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epidermal growth factor receptor

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Target not currently curated in GtoImmuPdb

Target id: 1797

Nomenclature: epidermal growth factor receptor

Abbreviated Name: EGFR

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

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1210 7p11.2 EGFR epidermal growth factor receptor
Mouse 1 1210 11 9.41 cM Egfr epidermal growth factor receptor
Rat - 1209 14q22 Egfr epidermal growth factor receptor
Previous and Unofficial Names Click here for help
HER1 | avian erythroblastic leukemia viral (v-erbB) oncogene homolog | Wa5 | ERBB1
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
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:  101
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:  70
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
amphiregulin {Sp: Human}
betacellulin {Sp: Human}
EGF {Sp: Human}
epigen {Sp: Human}
epiregulin {Sp: Human}
HB-EGF {Sp: Human}
TGFα {Sp: Human}

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
canertinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.7 pKd 24
pKd 9.7 (Kd 1.9x10-10 M) [24]
afatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.6 pKd 24
pKd 9.6 (Kd 2.5x10-10 M) [24]
erlotinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.2 pKd 24
pKd 9.2 (Kd 6.7x10-10 M) [24]
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 9.0 – 9.0 pKd 21,24
pKd 9.0 (Kd 1x10-9 M) [24]
pKd 9.0 (Kd 1.1x10-9 M) [21]
MS154 Small molecule or natural product Hs Inhibition 8.7 pKd 21
pKd 8.7 (Kd 1.8x10-9 M) [21]
Description: Dissociation constant determined for wild type EGFR in a competitive binding assay.
MS39 Small molecule or natural product Hs Inhibition 8.0 pKd 21
pKd 8.0 (Kd 1.1x10-8 M) [21]
Description: Dissociation constant determined for wild type EGFR in a competitive binding assay.
WZ4002 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pKd 110
pKd 7.3 (Kd 4.6x10-8 M) [110]
xiliertinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 10.3 pKi 79
pKi 10.3 (Ki 5x10-11 M) [79]
gefitinib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.3 pKi 98
pKi 8.3 (Ki 5.5x10-9 M) [98]
PD166285 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pKi 71
pKi 7.1 (Ki 8.75x10-8 M) [71]
rociletinib Small molecule or natural product Ligand has a PDB structure Hs Inhibition 6.5 pKi 94
pKi 6.5 (Ki 3.033x10-7 M) [94]
AG 9 Small molecule or natural product Primary target of this compound Hs Inhibition <3.4 pKi 34
pKi <3.4 (Ki >4x10-4 M) [34]
Description: Measuring phosphorylation of the EGFR exogenous substrate polyGAT [poly(Glu6Ala3Tyr)]
compound 56 [PMID: 8568816] Small molecule or natural product Primary target of this compound Hs Inhibition 11.2 pIC50 11
pIC50 11.2 (IC50 6x10-12 M) [11]
BPIQ-I Small molecule or natural product Primary target of this compound Hs Inhibition 10.6 pIC50 81
pIC50 10.6 (IC50 2.5x10-11 M) [81]
asandeutertinib Small molecule or natural product Hs Inhibition 8.6 – 10.9 pIC50 111
pIC50 10.9 (IC50 1.2x10-11 M) [111]
Description: Inhibition of phosphorylation of EGFR in NCI-H1975 cells with L858R/T790M EGFR double mutant
pIC50 10.7 (IC50 2x10-11 M) [111]
Description: Inhibition of phosphorylation of EGFR in PC9 cells with Exon19 deletion EGFR
pIC50 8.6 (IC50 2.53x10-9 M) [111]
Description: Inhibition of phosphorylation of WT EGFR in LoVo cells
TQB3804 Small molecule or natural product Hs Inhibition 9.7 – 9.8 pIC50 102
pIC50 9.8 (IC50 1.6x10-10 M) [102]
Description: Inhibition of EGFR L858R/T790M/C797S triple mutant
pIC50 9.7 (IC50 2.2x10-10 M) [102]
Description: Inhibition of EGFR Del19/T790M/C797S triple mutant
JBJ-04-125-02 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.6 pIC50 89
pIC50 9.6 (IC50 2.6x10-10 M) [89]
Description: Inhibition of EGFRL858R/T790M in a biochemical assay
CH7233163 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.6 pIC50 48
pIC50 9.6 (IC50 2.8x10-10 M) [48]
Description: Inhibition potency in a biochemical assay with EGFRDel19/T790M/C797S.
EGFR/ErbB-2/ErbB-4 inhibitor Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.5 pIC50 52
pIC50 9.5 (IC50 3x10-10 M) [52]
tesevatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.5 pIC50 35
pIC50 9.5 (IC50 3x10-10 M) [35]
mifanertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.4 pIC50 105
pIC50 9.4 (IC50 4x10-10 M) [105]
PD 174265 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.4 pIC50 30
pIC50 9.4 (IC50 4.5x10-10 M) [30]
allitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.3 pIC50 103
pIC50 9.3 (IC50 5x10-10 M) [103]
BI-4020 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.2 pIC50 25
pIC50 9.2 (IC50 6x10-10 M) [25]
Description: Inhibition od EGFR triple mutant del19/T790M/C797S in vitro
erlotinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 109
pIC50 9.0 (IC50 1x10-9 M) [109]
nazartinib Small molecule or natural product Hs Inhibition >9.0 pIC50 64
pIC50 >9.0 (IC50 <1x10-9 M) [64]
Description: Biochemical assay using EGFR L858R/T790M with a 90 minute preincubation with the inhibitor.
pirotinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pIC50 43
pIC50 9.0 (IC50 1x10-9 M) [43]
zorifertinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 – 9.5 pIC50 107
pIC50 9.5 (IC50 3x10-10 M) [107]
Description: Inhibition of wild type EGFR in vitro, at Km of ATP.
pIC50 8.1 (IC50 7.2x10-9 M) [107]
Description: Inhibition of EGFRL858R in vitro.
canertinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.8 pIC50 84
pIC50 8.8 (IC50 1.5x10-9 M) [84]
Description: Inhibition of kinase activity
almonertinib Small molecule or natural product Approved drug Hs Inhibition 8.7 pIC50 106
pIC50 8.7 (IC50 1.89x10-9 M) [106]
Description: Inhibition of wild type EGFR enzyme activity in a TR-FRET assay
AEE788 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 90
pIC50 8.7 (IC50 2x10-9 M) [90]
afatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 – 9.3 pIC50 23,55
pIC50 8.0 – 9.3 (IC50 1.1x10-8 – 5x10-10 M) [23,55]
CUDC-101 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 13
pIC50 8.6 (IC50 2.4x10-9 M) [13]
compound 17b [PMID: 35286086] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 1
pIC50 8.6 (IC50 2.5x10-9 M) [1]
pelitinib Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.8 – 9.2 pIC50 98-99
pIC50 7.8 – 9.2 (IC50 1.45x10-8 – 6x10-10 M) [98-99]
falnidamol Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 85
pIC50 8.5 (IC50 3x10-9 M) [85]
PKI166 Small molecule or natural product Hs Inhibition 8.4 pIC50 49
pIC50 8.4 (IC50 3.7x10-9 M) [49]
JAK3 inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 18
pIC50 8.4 (IC50 4x10-9 M) [18]
sapitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 9
pIC50 8.4 (IC50 4x10-9 M) [9]
zipalertinib Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.1 – 8.7 pIC50 39
pIC50 8.7 (IC50 2x10-9 M) [39]
Description: Inhibition of hEGFR with T790M/L858R mutation in a biochemical enzyme assay
pIC50 8.1 (IC50 7.4x10-9 M) [39]
Description: Inhibition of hEGFR with D770_N771insNPG insertion in a biochemical enzyme assay
pIC50 8.1 (IC50 8x10-9 M) [39]
Description: Inhibition of WT hEGFR in a biochemical enzyme assay
BMS-690514 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 65
pIC50 8.3 (IC50 5x10-9 M) [65]
ibrutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 12
pIC50 8.3 (IC50 5.3x10-9 M) [12]
JND3229 Small molecule or natural product Hs Inhibition 8.2 pIC50 62
pIC50 8.2 (IC50 5.8x10-9 M) [62]
Description: Inhibition of EGFRdel19/T790M/C797S
AG1478 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.2 pIC50 91
pIC50 8.2 (IC50 6x10-9 M) [91]
dacomitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 8
pIC50 8.2 (IC50 6x10-9 M) [8]
compound 38 [PMID: 24915291] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 58
pIC50 8.1 (IC50 7x10-9 M) [58]
abivertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 104
pIC50 8.1 (IC50 7.68x10-9 M) [104]
Description: In a biochemical assay.
poziotinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 pIC50 68
pIC50 8.1 (IC50 8x10-9 M) [68]
example 10 [CN110740999A] Small molecule or natural product Hs Inhibition 6.4 – 9.7 pIC50 54
pIC50 9.7 (IC50 2x10-10 M) [54]
Description: Inhibition of EGFR with triple del19/T790M/C797S mutation in an enzymatic assay
pIC50 9.1 (IC50 7x10-10 M) [54]
Description: Inhibition of EGFR with del19 mutation in an enzymatic assay
pIC50 8.4 (IC50 4x10-9 M) [54]
Description: Inhibition of EGFR with dual del19/T790M mutation in an enzymatic assay
pIC50 6.4 (IC50 4.3x10-7 M) [54]
Description: Inhibition of WT EGFR in an enzymatic assay
lapatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 83
pIC50 8.0 (IC50 1.02x10-8 M) [83]
ZM-306416 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1x10-8 M) [4]
pyrotinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Irreversible inhibition 7.9 pIC50 57
pIC50 7.9 (IC50 1.3x10-8 M) [57]
selatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 108
pIC50 7.9 (IC50 1.3x10-8 M) [108]
dosimertinib Small molecule or natural product Hs Inhibition 6.9 – 8.8 pIC50 67
pIC50 8.8 (IC50 1.7x10-9 M) [67]
Description: Enzymatic inhibitory activity vs. L858R/T790M EGFR
pIC50 6.9 (IC50 1.138x10-7 M) [67]
Description: Enzymatic inhibitory activity vs. WT EGFR
PD 158780 Small molecule or natural product Primary target of this compound Hs Inhibition 7.8 pIC50 80
pIC50 7.8 (IC50 1.5x10-8 M) [80]
Description: Inhibition of EGFR autophosphorylation
tigozertinib Small molecule or natural product Hs Inhibition >7.8 pIC50 14
pIC50 >7.8 (IC50 <1.5x10-8 M) [14]
Description: Biochemical enzyme inhibition assay (measuring inhibition of peptide substrate phosphorylation) using EGFR with triple mutation (del 19 or exon 21 L858R substitution mutation, T790M mutation, and C797S mutation)
compound 18j [PMID: 35446588] Small molecule or natural product Hs Inhibition 7.6 – 7.8 pIC50 19
pIC50 7.8 (IC50 1.58x10-8 M) [19]
Description: Inhibition of EGFRdel19/T790M/C797S
pIC50 7.6 (IC50 2.36x10-8 M) [19]
Description: Inhibition of EGFR L858R/T790M/C797S mutant
compound 52 [PMID: 36749735] Small molecule or natural product Hs Inhibition 7.6 – 7.8 pIC50 56
pIC50 7.8 (IC50 1.5x10-8 M) [56]
Description: Inhibition of EGFRL858R/T790M enzyme activity
pIC50 7.6 (IC50 2.5x10-8 M) [56]
Description: Inhibition of WT EGFR enzymatic activity
EGFR/ErbB-2 inhibitor Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 22
pIC50 7.7 (IC50 2x10-8 M) [22]
lazertinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition >7.7 pIC50 86
pIC50 >7.7 (IC50 <2x10-8 M) [86]
Description: Measuring inhibition of mutant EGFR kinase activities in biochemical assays (equivalent potency against Del19, L858R, L858R/T790M and Del19/T790M EGFR mutants). NOTE lazertinib is inactive vs. wild type EGFR.
EGFR inhibitor Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.7 pIC50 27
pIC50 7.7 (IC50 2.1x10-8 M) [27]
C34 [Zhu et al., 2023] Small molecule or natural product Hs Inhibition 7.0 – 8.3 pIC50 112
pIC50 8.3 (IC50 5.1x10-9 M) [112]
Description: Inhibition of EGFR triple mutant L858R/T790M/C797S
pIC50 7.0 (IC50 1.06x10-7 M) [112]
Description: Inhibition of wild type hEGFR
lifirafenib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 87
pIC50 7.5 (IC50 2.9x10-8 M) [87]
Description: Inhibition of wild type EGFR kinase domain (aa669-1210)
compound 6g [PMID: 30633509] Small molecule or natural product Hs Inhibition 7.5 pIC50 82
pIC50 7.5 (IC50 3x10-8 M) [82]
BMS-599626 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 32
pIC50 7.5 (IC50 3.2x10-8 M) [32]
AZ5104 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.5 pIC50 20
pIC50 7.5 (IC50 3.3x10-8 M) [20]
Description: Inhibition of wild type EGFR phosphorylation in human LoVo cells
icotinib Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 7.3 pIC50 41
pIC50 7.3 (IC50 4.5x10-8 M) [41]
Description: Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells.
DBPR112 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.3 pIC50 60
pIC50 7.3 (IC50 4.8x10-8 M) [60]
Description: Enzymatic activity inhibition of EGFRL858R/T790M
sunvozertinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.1 pIC50 59
pIC50 7.1 (IC50 8.04x10-8 M) [59]
Description: Inhibition of WT EGFR phosphorylation in A431 cells
neratinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.0 pIC50 78
pIC50 7.0 (IC50 9.2x10-8 M) [78]
Description: Inhibition of autophosphorylation of the cytoplasmic domain of the RTK in a cell free system.
mobocertinib Small molecule or natural product Approved drug Hs Inhibition 7.0 pIC50 42
pIC50 7.0 (IC50 1x10-7 M) [42]
Description: Inhibition of EGFR harbouring concurring exon 21, L858R and T790M mutations.
AG 112 Small molecule or natural product Primary target of this compound Hs Inhibition 6.9 pIC50 34
pIC50 6.9 (IC50 1.25x10-7 M) [34]
Description: Measuring inhibition of substrate phosphorylation.
brigatinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 50
pIC50 6.9 (IC50 1.29x10-7 M) [50]
PF-670462 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pIC50 7
pIC50 6.8 (IC50 1.5x10-7 M) [7]
Description: In a biochemical kinase assay.
PP1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 37
pIC50 6.6 (IC50 2.5x10-7 M) [37]
ralimetinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.2 – 8.0 pIC50 10
pIC50 8.0 (IC50 1.1x10-8 M) [10]
Description: Inhibitor potency for EGFRG719C
pIC50 6.7 (IC50 1.8x10-7 M) [10]
Description: Inhibitor potency for WT EGFR
pIC50 5.2 (IC50 6.06x10-6 M) [10]
Description: Inhibitor potency for EGFR with gatekeeper mutation T790M
PP121 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 5
pIC50 6.6 (IC50 2.6x10-7 M) [5]
BI-4142 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 97
pIC50 6.6 (IC50 2.7x10-7 M) [97]
Description: Inhibition of autophosphorylation of WT EGFR overexpressed in HEK293 cells
vandetanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 16
pIC50 6.5 (IC50 3x10-7 M) [16]
mavelertinib Small molecule or natural product Hs Inhibition 6.5 pIC50 76
pIC50 6.5 (IC50 3.07x10-7 M) [76]
olmutinib Small molecule or natural product Approved drug Hs Inhibition 6.0 – 7.0 pIC50 17
pIC50 6.0 – 7.0 (IC50 1x10-6 – 1x10-7 M) [17]
Description: Biochemical assay
tuxobertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 – 6.5 pIC50 28
pIC50 6.3 – 6.5 (IC50 5x10-7 – 3x10-7 M) [28]
Description: Inhibition of WT EGFR kinase activity
AG 490 Small molecule or natural product Primary target of this compound Hs Inhibition 6.4 pIC50 33
pIC50 6.4 (IC50 4x10-7 M) [33]
Description: Inhibition of substrate phosphorylation.
tucatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.3 pIC50 53
pIC50 6.3 (IC50 4.49x10-7 M) [53]
Description: Inhibition of enzyme activity in a biochemical assay.
osimertinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 6.3 pIC50 95
pIC50 6.3 (IC50 4.94x10-7 M) [95]
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 77
pIC50 6.3 (IC50 5.2x10-7 M) [77]
zongertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 96
pIC50 6.2 (IC50 5.79x10-7 M) [96]
Description: Inhibition of wild type EGFR phosphorylation
acalabrutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition <6.0 pIC50 12
pIC50 <6.0 (IC50 >1x10-6 M) [12]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pIC50 92
pIC50 5.7 (IC50 2x10-6 M) [92]
orantinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition <4.0 pIC50 47
pIC50 <4.0 (IC50 >1x10-4 M) [47]
naquotinib Small molecule or natural product Ligand has a PDB structure Hs Inhibition - - 66
[66]
tarloxotinib Small molecule or natural product Hs Inhibition - - 75
[75]
firmonertinib Small molecule or natural product Approved drug Hs Inhibition - - 63
[63]
rezivertinib Small molecule or natural product Hs Inhibition - - 74
[74]
befotertinib Small molecule or natural product Approved drug Hs Inhibition - - 46
[46]
Inhibitor Comments
AZD9291 is much more potent at mutant EGFRs, with IC50 values <100nM [6].
Note that the primary target of rociletinib, as a second-generation EGFR inhibitor, is mutant EGFR such as that with the gatekeeper T790M mutation [94].
Olmutinib potently inhibits EGFR in in vitro biochemical assay, but this does not translate to inhibition in vitro cellular assays [72].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
JBJ-09-063 Small molecule or natural product Hs Negative 10.1 pIC50 88
pIC50 10.1 (IC50 8.3x10-11 M) [88]
Description: Inhibition of enzyme activity of triple mutant EGFR L858R/T790M/C797S
EGFR inhibitor 57 Small molecule or natural product Hs Inhibition 7.7 – 8.7 pIC50 69
pIC50 8.7 (IC50 2x10-9 M) [69]
Description: Inhibition potency for EGFR with the L858R/T790M/C797S triple mutation.
pIC50 7.7 (IC50 2x10-8 M) [69]
Description: Inhibition potency for EGFR with the L858R/C797S double mutation
EAI045 Small molecule or natural product Hs Inhibition - - 45
[45]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
panitumumab Peptide Approved drug Primary target of this compound Hs Antagonist 10.3 pKd 29
pKd 10.3 (Kd 5x10-11 M) [29]
necitumumab Peptide Approved drug Primary target of this compound Hs Binding 9.5 pKd 61
pKd 9.5 (Kd 3.2x10-10 M) [61]
Description: Binding affinity of whole IMC-11F8 IgG using BIAcore sensor technology.
cetuximab Peptide Approved drug Primary target of this compound Hs Binding 9.4 pKd 36
pKd 9.4 (Kd 3.9x10-10 M) [36]
amivantamab Peptide Approved drug Primary target of this compound Click here for species-specific activity table Hs Binding 8.9 pKd 44
pKd 8.9 (Kd 1.4x10-9 M) [44]
Description: Binding affinity determined by surface plasmon resonance.
MM-151 Peptide Primary target of this compound Hs Binding - - 38,51
[38,51]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
amphiregulin {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Binding - -
betacellulin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Binding - -
EGF {Sp: Human} Peptide Ligand is endogenous in the given species Hs Binding - -
epigen {Sp: Human} Peptide Ligand is endogenous in the given species Hs Binding - -
epiregulin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Binding - -
HB-EGF {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Binding - -
TGFα {Sp: Human} Peptide Ligand is endogenous in the given species Hs Binding - -
DiscoveRx KINOMEscan® screen Click here for help
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: 24,100

Key to terms and symbols Click column headers to sort
Target used in screen: EGFR
Ligand Sp. Type Action Value Parameter
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 9.7 pKd
afatinib Small molecule or natural product Approved drug