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TargetIon channels

Transient receptor potential cation channel subfamily V member 2

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

Measurements
24
Compounds
7
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

TRPV2_HUMANTRPV2Homo sapiens

Transient receptor potential cation channel subfamily V member 2

Calcium-permeable, non-selective cation channel10201375. Seems to be regulated, at least in part, by growth factors, such as IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells (By similarity)

Quoted from UniProt’s FUNCTION annotation for Q9Y5S1 (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
TRPM70.9780.0000.9000.791
TRPM20.9630.0000.9000.639
TRPM80.9290.0000.0000.928
IGF10.9220.0000.9000.255
TRPA10.8980.0000.0000.895
TRPM40.8480.0000.0000.845
TRPC10.8440.0000.0000.844
TRPM30.8250.0000.0000.822
ANK10.8130.0000.0000.813
TRPM50.7900.0000.0000.787

Where it sits in the cell

  • Plasma membrane

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane · Cytoplasm · Melanosome

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.

  • Melanocytes54.3 nCPM
  • Hepatic stellate cells51.6 nCPM
  • Pericytes39.7 nCPM
  • Hofbauer cells39.6 nCPM
  • Mast cells39.2 nCPM
  • NK-cells37.9 nCPM
  • Macrophages34.8 nCPM
  • pDCs34.1 nCPM
  • cDC30.7 nCPM
  • Vascular smooth muscle cells29.3 nCPM
  • T-cells29.2 nCPM
  • monocytes27.4 nCPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 15

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Transient receptor potential cation channel subfamily V member 2Ion channelsIC508006.10Homo sapiensCHEMBL5096628
Transient receptor potential cation channel subfamily V member 2Ion channelsIC501,5005.82Homo sapiensCHEMBL5096628
Transient receptor potential cation channel subfamily V member 2Ion channelsEC501,7005.77Homo sapiensCHEMBL5096626
Transient receptor potential cation channel subfamily V member 2Ion channelsEC504,1005.39Homo sapiensCHEMBL5096626
Transient receptor potential cation channel subfamily V member 2Ion channelsIC506,5005.19Homo sapiensCHEMBL5096628
Transient receptor potential cation channel subfamily V member 2Ion channelsEC507,3005.14Homo sapiensCHEMBL5096626
Transient receptor potential cation channel subfamily V member 2Ion channelsIC5015,7004.80Homo sapiensCHEMBL5096628
Transient receptor potential cation channel subfamily V member 2Ion channelsEC5019,0004.72Homo sapiensCHEMBL5096626
Transient receptor potential cation channel subfamily V member 2Ion channelsIC5031,0004.51Homo sapiensCHEMBL5096628
Transient receptor potential cation channel subfamily V member 2Ion channelsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL6080636
Transient receptor potential cation channel subfamily V member 2Ion channelsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL1825340
Transient receptor potential cation channel subfamily V member 2Ion channelsIC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL1825341
Transient receptor potential cation channel subfamily V member 2Ion channelsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL4143894
Transient receptor potential cation channel subfamily V member 2Ion channelsIC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL4675876
Transient receptor potential cation channel subfamily V member 2Ion channelsEC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL4675877

Other measurements 9

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
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXRattus norvegicusCHEMBL4675878
Transient receptor potential cation channel subfamily V member 2Ion channelsEmax— no normalized value— value does not convert to pXRattus norvegicusCHEMBL1825339
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096627
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096627
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096627
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096627
Transient receptor potential cation channel subfamily V member 2Ion channelsEfficacy— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096627
Transient receptor potential cation channel subfamily V member 2Ion channelsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL3112351
Transient receptor potential cation channel subfamily V member 2Ion channelsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL3112356