TargetIon channels
Transient receptor potential cation channel subfamily A member 1
Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).
- Measurements
- 77
- Compounds
- 13
- 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.
Transient receptor potential cation channel subfamily A member 1
Ligand-activated Ca(2+)-permeable, nonselective cation channel involved in pain detection and possibly also in cold perception, oxygen concentration perception, cough, itch, and inner ear function17259981,21195050,21873995,23199233,25389312,33152265. Has a relatively high Ca(2+) selectivity, with a preference for divalent over monovalent cations (Ca(2+) > Ba(2+) > Mg(2+) > NH4(+) > Li(+) > K(+)), the influx of cation into the cytoplasm leads to membrane depolarization19202543,21195050. Has a central role in the pain response to endogenous inflammatory mediators, such as bradykinin and to a diverse array of irritants. Activated by a large variety of structurally unrelated electrophilic and non-electrophilic chemical compounds, such as allylthiocyanate (AITC) from mustard oil or wasabi, cinnamaldehyde, diallyl disulfide (DADS) from garlic, and acrolein, an environmental irritant20547126,25389312,27241698,30878828. Electrophilic ligands activate TRPA1 by interacting with critical N-terminal Cys residues in a covalent manner17164327,27241698,31866091,32641835. Non-electrophile agonists bind at distinct sites in the transmembrane domain to promote channel activation33152265. Also acts as an ionotropic cannabinoid receptor by being activated by delta(9)-tetrahydrocannabinol (THC), the psychoactive component of marijuana25389312. May be a component for the mechanosensitive transduction channel of hair cells in inner ear, thereby participating in the perception of sounds (By similarity)
Quoted from UniProt’s FUNCTION annotation for O75762 (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.
Where it sits in the cell
UniProt, curated 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.
- Goblet cells74.3 nCPM
- Fibroblasts59.2 nCPM
- Myosatellite cells53.6 nCPM
- Adipocytes49.1 nCPM
- Fibro-adipogenic progenitors40.1 nCPM
- Pericytes23.7 nCPM
- Vascular smooth muscle cells22.7 nCPM
- Late primary spermatocytes12.8 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.
- urinary bladder25.9 nTPM
- stomach 19.7 nTPM
- intestine8.6 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Functional readouts 48
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
Other measurements 29
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363421 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363428 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363428 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1224917 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Ratio EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3111826 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Ratio IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112179 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Ratio IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112180 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112182 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL5389258 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL5389258 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112349 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112354 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112359 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL2091724 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4347315 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4677022 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4347309 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4347316 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4347321 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Emax | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1825342 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL4675869 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096637 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096637 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096637 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096637 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096637 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112181 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112183 |
| Transient receptor potential cation channel subfamily A member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363421 |