation of postsynaptic cytosolic calcium ion concentrationbiological processAny process that regulates the concentration of calcium in the postsynaptic cytosol. [GOC:dos]
G protein-coupled glutamate receptor signaling pathwaybiological processA 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]
regulation of synaptic transmission, glutamatergicbiological processAny 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]