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TargetOther named receptors

Epidermal growth factor receptor

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
19
Compounds
11
Binding constants
7
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

EGFR_HUMANEGFRHomo sapiens

Epidermal growth factor receptor

Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses10805725,27153536,2790960,35538033. Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF12297049,15611079,17909029,20837704,27153536,2790960,7679104,8144591,9419975. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules27153536. May also activate the NF-kappa-B signaling cascade11116146. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling11602604. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin11483589. Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration20462955. Plays a role in enhancing learning and memory performance (By similarity). Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (By similarity)
Isoform 2 may act as an antagonist of EGF action
(Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry. Mediates HCV entry by promoting the formation of the CD81-CLDN1 receptor complexes that are essential for HCV entry and by enhancing membrane fusion of cells expressing HCV envelope glycoproteins

Quoted from UniProt’s FUNCTION annotation for P00533 (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
PTPN110.9990.9950.9000.991
HBEGF0.9990.8120.9000.998
NRG10.9990.7900.9000.997
TGFA0.9990.9830.9000.998
ERBB20.9990.9980.9000.983
DCN0.9990.5370.9000.986
SHC10.9990.9950.9000.994
SOS10.9990.9940.9000.942
PIK3CA0.9990.7900.9000.976
ERBB30.9990.9860.8000.984

Where it sits in the cell

  • Golgi apparatus
  • Plasma membrane
  • Cell Junctionsadditional
  • Primary ciliumadditional
  • Basal bodyadditional
  • Mid pieceadditional
  • Principal pieceadditional
  • End pieceadditional

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

UniProt, curated Cell membrane · Endoplasmic reticulum membrane · Golgi apparatus membrane · Nucleus membrane · Endosome · Endosome membrane · Nucleus · Secreted

Expression by cell type

Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Syncytiotrophoblasts1,481.8 nCPM
  • Cytotrophoblasts1,190.3 nCPM
  • Fibro-adipogenic progenitors1,097.7 nCPM
  • Respiratory basal cells935.5 nCPM
  • Myosatellite cells789.2 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.

  • placenta61.8 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

032 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of EGFR transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • cerebral cortex11.5 nTPM
  • retina9.4 nTPM
  • basal ganglia8.5 nTPM
  • amygdala6.1 nTPM
  • midbrain5.3 nTPM
  • hippocampal formation3.8 nTPM
  • hypothalamus3.3 nTPM
  • cerebellum2.7 nTPM
  • pituitary gland2.6 nTPM
  • spinal cord1.7 nTPM

Peripheral and autonomic · 16

  • liver32.2 nTPM
  • salivary gland20.7 nTPM
  • thyroid gland18.7 nTPM
  • pancreas14.6 nTPM
  • lung14.1 nTPM
  • urinary bladder13.7 nTPM
  • colon11.4 nTPM
  • kidney10.8 nTPM
  • adrenal gland10.6 nTPM
  • skeletal muscle10.2 nTPM
  • stomach 110.1 nTPM
  • small intestine9.1 nTPM
  • smooth muscle8.4 nTPM
  • heart muscle6.8 nTPM
  • duodenum5.3 nTPM
  • spleen4.7 nTPM

Transcript is not protein. These are RNA levels for EGFR, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 7

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203

Functional readouts 12

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

TargetClassTypeValue (nM)pXOrganismAssay
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291787
Epidermal growth factor receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291787
Epidermal growth factor receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291787
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL3778248
Epidermal growth factor receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291787
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203
Epidermal growth factor receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909203