Calcium-activated potassium channel subunit alpha-1
Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).
- Measurements
- 15
- Compounds
- 1
- 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.
Calcium-activated potassium channel subunit alpha-1
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+)14523450,29330545,31152168. It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX). Possibly induces sleep when activated by melatonin and through melatonin receptor MTNR1A-dependent dissociation of G-beta and G-gamma subunits, leading to increased sensitivity to Ca(2+) and reduced synaptic transmission32958651
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+)
Quoted from UniProt’s FUNCTION annotation for Q12791 (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 |
|---|---|---|---|---|
| KCNMB1 | 0.999 | 0.345 | 0.900 | 0.990 |
| KCNMB4 | 0.998 | 0.602 | 0.900 | 0.953 |
| KCNMB3 | 0.995 | 0.000 | 0.900 | 0.955 |
| KCNN4 | 0.981 | 0.000 | 0.900 | 0.826 |
| KCNN1 | 0.980 | 0.000 | 0.900 | 0.808 |
| LRRC26 | 0.970 | 0.292 | 0.000 | 0.960 |
| KCNMB2 | 0.970 | 0.292 | 0.900 | 0.620 |
| KCNN2 | 0.969 | 0.000 | 0.900 | 0.708 |
| KCNN3 | 0.966 | 0.000 | 0.900 | 0.672 |
| PRKACG | 0.944 | 0.128 | 0.900 | 0.411 |
Where it sits in the cell
UniProt, curated Cell membrane
Expression by cell type
Single cell type RNA, the 9 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Retinal bipolar cells1,789.6 nCPM
- Salivary ionocytes1,694.7 nCPM
- Salivary acinar cells1,516.9 nCPM
- Ependymal cells1,320.9 nCPM
- Myonuclei1,079.6 nCPM
- Lacrimal acinar cells1,058 nCPM
- Oligodendrocyte progenitor cells1,022.8 nCPM
- Kupffer cells870.1 nCPM
- Neutrophils829.9 nCPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Functional readouts 1
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638698 |
Other measurements 14
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 |
|---|---|---|---|---|---|---|
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638696 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638697 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638699 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638700 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638701 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638702 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638703 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638704 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638705 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638706 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638707 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638708 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | TIME | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638709 |
| Calcium-activated potassium channel subunit alpha-1 | Ion channels | Time | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5638710 |