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TargetGlutamate receptors

Metabotropic glutamate receptor 2

NMDA, AMPA, kainate and metabotropic receptors.

Measurements
2
Compounds
1
Binding constants
1
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

GRM2_HUMANGRM2Homo sapiens

Metabotropic glutamate receptor 2

Dimeric G protein-coupled receptor which is activated by the excitatory neurotransmitter L-glutamate37286794. Plays critical roles in modulating synaptic transmission and neuronal excitability. Upon activation by glutamate, inhibits presynaptic calcium channels, reducing further glutamate release and dampening excitatory signaling (By similarity). Mechanistically, ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization
(Microbial infection) Plays an important role in influenza virus internalization
(Microbial infection) Acts as a host entry factor for rabies virus that hijacks the endocytosis of GRM2 to enter cells
(Microbial infection) Acts as a host entry factor for SARS-CoV-2 that hijacks the endocytosis of GRM2 to enter cells

Quoted from UniProt’s FUNCTION annotation for Q14416 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
HTR2A0.9980.3430.0000.997
GNAI10.9900.9000.9000.132
GRIA10.9660.0000.0000.964
GRM40.9520.0000.4000.917
GRM70.9450.9000.4000.114
GRM30.9390.0000.9000.390
GNG20.9360.9220.0000.172
GNAI20.9100.0000.9000.131
GNAI30.9030.0000.9000.067
GRIA40.8400.0000.0000.832

Where it sits in the cell

UniProt, curated Cell membrane · Synapse · Cell projection, dendrite

Expression by cell type

Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Brain excitatory neurons12.7 nCPM
  • Retinal amacrine cells9.7 nCPM
  • Other brain neurons5.1 nCPM
  • Cone photoreceptor cells4.1 nCPM
  • Early primary spermatocytes3.4 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • brain4.6 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 1

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Metabotropic glutamate receptor 2Glutamate receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL718215

Functional readouts 1

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Metabotropic glutamate receptor 2Glutamate receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL820027