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TargetCholinergic receptors

Acetylcholine receptor subunit alpha

Muscarinic and nicotinic acetylcholine receptors.

Measurements
8
Compounds
2
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

ACHA_HUMANCHRNA1Homo sapiens

Acetylcholine receptor subunit alpha

Upon acetylcholine binding, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
Non functional acetylcholine receptor alpha subunit which is not integrated into functional acetylcholine-gated cation-selective channels

Quoted from UniProt’s FUNCTION annotation for P02708 (reviewed).

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
CHRND0.9590.6930.5400.681
CHRNE0.9410.5570.5400.707
CHRNG0.9260.5540.5400.580
CHRNB10.9120.4010.5400.673
RAPSN0.8830.0950.0000.863
CHRNA30.8440.4010.5400.422
CHRNA90.8280.3060.5400.458
CHRNA40.8120.3090.5400.409
CHRNB40.7670.4010.5400.126
AIRE0.7640.0450.0000.764

Where it sits in the cell

  • Plasma membrane

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

UniProt, curated Postsynaptic cell membrane · Cell membrane

Expression by cell type

Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Myosatellite cells166.5 nCPM
  • Myonuclei62.1 nCPM
  • Thymic myoid cells55.7 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.

  • skeletal muscle160.2 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

cerebral cortex — 0.6 nTPM, from CHRNA1cerebellum — no resolved target expressed herehippocampal formation — 6.2 nTPM, from CHRNA1amygdala — 0.3 nTPM, from CHRNA1hypothalamus — 0.1 nTPM, from CHRNA1thalamus — no resolved target expressed herebasal ganglia — 0.2 nTPM, from CHRNA1medulla 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: pituitary gland 3.1, spinal cord 1.3, midbrain 0.2.

Body

heart — 0.3 nTPM, from CHRNA1smooth muscle — no resolved target expressed herelung — 0.5 nTPM, from CHRNA1liver — 0.2 nTPM, from CHRNA1kidney — no resolved target expressed herestomach — no resolved target expressed hereduodenum — 0.2 nTPM, from CHRNA1small intestine — no resolved target expressed herecolon — 1.4 nTPM, from CHRNA1adrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — no resolved target expressed hereurinary bladder — no resolved target expressed hereskeletal muscle — 160.2 nTPM, from CHRNA1spleen — no resolved target expressed heresalivary gland — 3.4 nTPM, from CHRNA1
0160 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 CHRNA1 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 · 8

  • hippocampal formation6.2 nTPM
  • pituitary gland3.1 nTPM
  • spinal cord1.3 nTPM
  • cerebral cortex0.6 nTPM
  • amygdala0.3 nTPM
  • basal ganglia0.2 nTPM
  • midbrain0.2 nTPM
  • hypothalamus0.1 nTPM

Peripheral and autonomic · 7

  • skeletal muscle160.2 nTPM
  • salivary gland3.4 nTPM
  • colon1.4 nTPM
  • lung0.5 nTPM
  • heart muscle0.3 nTPM
  • liver0.2 nTPM
  • duodenum0.2 nTPM

Transcript is not protein. These are RNA levels for CHRNA1, 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.

TargetClassTypeValue (nM)pXOrganismAssay
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071478
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071478
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071479
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071479
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071480
Acetylcholine receptor subunit alphaCholinergic receptorsIC50— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3071480

Other measurements 2

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Acetylcholine receptor subunit alphaCholinergic receptorsInhibition— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3055638
Acetylcholine receptor subunit alphaCholinergic receptorsInhibition— no normalized value— value does not convert to pXTorpedo californicaCHEMBL3055637