Transient receptor potential cation channel subfamily M member 8
Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).
- Measurements
- 54
- Compounds
- 13
- Binding constants
- 1
- 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 M member 8
Non-selective ion channel permeable to monovalent and divalent cations, including Na(+), K(+), and Ca(2+), with higher permeability for Ca(2+). Activated by multiple factors, such as temperature, voltage, pressure, and changes in osmolality. Activated by cool temperatures (<23-28 degrees Celsius) and by chemical ligands evoking a sensation of coolness, such as menthol and icilin therefore plays a central role in the detection of environmental cold temperatures15306801,15852009,16174775,25559186,37857704. TRPM8 is a voltage-dependent channel; its activation by cold or chemical ligands shifts its voltage thresholds towards physiological membrane potentials, leading to the opening of the channel15306801. In addition to its critical role in temperature sensing, regulates basal tear secretion by sensing evaporation-induced cooling and changes in osmolality (By similarity). May play a role in prostate cancer cell migration16174775,25559186
Negatively regulates menthol- and cold-induced channel activity by stabilizing the closed state of the channel
Negatively regulates menthol- and cold-induced channel activity by stabilizing the closed state of the channel
Quoted from UniProt’s FUNCTION annotation for Q7Z2W7 (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 · Membrane raft · Endoplasmic reticulum 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.
- Prostatic glandular cells178.5 nCPM
- Prostatic club cells104.9 nCPM
- Hepatocytes64.2 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.
- prostate75.4 nTPM
- liver29.4 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 1
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 M member 8 | Ion channels | Kd | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112360 |
Functional readouts 29
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
Other measurements 24
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 M member 8 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3363141 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3363141 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112188 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3111827 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3111828 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Ratio IC50 | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3111829 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Ratio IC50 | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3111830 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112184 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112185 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112186 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112193 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112194 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112197 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112198 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112199 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112200 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112201 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112202 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112352 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Activity | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112357 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL2091727 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Kb | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112360 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112360 |
| Transient receptor potential cation channel subfamily M member 8 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL3112195 |