Transient receptor potential cation channel subfamily V member 1
Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).
- Measurements
- 49
- Compounds
- 10
- Binding constants
- 2
- 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 V member 1
Non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli11050376,11243859,11226139,12077606. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activated by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius37117175. Upon activation, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis
Quoted from UniProt’s FUNCTION annotation for Q8NER1 (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.
| Partner | Combined | Experiment | Database | Text mining |
|---|---|---|---|---|
| CALM3 | 0.998 | 0.922 | 0.000 | 0.977 |
| TRPM8 | 0.994 | 0.000 | 0.000 | 0.994 |
| CALML3 | 0.992 | 0.259 | 0.000 | 0.990 |
| CALML5 | 0.992 | 0.259 | 0.000 | 0.990 |
| TRPA1 | 0.991 | 0.000 | 0.000 | 0.991 |
| CALML4 | 0.990 | 0.126 | 0.000 | 0.990 |
| CALML6 | 0.990 | 0.126 | 0.000 | 0.990 |
| PRKACB | 0.963 | 0.091 | 0.900 | 0.627 |
| PRKACA | 0.963 | 0.091 | 0.900 | 0.629 |
| PRKACG | 0.963 | 0.091 | 0.900 | 0.630 |
Where it sits in the cell
UniProt, curated Postsynaptic cell membrane · Cell projection, dendritic spine membrane · Cell membrane
Expression by cell type
Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Rod photoreceptor cells25.7 nCPM
- Myonuclei25.5 nCPM
- Proximal tubule cells24.5 nCPM
- Myosatellite cells21.8 nCPM
- Astrocytes19.8 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.
- liver21.8 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
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: retina 12.0, midbrain 6.6, spinal cord 6.4, pituitary gland 5.0.
Body
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 TRPV1 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
- cerebellum12.1 nTPM
- retina12.0 nTPM
- midbrain6.6 nTPM
- spinal cord6.4 nTPM
- hippocampal formation6.3 nTPM
- cerebral cortex5.8 nTPM
- amygdala5.8 nTPM
- hypothalamus5.6 nTPM
- basal ganglia5.6 nTPM
- pituitary gland5.0 nTPM
Peripheral and autonomic · 16
- liver21.8 nTPM
- small intestine7.7 nTPM
- kidney7.2 nTPM
- duodenum6.9 nTPM
- heart muscle6.8 nTPM
- pancreas6.7 nTPM
- skeletal muscle6.0 nTPM
- stomach 15.2 nTPM
- colon5.1 nTPM
- urinary bladder4.6 nTPM
- adrenal gland4.4 nTPM
- thyroid gland4.1 nTPM
- spleen3.9 nTPM
- salivary gland3.7 nTPM
- lung2.8 nTPM
- smooth muscle1.5 nTPM
Transcript is not protein. These are RNA levels for TRPV1, 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.
Equilibrium binding constants 2
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Kd | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5327516 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Kd | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112345 |
Functional readouts 25
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
Other measurements 22
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 V member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363143 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3363143 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112203 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112346 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112347 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112348 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112353 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112358 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL902593 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4477448 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4477447 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4675881 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5327514 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Emax | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1825336 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096624 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096624 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096624 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096624 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096624 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112204 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Kb | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112345 |
| Transient receptor potential cation channel subfamily V member 1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3112196 |