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TargetGlutamate receptors

Metabotropic glutamate receptor 1

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

GRM1_HUMANGRM1Homo sapiens

Metabotropic glutamate receptor 1

G protein-coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system. May participate in the central action of glutamate in the CNS, such as long-term potentiation in the hippocampus and long-term depression in the cerebellum24603153,28886343,7476890. May function in the light response in the retina (By similarity). Induces GRID1 and GRID2 cation-channel activation via GNAQ-PLC-PKC pathway in dopaminergic neurons and cerebellar Purkinje cell, respectively24357660,27276689

Quoted from UniProt’s FUNCTION annotation for Q13255 (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
GNAQ0.9980.0000.9000.985
HOMER10.9980.3700.9000.971
HOMER30.9900.1350.9000.902
HOMER20.9890.0960.9000.893
GRM50.9770.0000.9000.728
CAMK2A0.9680.0910.9000.608
SPTBN20.9400.0000.9000.399
DLGAP10.9380.0000.5000.866
CAMK2B0.9330.0910.9000.248
AGAP20.9280.0950.9000.222

Where it sits in the cell

  • Vesicles

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane · Postsynaptic cell membrane · Cell projection, dendrite

Expression by cell type

Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Brain excitatory neurons529.4 nCPM
  • Rod photoreceptor cells392.7 nCPM
  • Brain inhibitory neurons328.5 nCPM
  • Retinal ganglion cells131.3 nCPM
  • Other brain neurons98.6 nCPM
  • Retinal amacrine cells84.6 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.

  • brain16 nTPM
  • retina5.1 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 4.0 nTPM, from GRM1cerebellum — 16.0 nTPM, from GRM1hippocampal formation — 2.6 nTPM, from GRM1amygdala — 1.6 nTPM, from GRM1hypothalamus — 1.8 nTPM, from GRM1thalamus — no resolved target expressed herebasal ganglia — 1.6 nTPM, from GRM1medulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: retina 5.1, midbrain 1.5, spinal cord 0.6.

Body

heart — 2.6 nTPM, from GRM1smooth muscle — no resolved target expressed herelung — no resolved target expressed hereliver — no resolved target expressed herekidney — 0.7 nTPM, from GRM1stomach — no resolved target expressed hereduodenum — no resolved target expressed heresmall intestine — no resolved target expressed herecolon — no resolved target expressed hereadrenal gland — no resolved target expressed herethyroid gland — 0.1 nTPM, from GRM1pancreas — no resolved target expressed hereurinary bladder — no resolved target expressed hereskeletal muscle — no resolved target expressed herespleen — no resolved target expressed heresalivary gland — no resolved target expressed here
016 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of GRM1 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 9

  • cerebellum16.0 nTPM
  • retina5.1 nTPM
  • cerebral cortex4.0 nTPM
  • hippocampal formation2.6 nTPM
  • hypothalamus1.8 nTPM
  • amygdala1.6 nTPM
  • basal ganglia1.6 nTPM
  • midbrain1.5 nTPM
  • spinal cord0.6 nTPM

Peripheral and autonomic · 3

  • heart muscle2.6 nTPM
  • kidney0.7 nTPM
  • thyroid gland0.1 nTPM

Transcript is not protein. These are RNA levels for GRM1, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

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 1Glutamate receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL719076

Functional readouts 1

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

TargetClassTypeValue (nM)pXOrganismAssay
Metabotropic glutamate receptor 1Glutamate receptorsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL822312