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TargetTrace amine receptors

Trace amine-associated receptor 1

TAAR family.

Measurements
19
Compounds
10
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

TAAR1_HUMANTAAR1Homo sapiens

Trace amine-associated receptor 1

Intracellular G protein-coupled receptor for trace amines, which recognizes endogenous amine-containing metabolites such as beta-phenylethylamine (beta-PEA), 3-iodothyronamine (T1AM), isoamylamine (IAA), cadaverine (CAD), cyclohexylamine (CHA), p-tyramine (p-TYR), trimethylamine (TMA), octopamine and tryptamine11459929,11723224,15718104,31399635,36100653,37935376,37935377,37963465,38168118. Also functions as a receptor for various drugs and psychoactive substances, such as amphetamine and methamphetamine31399635,37935376,37935377. Unresponsive to classical biogenic amines, such as epinephrine and histamine and only partially activated by dopamine and serotonin11459929,11723224. Expressed in both the central and peripheral nervous system: TAAR1 activation regulates the activity of several neurotransmitter signaling pathways by (1) decreasing the basal firing rates of the neurons involved and by (2) lowering the sensitivity of receptors to neurotransmitters37935376,37935377,37963465,38168118. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors31399635,37935376,37963465. TAAR1 is coupled with different G(i)/G(o)-, G(s)- or G(q)/G(11) classes of G alpha proteins depending on the ligand31399635,37935376,37963465. CAD-binding is coupled to G(i)/G(o) G alpha proteins and mediates inhibition of adenylate cyclase activity37935376,37963465. T1AM- or beta-PEA-binding is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity37935376,37963465. CHA- or IAA-binding is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers37935376,37963465. TMA-binding is coupled with all three G(i)/G(o)-, G(s)- or G(q)/G(11) G alpha protein subtypes37935376,37963465. Amphetamine-binding is coupled with G(s)- or G(12)/G(13) G alpha protein subtypes31399635

Quoted from UniProt’s FUNCTION annotation for Q96RJ0 (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
EPB41L4B0.8500.0000.0000.850
EPB41L4A0.8130.0000.0000.813
PTPN40.7610.0000.0000.761
TAAR90.6700.0000.4000.393
GNAS0.6490.2880.5000.095
SLC18A20.6040.0000.0000.604
SLC6A30.6010.0000.0000.601
GPR1420.5560.0000.0000.556
PTMA0.5430.0000.0000.543
RHO0.5270.0000.0000.519

Where it sits in the cell

UniProt, curated Endomembrane system · Endoplasmic reticulum 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.

  • Fallopian tube ciliated cells11.4 nCPM
  • Neutrophils6.4 nCPM
  • Neuroendocrine cells4.2 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.

  • stomach 14.7 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 11

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

TargetClassTypeValue (nM)pXOrganismAssay
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL1930653
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL4009953
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5036217
Trace amine-associated receptor 1Trace amine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2354289
Trace amine-associated receptor 1Trace amine receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2354269

Other measurements 8

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
Trace amine-associated receptor 1Trace amine receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL989986
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL989987
Trace amine-associated receptor 1Trace amine receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL5036218