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TargetIon channels

Calcium release-activated calcium channel protein 1

Voltage- and ligand-gated channels, including the TRP family and hERG (KCNH2).

Measurements
5
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

ORAI1_HUMANORAI1Homo sapiens

Calcium release-activated calcium channel protein 1

Pore-forming subunit of two major inward rectifying Ca(2+) channels at the plasma membrane: Ca(2+) release-activated Ca(2+) (CRAC) channels and arachidonate-regulated Ca(2+)-selective (ARC) channels (Probable)16645049,16733527,16807233,16921383,19249086,19706554,23307288,26956484,28219928. Assembles with ORAI2 and ORAI3 to form hexameric CRAC channels that mediate Ca(2+) influx upon depletion of endoplasmic reticulum Ca(2+) store and channel activation by Ca(2+) sensor STIM1, a process known as store-operated Ca(2+) entry (SOCE). Various pore subunit combinations may account for distinct CRAC channel spatiotemporal and cell-type specific dynamics. ORAI1 mainly contributes to the generation of Ca(2+) plateaus involved in sustained Ca(2+) entry and is dispensable for cytosolic Ca(2+) oscillations, whereas ORAI2 and ORAI3 generate oscillatory patterns. CRAC channels assemble in Ca(2+) signaling microdomains where Ca(2+) influx is coupled to calmodulin and calcineurin signaling and activation of NFAT transcription factors recruited to ORAI1 via AKAP5. Activates NFATC2/NFAT1 and NFATC3/NFAT4-mediated transcriptional responses. CRAC channels are the main pathway for Ca(2+) influx in T cells and promote the immune response to pathogens by activating NFAT-dependent cytokine and chemokine transcription16582901,17442569,19182790,20354224,22641696,26221052,32415068,33941685. Assembles with ORAI3 to form channels that mediate store-independent Ca(2+) influx in response to inflammatory metabolites arachidonate or its derivative leukotriene C4, termed ARC and LRC channels respectively19622606,32415068. Plays a prominent role in Ca(2+) influx at the basolateral membrane of mammary epithelial cells independently of the Ca(2+) content of endoplasmic reticulum or Golgi stores. May mediate transepithelial transport of large quantities of Ca(2+) for milk secretion (By similarity)20887894
Pore-forming subunit of both CRAC and ARC channels. Couples Ca(2+) influx to NFAT-mediated transcriptional responses
Pore-forming subunit of CRAC channels exclusively

Quoted from UniProt’s FUNCTION annotation for Q96D31 (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
STIM10.9990.9330.7000.999
STIM20.9990.4910.9000.999
ORAI30.9980.5410.9000.972
TRPC10.9960.2920.0000.995
ORAI20.9940.0000.9000.947
CALM30.9790.9000.0000.807
CALM10.9530.9000.5000.143
TRPC30.9410.2920.0000.921
PRKACA0.9210.0000.9000.233
PRKACB0.9200.0000.9000.233

Where it sits in the cell

UniProt, curated Cell membrane · Basolateral cell membrane

Expression by cell type

Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Choroid plexus epithelial cells10.3 nCPM
  • Microglia6.4 nCPM
  • Oligodendrocyte progenitor cells5.9 nCPM
  • Renal collecting duct intercalated cells5.8 nCPM
  • Papillary tip epithelial cells4.2 nCPM
  • Renal collecting duct principal cells3.7 nCPM
  • NK-cells3.3 nCPM
  • Renal connecting tubule cells3 nCPM
  • Platelets2.8 nCPM
  • Oligodendrocytes2.6 nCPM
  • Bergmann glia2.4 nCPM
  • Loop of henle epithelial cells2.4 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.

  • choroid plexus63.1 nTPM
  • skeletal muscle57.2 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 5

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 release-activated calcium channel protein 1Ion channelsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4477452
Calcium release-activated calcium channel protein 1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4477451
Calcium release-activated calcium channel protein 1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4477449
Calcium release-activated calcium channel protein 1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4477446
Calcium release-activated calcium channel protein 1Ion channelsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4477450