Skip to content
TargetUnclassified

P2X purinoceptor 7

Matched no rule. Shown as-is rather than assigned a class by guesswork. Values below are reported as measured; because this is not a molecular target, they are not treated as affinities anywhere on this site.

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

P2RX7_HUMANP2RX7Homo sapiens

P2X purinoceptor 7

ATP-gated nonselective transmembrane cation channel that requires high millimolar concentrations of ATP for activation17483156,25281740,9038151. Upon ATP binding, it rapidly opens to allow the influx of small cations Na(+) and Ca(2+), and the K(+) efflux17483156,20453110,28235784,39262850. Also has the ability to form a large pore in the cell membrane, allowing the passage of large cationic molecules17483156. In microglia, may mediate NADPH transport across the plasma membrane39142135. In immune cells, P2RX7 acts as a molecular sensor in pathological inflammatory states by detecting and responding to high local concentrations of extracellar ATP. In microglial cells, P2RX7 activation leads to the release of pro-inflammatory cytokines, such as IL-1beta and IL-18, through the activation of the NLRP3 inflammasome and caspase-126877061. Cooperates with KCNK6 to activate NLRP3 inflammasome (By similarity). Activates death pathways leading to apoptosis and autophagy21821797,23303206,28326637. Activates death pathways leading to pyroptosis (By similarity)
Shows ion channel activity but no macropore function
Non-functional channel
Non-functional channel

Quoted from UniProt’s FUNCTION annotation for Q99572 (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
P2RX40.9950.0000.9000.946
PANX10.9950.0000.7000.985
P2RX10.9870.0000.9000.872
P2RX30.9790.0000.9000.798
P2RX60.9490.0000.9000.478
P2RX50.9480.0000.9000.469
GRIN2A0.9090.0000.9000.115
GRIN10.9090.0000.9000.090
GRIN2C0.9060.0000.9000.090
GRIN2D0.9020.0000.9000.049

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 7 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Oligodendrocytes350.2 nCPM
  • Melanocytes194.7 nCPM
  • Oligodendrocyte progenitor cells187.4 nCPM
  • Microglia151.5 nCPM
  • cDC108.6 nCPM
  • Macrophages84.3 nCPM
  • monocytes81.3 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.

  • brain16.8 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
P2X purinoceptor 7UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620831
P2X purinoceptor 7UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620832
P2X purinoceptor 7UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620833
P2X purinoceptor 7UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620834
P2X purinoceptor 7UnclassifiedActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4620835