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TargetIon channels

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.

Protein

KCMA1_HUMANKCNMA1Homo sapiens

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.

PartnerCombinedExperimentDatabaseText mining
KCNMB10.9990.3450.9000.990
KCNMB40.9980.6020.9000.953
KCNMB30.9950.0000.9000.955
KCNN40.9810.0000.9000.826
KCNN10.9800.0000.9000.808
LRRC260.9700.2920.0000.960
KCNMB20.9700.2920.9000.620
KCNN20.9690.0000.9000.708
KCNN30.9660.0000.9000.672
PRKACG0.9440.1280.9000.411

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.

TargetClassTypeValue (nM)pXOrganismAssay
Calcium-activated potassium channel subunit alpha-1Ion channelsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638698

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.

TargetClassTypeValue (nM)pXOrganismAssay
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638696
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638697
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638699
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638700
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638701
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638702
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638703
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638704
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638705
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638706
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638707
Calcium-activated potassium channel subunit alpha-1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638708
Calcium-activated potassium channel subunit alpha-1Ion channelsTIME— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638709
Calcium-activated potassium channel subunit alpha-1Ion channelsTime— no normalized value— value does not convert to pXHomo sapiensCHEMBL5638710