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:  56
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:  38
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 13
pKd 9.7 (Kd 1.9x10-10 M) [13]
afatinib Hs Inhibition 9.6 pKd 13
pKd 9.6 (Kd 2.5x10-10 M) [13]
erlotinib Hs Inhibition 9.2 pKd 13
pKd 9.2 (Kd 6.7x10-10 M) [13]
gefitinib Hs Inhibition 9.0 pKd 13
pKd 9.0 (Kd 1x10-9 M) [13]
WZ4002 Hs Inhibition 7.3 pKd 58
pKd 7.3 (Kd 4.6x10-8 M) [58]
gefitinib Hs Inhibition 8.3 pKi 53
pKi 8.3 (Ki 5.5x10-9 M) [53]
PD166285 Hs Inhibition 7.1 pKi 39
pKi 7.1 (Ki 8.75x10-8 M) [39]
rociletinib Hs Inhibition 6.5 pKi 51
pKi 6.5 (Ki 3.033x10-7 M) [51]
AG 9 Hs Inhibition <3.4 pKi 20
pKi <3.4 (Ki >4x10-4 M) [20]
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 43
pIC50 10.6 (IC50 2.5x10-11 M) [43]
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibition 9.5 pIC50 30
pIC50 9.5 (IC50 3x10-10 M) [30]
XL-647 Hs Inhibition 9.5 pIC50 21
pIC50 9.5 (IC50 3x10-10 M) [21]
PD 174265 Hs Inhibition 9.4 pIC50 16
pIC50 9.4 (IC50 4.5x10-10 M) [16]
erlotinib Hs Inhibition 9.0 pIC50 57
pIC50 9.0 (IC50 1x10-9 M) [57]
nazartinib Hs Inhibition >9.0 pIC50 34
pIC50 >9.0 (IC50 <1x10-9 M) [34]
Description: Biochemical assay using EGFR L858R/T790M with a 90 minute preincubation with the inhibitor.
canertinib Hs Inhibition 8.8 pIC50 45
pIC50 8.8 (IC50 1.5x10-9 M) [45]
Description: Inhibition of kinase activity
AEE788 Hs Inhibition 8.7 pIC50 48
pIC50 8.7 (IC50 2x10-9 M) [48]
afatinib Hs Inhibition 8.0 – 9.3 pIC50 12,31
pIC50 8.0 – 9.3 (IC50 1.1x10-8 – 5x10-10 M) [12,31]
CUDC-101 Hs Inhibition 8.6 pIC50 8
pIC50 8.6 (IC50 2.4x10-9 M) [8]
pelitinib Hs Inhibition 7.8 – 9.2 pIC50 53-54
pIC50 7.8 – 9.2 (IC50 1.45x10-8 – 6x10-10 M) [53-54]
falnidamol Hs Inhibition 8.5 pIC50 46
pIC50 8.5 (IC50 3x10-9 M) [46]
PKI166 Hs Inhibition 8.4 pIC50 27
pIC50 8.4 (IC50 3.7x10-9 M) [27]
JAK3 inhibitor II Hs Inhibition 8.4 pIC50 10
pIC50 8.4 (IC50 4x10-9 M) [10]
sapitinib Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 4x10-9 M) [6]
BMS-690514 Hs Inhibition 8.3 pIC50 35
pIC50 8.3 (IC50 5x10-9 M) [35]
olmutinib Hs Inhibition 8.3 pIC50 40
pIC50 8.3 (IC50 4.96x10-9 M) [40]
Description: Biochemical assay
AG1478 Hs Inhibition 8.2 pIC50 49
pIC50 8.2 (IC50 6x10-9 M) [49]
dacomitinib Hs Inhibition 8.2 pIC50 5
pIC50 8.2 (IC50 6x10-9 M) [5]
compound 38 [PMID: 24915291] Hs Inhibition 8.1 pIC50 32
pIC50 8.1 (IC50 7x10-9 M) [32]
poziotinib Hs Inhibition 8.1 pIC50 37
pIC50 8.1 (IC50 8x10-9 M) [37]
lapatinib Hs Inhibition 8.0 pIC50 44
pIC50 8.0 (IC50 1.02x10-8 M) [44]
ZM-306416 Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [2]
PD 158780 Hs Inhibition 7.8 pIC50 42
pIC50 7.8 (IC50 1.5x10-8 M) [42]
Description: Inhibition of EGFR autophosphorylation
EGFR/ErbB-2 inhibitor Hs Inhibition 7.7 pIC50 11
pIC50 7.7 (IC50 2x10-8 M) [11]
EGFR inhibitor Hs Inhibition 7.7 pIC50 14
pIC50 7.7 (IC50 2.1x10-8 M) [14]
BGB-283 Hs Inhibition 7.5 pIC50 47
pIC50 7.5 (IC50 2.9x10-8 M) [47]
Description: Inhibition of wild type EGFR kinase domain (aa669-1210)
BMS-599626 Hs Inhibition 7.5 pIC50 18
pIC50 7.5 (IC50 3.2x10-8 M) [18]
icotinib Hs Inhibition 7.3 pIC50 25
pIC50 7.3 (IC50 4.5x10-8 M) [25]
Description: Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells.
neratinib Hs Inhibition 7.0 pIC50 41
pIC50 7.0 (IC50 9.2x10-8 M) [41]
Description: Inhibition of autophosphorylation of the cytoplasmic domain of the RTK in a cell free system.
AG 112 Hs Inhibition 6.9 pIC50 20
pIC50 6.9 (IC50 1.25x10-7 M) [20]
Description: Measuring inhibition of substrate phosphorylation.
brigatinib Hs Inhibition 6.9 pIC50 28
pIC50 6.9 (IC50 1.29x10-7 M) [28]
PP1 Hs Inhibition 6.6 pIC50 23
pIC50 6.6 (IC50 2.5x10-7 M) [23]
PP121 Hs Inhibition 6.6 pIC50 3
pIC50 6.6 (IC50 2.6x10-7 M) [3]
vandetanib Hs Inhibition 6.5 pIC50 9
pIC50 6.5 (IC50 3x10-7 M) [9]
AG 490 Hs Inhibition 6.4 pIC50 19
pIC50 6.4 (IC50 4x10-7 M) [19]
Description: Inhibition of substrate phosphorylation.
osimertinib Hs Inhibition 6.3 pIC50 52
pIC50 6.3 (IC50 4.94x10-7 M) [52]
dovitinib Hs Inhibition 5.7 pIC50 50
pIC50 5.7 (IC50 2x10-6 M) [50]
orantinib Hs Inhibition <4.0 pIC50 26
pIC50 <4.0 (IC50 >1x10-4 M) [26]
naquotinib Hs Inhibition - - 36
[36]
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 [51].
Olmutinib potently inhibits EGFR in in vitro biochemical assay, but this does not translate to inhibition in vitro cellular assays [40].
Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
panitumumab Hs Binding 10.3 pKd 15
pKd 10.3 (Kd 5x10-11 M) [15]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
necitumumab Hs Binding 9.5 pKd 33
pKd 9.5 (Kd 3.2x10-10 M) [33]
Description: Binding affinity of whole IMC-11F8 IgG using BIAcore sensor technology.
cetuximab Hs Binding 9.4 pKd 22
pKd 9.4 (Kd 3.9x10-10 M) [22]
MM-151 Hs Binding - - 24,29
[24,29]
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: 13,55

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