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PsychedeliaDokholyan Laboratory
TargetCholinergic receptors

Neuronal acetylcholine receptor subunit alpha-4

Muscarinic and nicotinic acetylcholine receptors.

Measurements
9
Compounds
9
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

ACHA4_HUMANCHRNA4Homo sapiens

Neuronal acetylcholine receptor subunit alpha-4

Component of neuronal acetylcholine receptors (nAChRs) that function as pentameric, ligand-gated cation channels with high calcium permeability among other activities. nAChRs are excitatory neurotrasnmitter receptors formed by a collection of nAChR subunits known to mediate synaptic transmission in the nervous system and the neuromuscular junction. Each nAchR subunit confers differential attributes to channel properties, including activation, deactivation and desensitization kinetics, pH sensitivity, cation permeability, and binding to allosteric modulators22361591,27698419,29720657,38454578. CHRNA4 forms heteropentameric neuronal acetylcholine receptors with CHRNB2 and CHRNB4, as well as CHRNA5 and CHRNB3 as accesory subunits. Is the most abundant nAChR subtype expressed in the central nervous system16835356,22361591,27698419,29720657,38454578. Found in two major stoichiometric forms,(CHRNA4)3:(CHRNB2)2 and (CHRNA4)2:(CHRNB2)3, the two stoichiometric forms differ in their unitary conductance, calcium permeability, ACh sensitivity and potentiation by divalent cation27698419,29720657,38454578. Involved in the modulation of calcium-dependent signaling pathways, influences the release of neurotransmitters, including dopamine, glutamate and GABA (By similarity)

Quoted from UniProt’s FUNCTION annotation for P43681 (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
CHRNB20.9940.8020.9000.683
CHRNA20.9390.0000.9000.391
CHRNA70.9250.0910.9000.172
KCNQ20.9240.0000.0000.899
CHRNB40.9200.1260.9000.118
CHRNA90.9160.0000.9000.134
CHRNA30.9150.1170.9000.091
JAK20.9030.0430.9000.073
CHRNA60.8910.1170.8000.412
CHRNA50.8770.1560.5400.695

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 Synaptic cell membrane · Cell membrane

Expression by cell type

Single cell type RNA, the 9 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Retinal horizontal cells110.2 nCPM
  • Hepatocytes68.6 nCPM
  • Gonadotrophs26.3 nCPM
  • Proximal tubule cells24.7 nCPM
  • Epididymal efferent duct absorptive cells24.5 nCPM
  • Retinal amacrine cells16.3 nCPM
  • Oligodendrocyte progenitor cells15.8 nCPM
  • Retinal bipolar cells12.4 nCPM
  • Epididymal efferent duct ciliated cells12.2 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.

  • liver82.6 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 — 10.6 nTPM, from CHRNA4cerebellum — 4.1 nTPM, from CHRNA4hippocampal formation — 7.0 nTPM, from CHRNA4amygdala — 7.7 nTPM, from CHRNA4hypothalamus — 8.5 nTPM, from CHRNA4thalamus — no resolved target expressed herebasal ganglia — 3.5 nTPM, from CHRNA4medulla 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: midbrain 14.0, spinal cord 5.1, retina 2.9, pituitary gland 1.0.

Body

heart — no resolved target expressed heresmooth muscle — no resolved target expressed herelung — no resolved target expressed hereliver — 82.6 nTPM, from CHRNA4kidney — 4.2 nTPM, from CHRNA4stomach — no resolved target expressed hereduodenum — no resolved target expressed heresmall intestine — no resolved target expressed herecolon — no resolved target expressed hereadrenal gland — 0.3 nTPM, from CHRNA4thyroid gland — 0.5 nTPM, from CHRNA4pancreas — no resolved target expressed hereurinary bladder — no resolved target expressed hereskeletal muscle — no resolved target expressed herespleen — 2.3 nTPM, from CHRNA4salivary gland — no resolved target expressed here
083 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 CHRNA4 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

  • midbrain14.0 nTPM
  • cerebral cortex10.6 nTPM
  • hypothalamus8.5 nTPM
  • amygdala7.7 nTPM
  • hippocampal formation7.0 nTPM
  • spinal cord5.1 nTPM
  • cerebellum4.1 nTPM
  • basal ganglia3.5 nTPM
  • retina2.9 nTPM
  • pituitary gland1.0 nTPM

Peripheral and autonomic · 5

  • liver82.6 nTPM
  • kidney4.2 nTPM
  • spleen2.3 nTPM
  • thyroid gland0.5 nTPM
  • adrenal gland0.3 nTPM

Transcript is not protein. These are RNA levels for CHRNA4, 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 9

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

TargetClassTypeValue (nM)pXOrganismAssay
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
Neuronal acetylcholine receptor subunit alpha-4Cholinergic receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291770
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