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Target Report Card

Target Name and Classification

Target ID CHEMBL203
Target Type SINGLE PROTEIN
Preferred Name Epidermal growth factor receptor erbB1
Synonyms EGFR | ERBB | ERBB1 | Epidermal growth factor receptor | HER1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase erbB-1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase egfr family

Target Components

Component Description Relationship Accession
Epidermal growth factor receptor SINGLE PROTEIN P00533

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2363049 Epidermal growth factor receptor PROTEIN FAMILY
CHEMBL3137284 MER intracellular domain/EGFR extracellular domain chimera CHIMERIC PROTEIN
CHEMBL2111431 Epidermal growth factor receptor and ErbB2 (HER1 and HER2) PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL939 GEFITINIB Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL1079742 ERLOTINIB HYDROCHLORIDE Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL1201179 LAPATINIB DITOSYLATE Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL1201577 CETUXIMAB Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL1201827 PANITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL1743047 NECITUMUMAB Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL2105712 AFATINIB DIMALEATE Epidermal growth factor receptor erbB1 inhibitor 4 DailyMed
CHEMBL3353410 OSIMERTINIB Epidermal growth factor receptor erbB1 inhibitor 4 PubMed PubMed
CHEMBL180022 NERATINIB Epidermal growth factor receptor erbB1 inhibitor 3 PubMed PubMed
CHEMBL545315 CANERTINIB DIHYDROCHLORIDE Epidermal growth factor receptor erbB1 inhibitor 3 PubMed PubMed
CHEMBL2105719 DACOMITINIB HYDRATE Epidermal growth factor receptor erbB1 inhibitor 3 Other PubMed
CHEMBL2107861 ZALUTUMUMAB Epidermal growth factor receptor erbB1 antagonist 3 PubMed
CHEMBL3545235 Simotinib Epidermal growth factor receptor erbB1 inhibitor 3 PubMed PubMed
CHEMBL3545308 ROCILETINIB Epidermal growth factor receptor erbB1 inhibitor 3 PubMed
CHEMBL3545311 BRIGATINIB Epidermal growth factor receptor erbB1 inhibitor 3 Other Other PubMed
CHEMBL587723 AEE-788 Epidermal growth factor receptor erbB1 inhibitor 2 PubMed
CHEMBL607707 PELITINIB Epidermal growth factor receptor erbB1 inhibitor 2 PubMed PubMed
CHEMBL2103842 VARLITINIB Epidermal growth factor receptor erbB1 inhibitor 2 Other Other
CHEMBL2108038 MATUZUMAB Epidermal growth factor receptor erbB1 inhibitor 2 PubMed
CHEMBL2109390 mAb-425 Epidermal growth factor receptor erbB1 inhibitor 2 PubMed
CHEMBL2109391 MDX-447 Epidermal growth factor receptor erbB1 other 2 PubMed
CHEMBL2109393 RG-7160 Epidermal growth factor receptor erbB1 antagonist 2 PubMed
CHEMBL2408045 SAPITINIB Epidermal growth factor receptor erbB1 inhibitor 2 PubMed PubMed
CHEMBL3544956 Pyrotinib Epidermal growth factor receptor erbB1 inhibitor 2 Other
CHEMBL3544983 TESEVATINIB Epidermal growth factor receptor erbB1 inhibitor 2 Other PubMed PubMed
CHEMBL3545234 EGF816 Epidermal growth factor receptor erbB1 inhibitor 2 ClinicalTrials DOI Other
CHEMBL3545396 BMS-690514 Epidermal growth factor receptor erbB1 inhibitor 2 PubMed PubMed
CHEMBL3545430 HM-61713 Epidermal growth factor receptor erbB1 inhibitor 2 Other PubMed
CHEMBL422872 AZD-4769 Epidermal growth factor receptor erbB1 inhibitor 1 Other
CHEMBL258940 FALNIDAMOL Epidermal growth factor receptor erbB1 inhibitor 1 PubMed PubMed
CHEMBL598797 CUDC-101 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed
CHEMBL1614725 TAK-285 Epidermal growth factor receptor erbB1 inhibitor 1 DOI PubMed
CHEMBL1645462 AC-480 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed PubMed
CHEMBL1963502 PKI-166 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed
CHEMBL2029988 CEP-32496 Epidermal growth factor receptor erbB1 inhibitor 1 Other
CHEMBL3545002 MP-412 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed PubMed
CHEMBL3545088 Puquitinib Epidermal growth factor receptor erbB1 inhibitor 1 DOI PubMed PubMed
CHEMBL3545121 Epitinib Epidermal growth factor receptor erbB1 inhibitor 1 ClinicalTrials Other
CHEMBL3545133 JNJ-26483327 Epidermal growth factor receptor erbB1 inhibitor 1 DOI PubMed
CHEMBL3545180 Theliatinib Epidermal growth factor receptor erbB1 inhibitor 1 ClinicalTrials Other
CHEMBL3545196 PD-0166285 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed
CHEMBL3545200 S-222611 Epidermal growth factor receptor erbB1 inhibitor 1 PubMed PubMed
CHEMBL3545244 Allitinib Epidermal growth factor receptor erbB1 inhibitor 1 PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000146648
Ensembl ENSG00000146648
GO Cellular Component GO:0000139 (Golgi membrane)
GO:0005576 (extracellular region)
GO:0005615 (extracellular space)
GO:0005622 (intracellular)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005768 (endosome)
GO:0005783 (endoplasmic reticulum)
GO:0005789 (endoplasmic reticulum membrane)
GO:0005794 (Golgi apparatus)
GO:0005886 (plasma membrane)
GO:0005913 (cell-cell adherens junction)
GO:0005925 (focal adhesion)
GO:0009986 (cell surface)
GO:0010008 (endosome membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0030122 (AP-2 adaptor complex)
GO:0030139 (endocytic vesicle)
GO:0031901 (early endosome membrane)
GO:0031965 (nuclear membrane)
GO:0043235 (receptor complex)
GO:0045121 (membrane raft)
GO:0048471 (perinuclear region of cytoplasm)
GO:0070435 (Shc-EGFR complex)
GO:0097489 (multivesicular body, internal vesicle lumen)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0003682 (chromatin binding)
GO:0003690 (double-stranded DNA binding)
GO:0004672 (protein kinase activity)
GO:0004709 (MAP kinase kinase kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0004871 (signal transducer activity)
GO:0004888 (transmembrane signaling receptor activity)
GO:0005006 (epidermal growth factor-activated receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019899 (enzyme binding)
GO:0019903 (protein phosphatase binding)
GO:0030235 (nitric-oxide synthase regulator activity)
GO:0031625 (ubiquitin protein ligase binding)
GO:0042802 (identical protein binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO:0046982 (protein heterodimerization activity)
GO:0051015 (actin filament binding)
GO:0098641 (cadherin binding involved in cell-cell adhesion)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000186 (activation of MAPKK activity)
GO:0000902 (cell morphogenesis)
GO:0001503 (ossification)
GO:0001892 (embryonic placenta development)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0001942 (hair follicle development)
GO:0006468 (protein phosphorylation)
GO:0006950 (response to stress)
GO:0007165 (signal transduction)
GO:0007166 (cell surface receptor signaling pathway)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0007202 (activation of phospholipase C activity)
GO:0007275 (multicellular organism development)
GO:0007435 (salivary gland morphogenesis)
GO:0007611 (learning or memory)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008544 (epidermis development)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016337 (single organismal cell-cell adhesion)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021795 (cerebral cortex cell migration)
GO:0030307 (positive regulation of cell growth)
GO:0030335 (positive regulation of cell migration)
GO:0031659 (positive regulation of cyclin-dependent protein serine/threonine kinase activity involved in G1/S transition of mitotic cell cycle)
GO:0035413 (positive regulation of catenin import into nucleus)
GO:0038128 (ERBB2 signaling pathway)
GO:0042059 (negative regulation of epidermal growth factor receptor signaling pathway)
GO:0042127 (regulation of cell proliferation)
GO:0042177 (negative regulation of protein catabolic process)
GO:0042327 (positive regulation of phosphorylation)
GO:0043006 (activation of phospholipase A2 activity by calcium-mediated signaling)
GO:0043066 (negative regulation of apoptotic process)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0043547 (positive regulation of GTPase activity)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045739 (positive regulation of DNA repair)
GO:0045740 (positive regulation of DNA replication)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048146 (positive regulation of fibroblast proliferation)
GO:0048546 (digestive tract morphogenesis)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0050730 (regulation of peptidyl-tyrosine phosphorylation)
GO:0050999 (regulation of nitric-oxide synthase activity)
GO:0051205 (protein insertion into membrane)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0060571 (morphogenesis of an epithelial fold)
GO:0061029 (eyelid development in camera-type eye)
GO:0070141 (response to UV-A)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071230 (cellular response to amino acid stimulus)
GO:0071364 (cellular response to epidermal growth factor stimulus)
GO:0071392 (cellular response to estradiol stimulus)
GO:1903800 (positive regulation of production of miRNAs involved in gene silencing by miRNA)
GO:2000145 (regulation of cell motility)
Wikipedia Epidermal_growth_factor_receptor

Target Cross References - Protein

canSAR P00533
CGD Acute myeloid leukemia, familial; Lung cancer, familial, susceptibilty to
Human Protein Atlas ENSG00000146648
IntAct P00533
Guide to Pharmacology 1797
MICAD NBK23179 (Epidermal growth factor receptor)
NBK23211 (Epidermal growth factor receptor)
NBK23370 (Epidermal growth factor receptor (EGFR, HER1/erbB-1))
NBK23376 (Epidermal growth factor receptor (EGFR))
Open Targets ENSG00000146648
PharmGKB PA7360
Pharos P00533 (Tclin)
Reactome R-HSA-1227986 (Signaling by ERBB2.)
R-HSA-1236382 (Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants.)
R-HSA-1236394 (Signaling by ERBB4.)
R-HSA-1250196 (SHC1 events in ERBB2 signaling.)
R-HSA-1251932 (PLCG1 events in ERBB2 signaling.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-177929 (Signaling by EGFR.)
R-HSA-179812 (GRB2 events in EGFR signaling.)
R-HSA-180292 (GAB1 signalosome.)
R-HSA-180336 (SHC1 events in EGFR signaling.)
R-HSA-182971 (EGFR downregulation.)
R-HSA-1963640 (GRB2 events in ERBB2 signaling.)
R-HSA-1963642 (PI3K events in ERBB2 signaling.)
R-HSA-212718 (EGFR interacts with phospholipase C-gamma.)
R-HSA-2179392 (EGFR Transactivation by Gastrin.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-445144 (Signal transduction by L1.)
R-HSA-5637810 (Constitutive Signaling by EGFRvIII.)
R-HSA-5638303 (Inhibition of Signaling by Overexpressed EGFR.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6785631 (ERBB2 Regulates Cell Motility.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8847993 (ERBB2 Activates PTK6 Signaling.)
R-HSA-8856825 (Cargo recognition for clathrin-mediated endocytosis.)
R-HSA-8856828 (Clathrin-mediated endocytosis.)
R-HSA-8857538 (PTK6 promotes HIF1A stabilization.)
R-HSA-8863795 (Downregulation of ERBB2 signaling.)
R-HSA-8866910 (TFAP2 (AP-2) family regulates transcription of growth factors and their receptors.)
UniProt O00688 O00732 P00533 P06268 Q14225 Q68GS5 Q92795 Q9BZS2 Q9GZX1 Q9H2C9 Q9H3C9 Q9UMD7 Q9UMD8 Q9UMG5

Target Cross References - Domain

InterPro IPR000494 (Rcpt_L-dom.)
IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR006211 (Furin-like_Cys-rich_dom.)
IPR006212 (Furin_repeat.)
IPR008266 (Tyr_kinase_AS.)
IPR009030 (Growth_fac_rcpt_.)
IPR011009 (Kinase-like_dom.)
IPR016245 (Tyr_kinase_EGF/ERB/XmrK_rcpt.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR032675 (L_dom-like.)
IPR032778 (GF_recep_IV.)
Pfam PF00757 (Furin-like)
PF01030 (Recep_L_domain)
PF07714 (Pkinase_Tyr)
PF14843 (GF_recep_IV)

Target Cross References - Structure

PDBe 1IVO 1M14 1M17 1MOX 1NQL 1XKK 1YY9 2EB2 2EB3 2GS2 2GS6 2GS7 2ITN 2ITO 2ITP 2ITQ 2ITT 2ITU 2ITV 2ITW 2ITX 2ITY 2ITZ 2J5E More...
CREDO 1IVO 1M14 1M17 1MOX 1NQL 1XKK 1YY9 2EB2 2EB3 2GS2 2GS6 2GS7 2ITN 2ITO 2ITP 2ITQ 2ITT 2ITU 2ITV 2ITW 2ITX 2ITY 2ITZ 2J5E More...
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