General Information of the Protein
Protein ID
PT01605
Protein Name
Epidermal growth factor receptor
Gene Name
EGFR
Sequence
MRPSGTARTTLLVLLTALCAAGGALEEKKVCQGTSNRLTQLGTFEDHFLSLQRMYNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNALYENTYALAILSNYGTNRTGLRELPMRNLQEILIGAVRFSNNPILCNMDTIQWRDIVQNVFMSNMSMDLQSHPSSCPKCDPSCPNGSCWGGGEENCQKLTKIICAQQCSHRCRGRSPSDCCHNQCAAGCTGPRESDCLVCQKFQDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGPDYYEVEEDGIRKCKKCDGPCRKVCNGIGIGEFKDTLSINATNIKHFKYCTAISGDLHILPVAFKGDSFTRTPPLDPRELEILKTVKEITGFLLIQAWPDNWTDLHAFENLEIIRGRTKQHGQFSLAVVGLNITSLGLRSLKEISDGDVIISGNRNLCYANTINWKKLFGTPNQKTKIMNNRAEKDCKAVNHVCNPLCSSEGCWGPEPRDCVSCQNVSRGRECVEKCNILEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGIMGENNTLVWKYADANNVCHLCHANCTYGCAGPGLQGCEVWPSGPKIPSIATGIVGGLLFIVVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQAHLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPYGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASDISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELILEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMEDVVDADEYLIPQQGFFNSPSTSRTPLLSSLSATSNNSTVACINRNGSCRVKEDAFLQRYSSDPTGAVTEDNIDDAFLPVPEYVNQSVPKRPAGSVQNPVYHNQPLHPAPGRDLHYQNPHSNAVGNPEYLNTAQPTCLSSGFNSPALWIQKGSHQMSLDNPDYQQDFFPKETKPNGIFKGPTAENAEYLRVAPPSSEFIGA
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase EGFR family
Function
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:8404850). Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin (By similarity). Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration (By similarity). Plays a role in enhancing learning and memory performance (PubMed:20639532). Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (PubMed:35131940).
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Uniprot ID
Q01279
Ensembl ID
ENSG00000146648
Subcellular Location
Cell membrane
Endoplasmic reticulum membrane
Golgi apparatus membrane
Nucleus membrane
Endosome
Endosome membrane
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0033646
AZD-9291
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C28H33N7O2
 2
1
GI50 = 2600 nM
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2
IC50 = 81 nM
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CP0911447
4-(4-{3-[4-(3,4-Dimethoxy-phenylamino)-6-methoxy-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C29H27N3O5S3
 1
1
GI50 = 2650 nM
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CP0871203
4-(4-{3-[6-Methoxy-4-(4-nitro-phenylamino)-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C27H22N4O5S3
 1
1
GI50 = 3790 nM
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CP0914491
4-(4-{3-[6-Methoxy-4-(3-trifluoromethyl-phenylamino)-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C28H22F3N3O3S3
 1
1
GI50 = 3790 nM
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CP0961271
3-Allyldisulfanyl-propionic acid 3-[4-(4-bromo-phenylamino)-6-methoxy-quinazolin-7-yloxy]-propyl ester
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C24H26BrN3O4S2
 1
1
GI50 = 3910 nM
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CP0871192
N-[4-(3-Chloro-4-fluoro-phenylamino)-quinazolin-6-yl]-2-[4-(3-oxo-3H-[1,2]dithiol-4-yl)-phenoxy]-acetamide
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C25H16ClFN4O3S2
 1
1
GI50 = 4270 nM
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CP0871193
4-(4-{3-[4-(3-Bromo-phenylamino)-6-methoxy-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C27H22BrN3O3S3
 1
1
GI50 = 9230 nM
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CP0871205
4-(4-{3-[4-(4-Bromo-phenylamino)-6-methoxy-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C27H22BrN3O3S3
 1
1
GI50 = 9230 nM
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CP0486473
3-[4-(3-bromoanilino)-6-methoxyquinazolin-7-yl]oxypropyl 3-(prop-2-enyldisulfanyl)propanoate
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C24H26BrN3O4S2
 1
1
GI50 > 10000 nM
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CP0871191
2-But-3-enyldisulfanyl-N-[4-(3-chloro-4-fluoro-phenylamino)-quinazolin-6-yl]-acetamide
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C20H18ClFN4OS2
 1
1
GI50 > 10000 nM
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CP0911710
N-[4-(3-Bromo-phenylamino)-quinazolin-6-yl]-2-but-3-enyldisulfanyl-acetamide
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C20H19BrN4OS2
 1
1
GI50 > 10000 nM
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CP0955273
4-(4-{3-[4-(3-Chloro-4-fluoro-phenylamino)-6-methoxy-quinazolin-7-yloxy]-propoxy}-phenyl)-[1,2]dithiole-3-thione
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C27H21ClFN3O3S3
 1
1
GI50 > 10000 nM
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CP0458073
(11R)-5,11,26-trimethyl-16-[(4-methylpiperazin-1-yl)methyl]-7-oxa-4,5,13,20,22,27-hexazapentacyclo[22.3.1.02,6.013,21.014,19]octacosa-1(27),2(6),3,14(19),15,17,20,24(28),25-nonaen-23-one
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C30H38N8O2
 1
1
IC50 = 190 nM
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CP0458074
26-fluoro-5-methyl-7-oxa-4,5,13,20,22,27-hexazapentacyclo[22.3.1.02,6.013,21.014,19]octacosa-1(27),2(6),3,14,16,18,20,24(28),25-nonaen-23-one
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C22H21FN6O2
 1
1
IC50 = 270 nM
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CP0535683
N-[1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-2-(4-methoxypyridin-3-yl)pyridine-4-carboxamide
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C23H23N5O3
 1
1
IC50 = 700 nM
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CP0270683
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-(3-phenyl-propyl)-benzamide
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C23H24N2O4
 1
1
IC50 = 1000 nM
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CP0482076
(11R)-5,11,26-trimethyl-7-oxa-4,5,13,20,22,27-hexazapentacyclo[22.3.1.02,6.013,21.014,19]octacosa-1(27),2(6),3,14,16,18,20,24(28),25-nonaen-23-one
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C24H26N6O2
 1
1
IC50 = 1100 nM
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CP0482077
8-oxa-14,21,23,28-tetrazapentacyclo[23.3.1.02,7.014,22.015,20]nonacosa-1(28),2,4,6,15,17,19,21,25(29),26-decaen-24-one
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C24H22N4O2
 1
1
IC50 = 1300 nM
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CP0563815
5,26-dimethyl-7-oxa-4,5,13,20,22,27-hexazapentacyclo[22.3.1.02,6.013,21.014,19]octacosa-1(27),2(6),3,14,16,18,20,24(28),25-nonaen-23-one
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C23H24N6O2
 1
1
IC50 = 2300 nM
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CP0458075
N-[1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-2-pyridin-3-ylpyridine-4-carboxamide
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C22H21N5O2
 1
1
IC50 = 3600 nM
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CP0163636
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-(1,2,3,4-tetrahydro-naphthalen-2-yl)-benzamide
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C24H24N2O4
 1
1
IC50 = 4000 nM
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CP0268441
5-(2,5-Dihydroxy-benzylamino)-N-[2-(4-fluoro-phenyl)-ethyl]-2-hydroxy-benzamide
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C22H21FN2O4
 1
1
IC50 = 4000 nM
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CP0476182
N-[1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-2-(1-methylpyrazol-4-yl)pyridine-4-carboxamide
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C21H22N6O2
 1
1
IC50 = 5100 nM
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CP0320349
N-benzyl-5-[(2,5-dihydroxyphenyl)methylamino]-2-hydroxybenzamide
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C21H20N2O4
 1
1
IC50 = 8000 nM
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CP0212776
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-phenethyl-benzamide
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C22H22N2O4
 1
1
IC50 = 10000 nM
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CP0482073
N-[1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-2-phenylpyridine-4-carboxamide
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C23H22N4O2
 1
1
IC50 > 10000 nM
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CP0267543
5-(2,5-Dihydroxy-benzylamino)-N-hexyl-2-hydroxy-benzamide
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C20H26N2O4
 1
1
IC50 = 14000 nM
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CP0062042
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-(2-pyridin-2-yl-ethyl)-benzamide
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C21H21N3O4
 1
1
IC50 = 15000 nM
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CP0337077
4-(2,5-Dihydroxy-benzylamino)-N-(3-phenyl-propyl)-benzamide
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C23H24N2O3
 1
1
IC50 = 33000 nM
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CP0047056
5-(2,5-Dihydroxy-benzylamino)-N-dodecyl-2-hydroxy-benzamide
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C26H38N2O4
 1
1
IC50 = 35000 nM
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CP0184260
N-[2-(4-bromophenyl)ethyl]-5-[(2,5-dihydroxyphenyl)methylamino]-2-hydroxybenzamide
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C22H21BrN2O4
 1
1
IC50 = 35000 nM
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CP0358636
N-[2-(4-chlorophenyl)ethyl]-5-[(2,5-dihydroxyphenyl)methylamino]-2-hydroxybenzamide
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C22H21ClN2O4
 1
1
IC50 = 46000 nM
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CP0178481
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-(2-morpholin-4-yl-ethyl)-benzamide
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C20H25N3O5
 1
1
IC50 > 50000 nM
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CP0194921
5-(2,5-Dihydroxy-benzylamino)-2-hydroxy-N-[2-(4-methoxy-phenyl)-ethyl]-benzamide
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C23H24N2O5
 1
1
IC50 > 100000 nM
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CP0492215
N-benzyl-4-[(2,5-dihydroxyphenyl)methylamino]benzamide
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C21H20N2O3
 1
1
IC50 > 100000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 1
1 IC50 = 750.203627 nM