TargetGlutamate receptors

Glutamate receptor ionotropic, NMDA 1

NMDA, AMPA, kainate and metabotropic receptors.

Measurements: 6
Compounds: 6
Binding constants: 0
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

NMDZ1_HUMANGRIN1Homo sapiens

Glutamate receptor ionotropic, NMDA 1

Component of N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with high calcium permeability and voltage-dependent block by Mg(2+)21376300,26875626,26919761,28126851,28228639,36959261,7679115,7681588,7685113. NMDARs participate in synaptic plasticity for learning and memory formation by contributing to the long-term potentiation (LTP)26875626. Channel activation requires binding of the neurotransmitter L-glutamate to the GluN2 subunit, glycine or D-serine binding to the GluN1 subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+)21376300,26875626,26919761,27164704,28095420,28105280,28126851,28228639,36959261,38538865,7679115,7681588,7685113. NMDARs mediate simultaneously the potassium efflux and the influx of calcium and sodium (By similarity). Each GluN2 or GluN3 subunit confers differential attributes to channel properties, including activation, deactivation and desensitization kinetics, pH sensitivity, Ca2(+) permeability, and binding to allosteric modulators26875626,26919761,36309015,38598639

Quoted from UniProt’s FUNCTION annotation for Q05586 (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.

Partner	Combined	Experiment	Database	Text mining
GRIN2A	0.999	0.996	0.900	0.989
GRIN2B	0.999	0.997	0.900	0.988
GRIN2D	0.999	0.980	0.900	0.989
GRIN2C	0.999	0.811	0.900	0.989
GRIN3B	0.999	0.782	0.900	0.989
GRIN3A	0.999	0.782	0.900	0.991
DLG4	0.998	0.808	0.900	0.937
CALM3	0.996	0.902	0.650	0.913
CALML4	0.964	0.047	0.650	0.902
CALML3	0.960	0.068	0.650	0.889

Where it sits in the cell

UniProt, curated Cell membrane · Postsynaptic cell membrane · Postsynaptic density membrane · Synaptic cell membrane

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 inhibitory neurons259.5 nCPM
Brain excitatory neurons182.1 nCPM
Retinal amacrine cells129.2 nCPM
Other brain neurons119 nCPM
Retinal ganglion cells88.8 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.

brain215.2 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

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

Measured but not drawn — this anatomogram has no outline for them: midbrain 46.5, spinal cord 15.8, retina 3.1, pituitary gland 0.2.

Body

0215 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 GRIN1 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 · 10

cerebral cortex215.2 nTPM
basal ganglia137.0 nTPM
hippocampal formation111.2 nTPM
cerebellum109.1 nTPM
hypothalamus93.3 nTPM
amygdala84.6 nTPM
midbrain46.5 nTPM
spinal cord15.8 nTPM
retina3.1 nTPM
pituitary gland0.2 nTPM

Peripheral and autonomic · 7

salivary gland1.2 nTPM
colon0.7 nTPM
small intestine0.4 nTPM
stomach 10.3 nTPM
duodenum0.3 nTPM
adrenal gland0.1 nTPM
pancreas0.1 nTPM

Transcript is not protein. These are RNA levels for GRIN1, 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.

Functional readouts 6

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

Target	Class	Type	Value (nM)	pX	Organism	Assay
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805
Glutamate receptor ionotropic, NMDA 1	Glutamate receptors	AC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL5291805

← All targets