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
DrugBank Target
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Enzyme
KEGG Gene
NeXtProt
OMIM
Orphanet
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:  46
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:  31
Enzyme Reaction
EC Number: 2.7.10.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
canertinib Hs Inhibition 9.7 pKd 12
pKd 9.7 (Kd 1.9x10-10 M) [12]
afatinib Hs Inhibition 9.6 pKd 12
pKd 9.6 (Kd 2.5x10-10 M) [12]
erlotinib Hs Inhibition 9.2 pKd 12
pKd 9.2 (Kd 6.7x10-10 M) [12]
gefitinib Hs Inhibition 9.0 pKd 12
pKd 9.0 (Kd 1x10-9 M) [12]
gefitinib Hs Inhibition 8.3 pKi 43
pKi 8.3 (Ki 5.5x10-9 M) [43]
PD166285 Hs Inhibition 7.1 pKi 32
pKi 7.1 (Ki 8.75x10-8 M) [32]
rociletinib Hs Inhibition 6.5 pKi 42
pKi 6.5 (Ki 3.033x10-7 M) [42]
AG 9 Hs Inhibition <3.4 pKi 18
pKi <3.4 (Ki >4x10-4 M) [18]
Description: Measuring phosphorylation of the EGFR exogenous substrate polyGAT [poly(Glu6Ala3Tyr)]
compound 56 [PMID: 8568816] Hs Inhibition 11.2 pIC50 7
pIC50 11.2 (IC50 6x10-12 M) [7]
BPIQ-I Hs Inhibition 10.6 pIC50 35
pIC50 10.6 (IC50 2.5x10-11 M) [35]
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibition 9.5 pIC50 25
pIC50 9.5 (IC50 3x10-10 M) [25]
XL-647 Hs Inhibition 9.5 pIC50 19
pIC50 9.5 (IC50 3x10-10 M) [19]
PD 174265 Hs Inhibition 9.4 pIC50 14
pIC50 9.4 (IC50 4.5x10-10 M) [14]
erlotinib Hs Inhibition 9.0 pIC50 47
pIC50 9.0 (IC50 1x10-9 M) [47]
canertinib Hs Inhibition 8.8 pIC50 37
pIC50 8.8 (IC50 1.5x10-9 M) [37]
Description: Inhibition of kinase activity
AEE788 Hs Inhibition 8.7 pIC50 39
pIC50 8.7 (IC50 2x10-9 M) [39]
afatinib Hs Inhibition 8.0 – 9.3 pIC50 11,26
pIC50 8.0 – 9.3 (IC50 1.1x10-8 – 5x10-10 M) [11,26]
pelitinib Hs Inhibition 7.8 – 9.2 pIC50 43-44
pIC50 7.8 – 9.2 (IC50 1.45x10-8 – 6x10-10 M) [43-44]
falnidamol Hs Inhibition 8.5 pIC50 38
pIC50 8.5 (IC50 3x10-9 M) [38]
PKI166 Hs Inhibition 8.4 pIC50 23
pIC50 8.4 (IC50 3.7x10-9 M) [23]
JAK3 inhibitor II Hs Inhibition 8.4 pIC50 9
pIC50 8.4 (IC50 4x10-9 M) [9]
sapitinib Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 4x10-9 M) [6]
BMS-690514 Hs Inhibition 8.3 pIC50 29
pIC50 8.3 (IC50 5x10-9 M) [29]
AG1478 Hs Inhibition 8.2 pIC50 40
pIC50 8.2 (IC50 6x10-9 M) [40]
dacomitinib Hs Inhibition 8.2 pIC50 5
pIC50 8.2 (IC50 6x10-9 M) [5]
compound 38 [PMID: 24915291] Hs Inhibition 8.1 pIC50 27
pIC50 8.1 (IC50 7x10-9 M) [27]
poziotinib Hs Inhibition 8.1 pIC50 30
pIC50 8.1 (IC50 8x10-9 M) [30]
lapatinib Hs Inhibition 8.0 pIC50 36
pIC50 8.0 (IC50 1.02x10-8 M) [36]
ZM-306416 Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [2]
PD 158780 Hs Inhibition 7.8 pIC50 34
pIC50 7.8 (IC50 1.5x10-8 M) [34]
Description: Inhibition of EGFR autophosphorylation
EGFR/ErbB-2 inhibitor Hs Inhibition 7.7 pIC50 10
pIC50 7.7 (IC50 2x10-8 M) [10]
EGFR inhibitor Hs Inhibition 7.7 pIC50 13
pIC50 7.7 (IC50 2.1x10-8 M) [13]
BMS-599626 Hs Inhibition 7.5 pIC50 16
pIC50 7.5 (IC50 3.2x10-8 M) [16]
icotinib Hs Inhibition 7.3 pIC50 21
pIC50 7.3 (IC50 4.5x10-8 M) [21]
Description: Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells.
neratinib Hs Inhibition 7.0 pIC50 33
pIC50 7.0 (IC50 9.2x10-8 M) [33]
Description: Inhibition of autophosphorylation of the cytoplasmic domain of the RTK in a cell free system.
AG 112 Hs Inhibition 6.9 pIC50 18
pIC50 6.9 (IC50 1.25x10-7 M) [18]
Description: Measuring inhibition of substrate phosphorylation.
AP26113 Hs Inhibition 6.9 pIC50 24
pIC50 6.9 (IC50 1.29x10-7 M) [24]
PP121 Hs Inhibition 6.6 pIC50 3
pIC50 6.6 (IC50 2.6x10-7 M) [3]
vandetanib Hs Inhibition 6.5 pIC50 8
pIC50 6.5 (IC50 3x10-7 M) [8]
AG 490 Hs Inhibition 6.4 pIC50 17
pIC50 6.4 (IC50 4x10-7 M) [17]
Description: Inhibition of substrate phosphorylation.
AZD9291 Hs Inhibition 5.7 – 6.3 pIC50 4
pIC50 5.7 – 6.3 (IC50 2x10-6 – 5x10-7 M) [4]
dovitinib Hs Inhibition 5.7 pIC50 41
pIC50 5.7 (IC50 2x10-6 M) [41]
orantinib Hs Inhibition <4.0 pIC50 22
pIC50 <4.0 (IC50 >1x10-4 M) [22]
Inhibitor Comments
AZD9291 is much more potent at mutant EGFRs, with IC50 values <100nM [4].
Note that the primary target of rociletinib, as a second-generation EGFR inhibitor, is mutant EGFR such as that with the gatekeeper T790M mutation [42].
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
necitumumab Hs Binding 9.5 pKd 28
pKd 9.5 (Kd 3.2x10-10 M) [28]
Description: Binding affinity of whole IMC-11F8 IgG using BIAcore sensor technology.
cetuximab Hs Binding 9.4 pKd 20
pKd 9.4 (Kd 3.9x10-10 M) [20]
panitumumab Hs Inhibition - -
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
amphiregulin {Sp: Human} Hs Binding - -
betacellulin {Sp: Human} Hs Binding - -
EGF {Sp: Human} Hs Binding - -
epigen {Sp: Human} Hs Binding - -
epiregulin {Sp: Human} Hs Binding - -
HB-EGF {Sp: Human} Hs Binding - -
TGFα {Sp: Human} Hs Binding - -
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: 12,45

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 9.7 pKd
afatinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.2 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.6 pKd
vandetanib Hs Inhibitor Inhibition 8.0 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
dasatinib Hs Inhibitor Inhibition 6.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
Target used in screen: EGFR(E746-A750del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 10.0 pKd
canertinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.3 pKd
gefitinib Hs Inhibitor Inhibition 9.3 pKd
neratinib Hs Inhibitor Inhibition 8.6 pKd
vandetanib Hs Inhibitor Inhibition 8.3 pKd
lapatinib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd
staurosporine Hs Inhibitor Inhibition 6.9 pKd
Target used in screen: EGFR(G719C)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 10.0 pKd
canertinib Hs Inhibitor Inhibition 9.9 pKd
neratinib Hs Inhibitor Inhibition 9.4 pKd
erlotinib Hs Inhibitor Inhibition 9.1 pKd
lapatinib Hs Inhibitor Inhibition 9.0 pKd
gefitinib Hs Inhibitor Inhibition 8.7 pKd
vandetanib Hs Inhibitor Inhibition 8.0 pKd
bosutinib Hs Inhibitor Inhibition 7.0 pKd
barasertib-hQPA Hs Inhibitor Inhibition 6.9 pKd
foretinib Hs Inhibitor Inhibition 6.9 pKd
Target used in screen: EGFR(G719S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.7 pKd
canertinib Hs Inhibitor Inhibition 9.7 pKd
erlotinib Hs Inhibitor Inhibition 9.3 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.7 pKd
vandetanib Hs Inhibitor Inhibition 8.2 pKd
bosutinib Hs Inhibitor Inhibition 7.6 pKd
dasatinib Hs Inhibitor Inhibition 7.1 pKd
cediranib Hs Inhibitor Inhibition 7.1 pKd
Target used in screen: EGFR(L747-E749del, A750P)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.9 pKd
canertinib Hs Inhibitor Inhibition 9.8 pKd
erlotinib Hs Inhibitor Inhibition 9.3 pKd
gefitinib Hs Inhibitor Inhibition 9.2 pKd
neratinib Hs Inhibitor Inhibition 9.2 pKd
lapatinib Hs Inhibitor Inhibition 8.7 pKd
vandetanib Hs Inhibitor Inhibition 7.9 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd
staurosporine Hs Inhibitor Inhibition 7.0 pKd
Target used in screen: EGFR(L747-S752del, P753S)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.9 pKd
canertinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.3 pKd
gefitinib Hs Inhibitor Inhibition 9.2 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.4 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd
foretinib Hs Inhibitor Inhibition 6.7 pKd
Target used in screen: EGFR(L747-T751del,Sins)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.9 pKd
canertinib Hs Inhibitor Inhibition 9.6 pKd
erlotinib Hs Inhibitor Inhibition 9.5 pKd
gefitinib Hs Inhibitor Inhibition 9.3 pKd
neratinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.5 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.5 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 9.6 pKd
neratinib Hs Inhibitor Inhibition 9.2 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
erlotinib Hs Inhibitor Inhibition 9.0 pKd
lapatinib Hs Inhibitor Inhibition 8.6 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
dasatinib Hs Inhibitor Inhibition 6.9 pKd
Target used in screen: EGFR(L858R,T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.6 pKd
staurosporine Hs Inhibitor Inhibition 9.5 pKd
afatinib Hs Inhibitor Inhibition 9.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
midostaurin Hs Inhibitor Inhibition 8.1 pKd
neratinib Hs Inhibitor Inhibition 7.6 pKd
tamatinib Hs Inhibitor Inhibition 7.2 pKd
gefitinib Hs Inhibitor Inhibition 6.8 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.8 pKd
Target used in screen: EGFR(L861Q)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 9.7 pKd
afatinib Hs Inhibitor Inhibition 9.6 pKd
neratinib Hs Inhibitor Inhibition 9.4 pKd
lapatinib Hs Inhibitor Inhibition 8.9 pKd
erlotinib Hs Inhibitor Inhibition 8.9 pKd
gefitinib Hs Inhibitor Inhibition 8.9 pKd
vandetanib Hs Inhibitor Inhibition 8.0 pKd
bosutinib Hs Inhibitor Inhibition 7.2 pKd
foretinib Hs Inhibitor Inhibition 7.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd
Target used in screen: EGFR(S752-I759del)
Ligand Sp. Type Action Affinity Units
afatinib Hs Inhibitor Inhibition 9.9 pKd
canertinib Hs Inhibitor Inhibition 9.7 pKd
neratinib Hs Inhibitor Inhibition 9.2 pKd
gefitinib Hs Inhibitor Inhibition 9.0 pKd
erlotinib Hs Inhibitor Inhibition 8.8 pKd
lapatinib Hs Inhibitor Inhibition 8.4 pKd
vandetanib Hs Inhibitor Inhibition 7.9 pKd
bosutinib Hs Inhibitor Inhibition 7.0 pKd
staurosporine Hs Inhibitor Inhibition 6.5 pKd
dasatinib Hs Inhibitor Inhibition 6.5 pKd
Target used in screen: EGFR(T790M)
Ligand Sp. Type Action Affinity Units
canertinib Hs Inhibitor Inhibition 10.0 pKd
afatinib Hs Inhibitor Inhibition 9.2 pKd
staurosporine Hs Inhibitor Inhibition 9.1 pKd
neratinib Hs Inhibitor Inhibition 8.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.1 pKd
midostaurin Hs Inhibitor Inhibition 8.0 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
gefitinib Hs Inhibitor Inhibition 7.4 pKd
tamatinib Hs Inhibitor Inhibition 7.1 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.1 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