epidermal growth factor receptor

Target id: 1797

Nomenclature: epidermal growth factor receptor

Abbreviated Name: EGFR

Family: Type I RTKs: ErbB (epidermal growth factor) receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1210 7p12 EGFR epidermal growth factor receptor
Mouse 1 1210 11 A1-A4 Egfr epidermal growth factor receptor
Rat - 1209 14q22 Egfr epidermal growth factor receptor
Previous and Unofficial Names
HER1
avian erythroblastic leukemia viral (v-erbB) oncogene homolog
Wa5
ERBB1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  EGFR kinase domain complexed with a quinazoline inhibitor- GW572016
PDB Id:  1XKK
Ligand:  lapatinib
Resolution:  2.4Å
Species:  Human
References:  30
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains.
PDB Id:  1IVO
Resolution:  3.3Å
Species:  Human
References:  20
Enzyme Reaction
EC Number: 2.7.10.1
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
gefitinib Hs Inhibition 8.3 pKi 27
pKi 8.3 (Ki 5.5x10-9 M) [27]
AG 9 Hs Inhibition <3.4 pKi 13
pKi <3.4 (Ki >4x10-4 M) [13]
Description: Measuring phosphorylation of the EGFR exogenous substrate polyGAT [poly(Glu6Ala3Tyr)]
compound 56 [PMID:8568816] Hs Inhibition 11.22 pIC50 5
pIC50 11.22 (IC50 6x10-12 M) [5]
BPIQ-I Hs Inhibition 10.6 pIC50 23
pIC50 10.6 (IC50 2.5x10-11 M) [23]
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibition 9.52 pIC50 18
pIC50 9.52 (IC50 3x10-10 M) [18]
PD 174265 Hs Inhibition 9.35 pIC50 10
pIC50 9.35 (IC50 4.5x10-10 M) [10]
erlotinib Hs Inhibition 9.0 pIC50 31
pIC50 9.0 (IC50 1x10-9 M) [31]
AEE788 Hs Inhibition 8.7 pIC50 26
pIC50 8.7 (IC50 2x10-9 M) [26]
pelitinib Hs Inhibition 7.84 – 9.22 pIC50 27-28
pIC50 7.84 – 9.22 (IC50 1.45x10-8 – 6x10-10 M) [27-28]
falnidamol Hs Inhibition 8.52 pIC50 25
pIC50 8.52 (IC50 3x10-9 M) [25]
PKI166 Hs Inhibition 8.43 pIC50 16
pIC50 8.43 (IC50 3.7x10-9 M) [16]
sapitinib Hs Inhibition 8.4 pIC50 4
pIC50 8.4 (IC50 4x10-9 M) [4]
JAK3 inhibitor II Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 4x10-9 M) [6]
BMS-690514 Hs Inhibition 8.3 pIC50 19
pIC50 8.3 (IC50 5x10-9 M) [19]
dacomitinib Hs Inhibition 8.22 pIC50 3
pIC50 8.22 (IC50 6x10-9 M) [3]
lapatinib Hs Inhibition 8.0 pIC50 24
pIC50 8.0 (IC50 1.02x10-8 M) [24]
afatinib Hs Inhibition 7.96 pIC50 7
pIC50 7.96 (IC50 1.1x10-8 M) [7]
PD 158780 Hs Inhibition 7.82 pIC50 22
pIC50 7.82 (IC50 1.5x10-8 M) [22]
Description: Inhibition of EGFR autophosphorylation
EGFR inhibitor Hs Inhibition 7.68 pIC50 9
pIC50 7.68 (IC50 2.1x10-8 M) [9]
BMS-599626 Hs Inhibition 7.49 pIC50 12
pIC50 7.49 (IC50 3.2x10-8 M) [12]
icotinib Hs Inhibition 7.35 pIC50 14
pIC50 7.35 (IC50 4.5x10-8 M) [14]
Description: Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells.
neratinib Hs Inhibition 7.04 pIC50 21
pIC50 7.04 (IC50 9.2x10-8 M) [21]
Description: Inhibition of autophosphorylation of the cytoplasmic domain of the RTK in a cell free system.
AP26113 Hs Inhibition 6.89 pIC50 17
pIC50 6.89 (IC50 1.29x10-7 M) [17]
AZD9291 Hs Inhibition 5.7 – 6.3 pIC50 2
pIC50 5.7 – 6.3 (IC50 2x10-6 – 5x10-7 M) [2]
orantinib  Hs Inhibition <4.0 pIC50 15
pIC50 <4.0 (IC50 >1x10-4 M) [15]
Inhibitor Comments
AZD9291 is much more potent at mutant EGFRs, with IC50 values <100nM [2].
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
cetuximab Hs Inhibition - -
panitumumab Hs Inhibition - -
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 8,29

Key to terms and symbols Click column headers to sort
Target used in screen: EGFR
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.72 pKd
afatinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.17 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
neratinib Hs Inhibitor Inhibition 8.96 pKd
lapatinib Hs Inhibitor Inhibition 8.62 pKd
vandetanib Hs Inhibitor Inhibition 8.02 pKd
bosutinib Hs Inhibitor Inhibition 7.46 pKd
dasatinib Hs Inhibitor Inhibition 6.92 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.74 pKd
Target used in screen: EGFR(E746-A750del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.96 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.32 pKd
gefitinib Hs Inhibitor Inhibition 9.27 pKd
neratinib Hs Inhibitor Inhibition 8.64 pKd
vandetanib Hs Inhibitor Inhibition 8.32 pKd
lapatinib Hs Inhibitor Inhibition 8.07 pKd
bosutinib Hs Inhibitor Inhibition 7.74 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.09 pKd
staurosporine Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(G719C)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 10.0 pKd
canertinib Hs Inhibitor Inhibition 9.89 pKd
neratinib Hs Inhibitor Inhibition 9.43 pKd
erlotinib Hs Inhibitor Inhibition 9.07 pKd
lapatinib Hs Inhibitor Inhibition 9.04 pKd
gefitinib Hs Inhibitor Inhibition 8.7 pKd
vandetanib Hs Inhibitor Inhibition 8.02 pKd
bosutinib Hs Inhibitor Inhibition 7.01 pKd
barasertib-hQPA Hs Inhibitor Inhibition 6.92 pKd
foretinib Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(G719S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.72 pKd
canertinib Hs Inhibitor Inhibition 9.72 pKd
erlotinib Hs Inhibitor Inhibition 9.28 pKd
neratinib Hs Inhibitor Inhibition 9.04 pKd
gefitinib Hs Inhibitor Inhibition 8.96 pKd
lapatinib Hs Inhibitor Inhibition 8.68 pKd
vandetanib Hs Inhibitor Inhibition 8.23 pKd
bosutinib Hs Inhibitor Inhibition 7.59 pKd
dasatinib Hs Inhibitor Inhibition 7.1 pKd
cediranib Hs Inhibitor Inhibition 7.08 pKd
Target used in screen: EGFR(L747-E749del, A750P)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.85 pKd
canertinib Hs Inhibitor Inhibition 9.77 pKd
erlotinib Hs Inhibitor Inhibition 9.28 pKd
gefitinib Hs Inhibitor Inhibition 9.24 pKd
neratinib Hs Inhibitor Inhibition 9.21 pKd
lapatinib Hs Inhibitor Inhibition 8.66 pKd
vandetanib Hs Inhibitor Inhibition 7.92 pKd
bosutinib Hs Inhibitor Inhibition 7.54 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.14 pKd
staurosporine Hs Inhibitor Inhibition 7.02 pKd
Target used in screen: EGFR(L747-S752del, P753S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.92 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.33 pKd
gefitinib Hs Inhibitor Inhibition 9.24 pKd
neratinib Hs Inhibitor Inhibition 9.03 pKd
lapatinib Hs Inhibitor Inhibition 8.41 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.42 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.96 pKd
foretinib Hs Inhibitor Inhibition 6.68 pKd
Target used in screen: EGFR(L747-T751del,Sins)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.92 pKd
canertinib Hs Inhibitor Inhibition 9.59 pKd
erlotinib Hs Inhibitor Inhibition 9.46 pKd
gefitinib Hs Inhibitor Inhibition 9.28 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.46 pKd
vandetanib Hs Inhibitor Inhibition 8.05 pKd
bosutinib Hs Inhibitor Inhibition 7.52 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd
foretinib Hs Inhibitor Inhibition 6.8 pKd
Target used in screen: EGFR(L858R)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.7 pKd
canertinib Hs Inhibitor Inhibition 9.62 pKd
neratinib Hs Inhibitor Inhibition 9.17 pKd
gefitinib Hs Inhibitor Inhibition 9.03 pKd
erlotinib Hs Inhibitor Inhibition 9.01 pKd
lapatinib Hs Inhibitor Inhibition 8.55 pKd
vandetanib Hs Inhibitor Inhibition 8.06 pKd
bosutinib Hs Inhibitor Inhibition 7.64 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.34 pKd
dasatinib Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: EGFR(L858R,T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.55 pKd
staurosporine Hs Inhibitor Inhibition 9.46 pKd
afatinib Hs Inhibitor Inhibition 8.96 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.47 pKd
lestaurtinib Hs Inhibitor Inhibition 8.11 pKd
midostaurin Hs Inhibitor Inhibition 8.06 pKd
neratinib Hs Inhibitor Inhibition 7.57 pKd
R406 Hs Inhibitor Inhibition 7.21 pKd
gefitinib Hs Inhibitor Inhibition 6.85 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.82 pKd
Target used in screen: EGFR(L861Q)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.66 pKd
afatinib Hs Inhibitor Inhibition 9.64 pKd
neratinib Hs Inhibitor Inhibition 9.43 pKd
lapatinib Hs Inhibitor Inhibition 8.92 pKd
erlotinib Hs Inhibitor Inhibition 8.92 pKd
gefitinib Hs Inhibitor Inhibition 8.85 pKd
vandetanib Hs Inhibitor Inhibition 7.96 pKd
bosutinib Hs Inhibitor Inhibition 7.15 pKd
foretinib Hs Inhibitor Inhibition 7.07 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.01 pKd
Target used in screen: EGFR(S752-I759del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.85 pKd
canertinib Hs Inhibitor Inhibition 9.72 pKd
neratinib Hs Inhibitor Inhibition 9.2 pKd
gefitinib Hs Inhibitor Inhibition 9.01 pKd
erlotinib Hs Inhibitor Inhibition 8.8 pKd
lapatinib Hs Inhibitor Inhibition 8.38 pKd
vandetanib Hs Inhibitor Inhibition 7.92 pKd
bosutinib Hs Inhibitor Inhibition 6.96 pKd
staurosporine Hs Inhibitor Inhibition 6.54 pKd
dasatinib Hs Inhibitor Inhibition 6.48 pKd
Target used in screen: EGFR(T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 10.0 pKd
afatinib Hs Inhibitor Inhibition 9.21 pKd
staurosporine Hs Inhibitor Inhibition 9.11 pKd
neratinib Hs Inhibitor Inhibition 8.82 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.15 pKd
midostaurin Hs Inhibitor Inhibition 8.01 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
gefitinib Hs Inhibitor Inhibition 7.4 pKd
R406 Hs Inhibitor Inhibition 7.14 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.13 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,11

Key to terms and symbols Click column headers to sort
Target used in screen: EGFR/EGFR
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
AG1478 Hs Inhibitor Inhibition 0.7 -5.0 -3.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 1.2 -4.0 -3.0
PD 158780 Hs Inhibitor Inhibition 2.0 -2.0 -3.0
compound 56 [PMID:8568816] Hs Inhibitor Inhibition 2.0 -5.0 -4.0
PD 174265 Hs Inhibitor Inhibition 2.2 -3.0 -3.0
JAK3 inhibitor II Hs Inhibitor Inhibition 2.2 -4.0 -3.0
gefitinib Hs Inhibitor Inhibition 3.0
BPIQ-I Hs Inhibitor Inhibition 3.6 -4.0 -3.0
bosutinib Hs Inhibitor Inhibition 3.8
erlotinib Hs Inhibitor Inhibition 4.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Lung cancer; Giant cell glioblastoma
OMIM:  211980
Orphanet:  251579
Disease:  Lung cancer; Gliosarcoma
OMIM:  211980
Orphanet:  251576

References

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How to cite this page

Type I RTKs: ErbB (epidermal growth factor) receptor family: epidermal growth factor receptor. Last modified on 05/11/2014. Accessed on 24/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1797.