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TargetSerotonin receptors

5-HT3A

5-HT receptor subtypes.

Measurements
25
Compounds
17
Binding constants
7
Median pX
9.02

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

5HT3A_HUMANHTR3AHomo sapiens

5-hydroxytryptamine receptor 3A

Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons

Quoted from UniProt’s FUNCTION annotation for P46098 (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
HTR3B0.9990.6060.9000.978
HTR3D0.9950.3290.9000.932
HTR3C0.9930.3290.9000.912
HTR3E0.9790.3290.9000.714
RIC30.9380.0510.0000.938
HTR2A0.8810.0000.0000.881
GRIN2A0.8400.0000.7200.451
GRIN2B0.8180.0000.7200.376
GRIA10.8140.0000.7200.355
GRIA20.8060.0000.7200.329

Where it sits in the cell

UniProt, curated Postsynaptic cell membrane · Cell membrane

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • B-cells5.5 nCPM
  • Pancreatic acinar cells5.5 nCPM
  • Salivary acinar cells2.9 nCPM
  • Brain inhibitory neurons2.6 nCPM
  • cDC2.4 nCPM
  • pDCs2.1 nCPM
  • Salivary myoepithelial cells1.9 nCPM
  • Submucosal glandular cells1.1 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.

  • lymphoid tissue7.5 nTPM
  • salivary gland4.8 nTPM
  • pancreas2.7 nTPM
  • brain2.3 nTPM
  • intestine2 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 — 0.9 nTPM, from HTR3Acerebellum — no resolved target expressed herehippocampal formation — 1.5 nTPM, from HTR3Aamygdala — 1.4 nTPM, from HTR3Ahypothalamus — no resolved target expressed herethalamus — no resolved target expressed herebasal ganglia — 2.3 nTPM, from HTR3Amedulla 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 0.1.

05 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 HTR3A 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 · 5

  • basal ganglia2.3 nTPM
  • hippocampal formation1.5 nTPM
  • amygdala1.4 nTPM
  • cerebral cortex0.9 nTPM
  • midbrain0.1 nTPM

Peripheral and autonomic · 11

  • salivary gland4.8 nTPM
  • pancreas2.7 nTPM
  • colon2.0 nTPM
  • small intestine1.6 nTPM
  • stomach 10.8 nTPM
  • smooth muscle0.6 nTPM
  • duodenum0.6 nTPM
  • spleen0.5 nTPM
  • adrenal gland0.3 nTPM
  • kidney0.1 nTPM
  • urinary bladder0.1 nTPM

Transcript is not protein. These are RNA levels for HTR3A, 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.

III · Ranking

Compounds by strongest binding constant

One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.

  1. 01quipazine9.02

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 7

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

TargetClassTypeValue (nM)pXOrganismAssay
5-HT3ASerotonin receptorsKi0.9609.02Rattus norvegicusCHEMBL1006686
5-HT3ASerotonin receptorsKi0.9609.02Rattus norvegicusCHEMBL1037804
5-HT3ASerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235596
5-HT3ASerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235596
5-HT3ASerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL896285
5-HT3ASerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL896285
5-HT3ASerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2393673

Functional readouts 9

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

TargetClassTypeValue (nM)pXOrganismAssay
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824
5-HT3ASerotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291824

Other measurements 9

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
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054022
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054022
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054022
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054023
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054023
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054023
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054023
5-HT3ASerotonin receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687656
5-HT3ASerotonin receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054022