Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00441
[1], [2], [3], [4], [5]
RNA modification MIR214 MIR214 ADARB1 Methylation : modification sites Indirect Inhibition m6A modification EGFR EGFR METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Epidermal growth factor receptor (EGFR)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Adenosine-to-Inosine editing (A-to-I)
Epigenetic Regulator Double-stranded RNA-specific editase 1 (ADARB1) WRITER View Details
Regulated Target MicroRNA 214 (MIR214) View Details
Crosstalk Relationship A-to-I  →  m6A Inhibition
Crosstalk Mechanism RNA modification indirectly impacts m6A modification through downstream signaling pathways
Crosstalk Summary ADARB1 interacts with MicroRNA 214 (MIR214), increasing it's A-to-I level and inhibiting its physical interaction with Epidermal growth factor receptor (EGFR), which was regulated by METTL3-mediated m6A modification.
In-vitro Model
A-549 Lung adenocarcinoma Homo sapiens CVCL_0023
NCI-H1299 Lung large cell carcinoma Homo sapiens CVCL_0060
NCI-H460 Lung large cell carcinoma Homo sapiens CVCL_0459
A-375 Amelanotic melanoma Homo sapiens CVCL_0132
Huh-7 Adult hepatocellular carcinoma Homo sapiens CVCL_0336
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Epidermal growth factor receptor (EGFR) 222 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Necitumumab Approved [6]
Synonyms
LY3012211
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name HEGF Approved [7]
MOA Activator
External Link
 Compound Name Erlotinib Approved [8]
Synonyms
Erlotinin; Tarceva; Erlotinib Base; OSI 744; R 1415; CP 358,774; CP-358774; Erlotinib(Tarceva); Tarceva (TN); CP-358,774; Erlotinib, OS-774; N-(3-ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine; [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE; [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine; 4-[(3-Ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.1 nM
External Link
 Compound Name Gefitinib Approved [9]
Synonyms
Gefitini; IRE; Iressa; Irressat; Gefitinib [USAN]; ZD 1839; ZD1839; Iressa (TN); Iressa(TM); ZD-1839; CU-00000000396-1; Gefitinib,Iressa, ZD1839; Gefitinib (JAN/USAN/INN); ZD-1839, Iressa, Gefitinib; N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamide; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine; N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline; 6-(3-morpholinopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.1 nM
External Link
 Compound Name Panitumumab Approved [10]
Synonyms
Vectibix; Panitumumab (genetical recombination); Vectibix (TN); Panitumumab (USAN/INN); Panitumumab (genetical recombination) (JAN); Panitumumab (EGFR mAb inhibitor)
    Click to Show/Hide
MOA Suppressor
External Link
 Compound Name Cetuximab Approved [11]
Synonyms
Erbitux; Cetuximab (genetical recombination); Erbitux (TN); Cetuximab (USAN/INN); Cetuximab (genetical recombination) (JAN); novel EGFR mAb inhibitors
    Click to Show/Hide
External Link
 Compound Name BIBW 2992 Approved [12]
Synonyms
Afatinib; Tomtovok; Tovok; BIBW-2992; Tovok (TN); Tovok, BIBW2992; (2E)-N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydrofuran-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide; EGFR inhibitor 2nd gens
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.19 nM
External Link
 Compound Name Nitroglycerin Approved [7]
Synonyms
Glyceryl trinitrate; Trinitroglycerin; Nitroglycerol; Nitrostat; Nitroglycerine; Nitro-dur; Minitran; Trinitroglycerol; 55-63-0; Nitroderm; Nitroglyn; Nitrospan; Nitronet; Tridil; Glycerol trinitrate; Transderm-nitro; Transderm Nitro; Epinitril; Susadrin; Perlinganit; Nitrolingual; Nitrolan; Sustonit; Nitrocine; Trinitrin; Natispray; Lenitral; Nitrong; Niong; Nitro-Bid; Nitroderm TTS; Trinitrosan; Rectogesic; Nitroglicerina; Cordipatch; Perglottal; Nitrorectal; Gilustenon; Nitroretard; Nitroplast; Corditrine; Trinitrolong; Adesitrin; Aldonitrin; Angibid; Angiolingual; Angiplex; Anglix; Angonist; Angorin; Anogesic; Buccal; Buccard; Cardabid; Cardamist; Cardinit; Cardiodisco; Cellegesic; Chitamite; Colenitral; Dauxona; Deponit; Diafusor; Discotrine; Dynamite; GTN; Glonoin; Glycerintrinitrate; Glyceroltrinitraat; Glyceryl; Glycerylnitrat; Glytrin; Herwicard; Herzer; Klavikordal; Lentonitrina; Millisrol; Minitram; Minitro; Mionitrat; Myocon; Myoglycerin; Myovin; NTG; Niglin; Niglycon; Nirmin; Nitora; Nitradisc; Nitrangin; Nitrek; Nitriderm; NitroBid; NitroCor; NitroDur; NitroMist; NitroQuick; NitroQuik; Nitroard; Nitrobaat; Nitrobukal; Nitrocap; Nitrocard; Nitrocerin; Nitroclyn; Nitrocontin; Nitrocot; Nitrodisc; Nitrodyl; Nitrogard; Nitrogliceryna; Nitroglin; Nitroject; Nitroletten; Nitrolin; Nitrolowe; Nitromel; Nitromex; Nitromint; Nitropatch; Nitropen; Nitropercuten; Nitroperlinit; Nitroprol; Nitropront; Nitroprontan; Nitrorex; Nitrostabilin; Nitrovis; Nysconitrine; Percutol; Perganit; Plastranit; Polnitrin; Ratiopharm; Soup; Suscard; Sustac; Sustak; TNG; Temponitrin; Trinalgon; Trinipatch; Triniplas; Trinitrol; Trinitron; Turicard; Vascana; Vasoglyn; Vasolator; Vernies; Willong; Blasting gelatin; Blasting oil; Gepan Nitroglicerin; Gilucor nitro; Glycerin trinitrate; Glycerine trinitrate; Glyceryl nitrate; NITRO IV; Neos nitro OPT; Niong Retard; Nitradisc Pad; Nitradisc TTS; Nitriderm TTS; Nitro Bid; Nitro Dur; Nitro Dur TTS; Nitro Mack Retard; Nitro Retard; Nitro Rorer; Nitrobid Oint; Nitrocontin Continus; Nitroderm TTS Ext; Nitrodyl TTS; Nitrol Ointment; Nitrolingual Spray; Nitromack Retard; Nitromint Aerosol; Nitromint Retard; Nitronal Aqueous; Nitrong Retard; Nitrong parenteral; Nitrozell retard; Percutol Oint; Spirit of glonoin; Tridil sublin; Trinitrin Tablets; Trinitrina Erba; Deponit 5; Deponit TTS 10; Deponit TTS 5; Nitrocine 5; Aquo-Trimitrosan; Coro-Nitro; Deponit-5; GTN-Pohl; IMX-150; MED-2002; MQX-503; Mi-Trates; Minitran (TN); NK-843; Natispray (TN); Nit-Ret; Nitrine-TDC; Nitro-Dur 10; Nitro-Dur 5; Nitro-Gesanit Retard; Nitro-Mack Retard; Nitro-Par; Nitro-Pflaster; Nitro-Span; Nitro-Time; Nitro-lent; NitrocapTD; Nitroderm TTS-5; Nitrogard-SR; Nitroglycerin (NG); Nitroglycerin-ACC; Nitrolingual Pump Spray (TN); Nitromist (TN); Nitrong-SR; Nitrospan (TN); Nitrostat (TN); SDM No 17; SK-106N; SK-866; SK-878; Top-Nitro; Transderm Nitro (TN); Transderm-N TTS; Transderm-Nitro TTS; Transiderm-nitro; Tridil (TN); Trinipatch (TN); Trinitrate, Glyceryl; Nitro-Dur (TN); Nitro-M-Bid; Nitro-bid (TN); Transderm-nitro (TN); DWP-401
    Click to Show/Hide
MOA Activator
External Link
 Compound Name Epidermal growth factor Approved [13]
Synonyms
62229-50-9; Urogastrone; Uroenterone; Uroanthelone; Urogastron; Kutrol; beta-Urogastrone; Anthelone U; Urogastrone [JAN]; Gastrone, gamma-uro-; Gastrone, beta-uro- (human); Epidermal growth factor (egf); CCRIS 7234; EINECS 263-468-7; EPIDERMAL GROWTH FACTOR-UROGASTRONE; Gastrone, uro- (9CI); 9010-53-1; Gentel (TN); EGF
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Osimertinib Approved [14]
Synonyms
Tagrisso
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.421 nM
External Link
 Compound Name NERATINIB MALEATE Approved [15]
Synonyms
UNII-9RM7XY23ZS; 9RM7XY23ZS; Neratinib maleate [MI]; hki-272 maleate; Nerlynx (TN); SCHEMBL2180998; MolPort-044-561-003; AKOS030524209; DS-19892
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name Amivantamab Approved [16]
MOA Inhibitor
External Link
 Compound Name SKI-758 Approved [17]
Synonyms
SCHEMBL3992463; CHEMBL219557; BDBM13047; 3-quinolinecarbonitrile analog 10; ANUHLKPVOXDYSK-UHFFFAOYSA-N; 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-{5-[(4-methylpiperazin-1-yl)methyl]furan-3-yl}quinoline-3-carbonitrile; 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6 methoxy-7-{5-[(4-methylpiperazin-1-yl)methyl]-3-furyl}-3-quinolinecarbonitrile
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 230 nM
External Link
 Compound Name Dacomitinib Approved [13]
Synonyms
PF-00299804
    Click to Show/Hide
MOA Antagonist
Activity IC50 = 1.8 nM
External Link
 Compound Name Lapatinib Approved [18]
Synonyms
FMM; Tycerb; Lapatinib Ditosylate; Lapatinib [INN]; Lapatinib tosilate hydrate; GSK 572016; GSK572016; GW 572016; GW 572016X; GW572016; Lapatinib (INN); Tykerb (TN); Lapatinib, Tykerb, GW572016; N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine; N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE; N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-((2-methylsulfonylethylamino)methyl)-2-furyl)quinazolin-4-amine; N-(3-Chloro-4-{[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine; 4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline; Lapatinib (ERBB2 inhibitor)
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3 nM
External Link
 Compound Name Merimepodib Approved [19]
Synonyms
Merimebodib; Merimepodib [USAN:INN]; Tyverb/Tykerb; MMPD; 198821-22-6; 2ZL2BA06FU; C23H24N4O6; CHEMBL304087; MERIMEPODIB, VI-21497, VX-497; UNII-2ZL2BA06FU; VI-21497; VX-497; VX497; Vx 497; carbamic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Vandetanib Approved [20]
Synonyms
Zactima; Vandetanib [INN]; CH 331; ZD 6474; ZD6474; AZD-6474; CH-331; F9995-0087; ZD-6474; Zactima, ZD6474; Vandetanib (JAN/INN); Vandetanib, Zactima, ZD6474; N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine; N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methyl-4-piperidinyl)methoxy)-4-quinazolinamine; N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine; 4-(4-Bromo-2-fluoroanilino)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazoline; Vandetanib (Pan-TK inhibitor)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 200 nM
External Link
 Compound Name Sorafenib Approved [21]
Synonyms
Nexavar; Sorafenibum; Sorafenib [INN]; Nexavar (TN); Sorafenib (INN); N-[4-Chloro-3-(trifluoromethyl)phenyl]-N'-[4-[2-(N-methylcarbamoyl)-4-pyridyloxy]phenyl]urea; N-(4-Chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea; N-(4-chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcar bamoyl)-4-pyridyloxy)phenyl)urea; 4(4-{3-[4-Chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N(sup 2)-methylpyridine-2-carboxamide; 4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-2-pyridinecarboxamide; 4-(4-(3-(4-chloro-3-trifluoromethylphenyl)ureido)phenoxy)pyridine-2-carboxyllic acid methyamide-4-methylbenzenesulfonate; 4-(4-{3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido}phenoxy)-N(sup 2)-methylpyridine-2-carboxamide; 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide; 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide; 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide; 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide; 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE; Sorafenib (Pan-TK inhibitor)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 43.5 nM
External Link
 Compound Name Icotinib hydrochloride Registered [22]
Synonyms
Conmana; Conmanna; Icotinib; BPI-2009-H
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name Rindopepimut Phase 3 [6]
MOA Modulator
External Link
 Compound Name SYM-004 Phase 3 [23]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
    Click to Show/Hide
External Link
 Compound Name DE-766 Phase 3 [13]
MOA Modulator
External Link
 Compound Name EGF816 Phase 3 [24]
MOA Inhibitor
Activity IC50 = 160.6 nM
External Link
 Compound Name CO-1686 Phase 3 [25]
Synonyms
1374640-70-6; AVL-301; CO1686; UNII-72AH61702G; CNX-419; CO-1686 (AVL-301); Rociletinib(AVL-301,CNX-419,CO-1686); 72AH61702G; N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide; CO 1686; Rociletinib (CO-1686, AVL-301); Rociletinib [USAN:INN]; Tube721; Rociletinib (USAN/INN); Rociletinib (CO-1686); SCHEMBL4177736; GTPL7966; CHEMBL3545308; EX-A228; MolPort-035-395-816; C27H28F3N7O3; HMS3653G08; BDBM149404; BCP07085; AOB87314; ZINC98043800; s7284
    Click to Show/Hide
MOA Modulator
Activity IC50 = 1.6 nM
External Link
 Compound Name Zalutumumab Phase 3 [13]
External Link
 Compound Name Almonertinib Phase 3 [26]
Synonyms
HS-10296; Ameile; 1899921-05-1; Egfr T790M inhibitor HS-10296; N-(5-((4-(1-Cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide; UNII-T4RS462G19; SCHEMBL17683063; GTPL11136; T4RS462G19; EX-A3721; HS 10296 [WHO-DD]; s8817; HS10296; example 26 [WO2016054987A1]; HY-112823; CS-0066162; 2-Propenamide, N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)-2-pyrimidinyl)amino)-2-((2-(dimethylamino)ethyl)methylamino)-4-methoxyphenyl)-; C1(CC1)N1C=C(C2=CC=CC=C12)C1=NC(=NC=C1)NC=1C(=CC(=C(C=1)NC(C=C)=O)N(C)CCN(C)C)OC; N-[5-[[4-(1-cyclopropylindol-3-yl)pyrimidin-2-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]-4-methoxyphenyl]prop-2-enamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name ASP1929 Phase 3 [27]
Synonyms
Cetuximab sarotalocan
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name A140 Phase 3 [28]
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [29]
MOA Inhibitor
External Link
 Compound Name HKI-272 Phase 3 [30]
Synonyms
Neratinib (ERBB2 inhibitor)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.08 nM
External Link
 Compound Name Indium-111 Phase 2/3 [31]
Synonyms
ABT-806
    Click to Show/Hide
External Link
 Compound Name Varlitinib Phase 2/3 [32]
Synonyms
845272-21-1; ARRY-334543; ARRY334543; ARRY 334543; ARRY-543; UNII-846Y8197W1; ASLAN-001; 846Y8197W1; (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine; Varlitinib [USAN:INN]; Varlitinib (ARRY334543); Varlitinib free base; Varlitinib (USAN/INN); MLS006011274; GTPL7645; SCHEMBL1384578; CHEMBL2103842; SYN1192; MolPort-028-720-424; EX-A1005; 4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
    Click to Show/Hide
MOA Modulator
Activity IC50 = 7 nM
External Link
 Compound Name ASP8273 Phase 2 [33]
MOA Inhibitor
Activity IC50 = 8 nM
External Link
 Compound Name ABT-414 Phase 2 [34]
External Link
 Compound Name Depatuxizumab Phase 2 [35]
MOA Antagonist
External Link
 Compound Name Matuzumab Phase 2 [36]
Synonyms
EMD-62000; EMD-72000; Anti-EGF receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-EGFR humanized mAb (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-epidermal growth factor receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals
    Click to Show/Hide
External Link
 Compound Name HER1-VSSP vaccine Phase 2 [37]
Synonyms
HER1-VSSP vaccine (cancer)
    Click to Show/Hide
External Link
 Compound Name RM-1929 Phase 2 [38]
MOA Antagonist
External Link
 Compound Name CetuGEX Phase 2 [39]
External Link
 Compound Name ABX-EGF Phase 2 [40]
External Link
 Compound Name Pelitinib Phase 2 [41]
Synonyms
EKB-569; EKI-569; WAY-EKB-569
    Click to Show/Hide
MOA Modulator
Activity IC50 = 8.02 nM
External Link
 Compound Name HM-78136B Phase 2 [38]
Synonyms
Pan-Her/EGFR inhibitors (cancer), Hanmi
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.218 nM
External Link
 Compound Name Pazopanib + Tyverb/Tykerb Phase 2 [19]
MOA Inhibitor
External Link
 Compound Name MEHD-7945A Phase 2 [32]
Synonyms
RG-7597; EGFR/HER3 dual monoclonal antibody, Genentech
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name TT-100 Phase 2 [42]
Synonyms
TT-100, TriAct; Dual IGF-1/EGFR inhibitor (non-small-cell lung cancer), TriAct
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BMS-599626 Phase 2 [43]
Synonyms
714971-09-2; AC480; AC-480; BMS 599626; (S)-Morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate; UNII-2252724U5N; CHEMBL1645462; BMS599626; AC480 (BMS-599626); 2252724U5N; J-502499; C27H27FN8O3; AC 480; AC1480 (free base); PubChem22432; GTPL7647; SCHEMBL12065349; CTK8B6780; DTXSID60221714; SYN1142; AOB5594; MolPort-023-279-418; EX-A2296; ZINC6717782; KS-000008GE; BDBM50333373; s1056; C27H44O11; ANW-54337; AKOS015999853; CS-0407; RL05125; BCP9000428; SB21703
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 32 nM
External Link
 Compound Name Tarloxotinib Phase 2 [44]
Synonyms
Tarloxotinib cation; UNII-H8768UL06V; H8768UL06V; [(E)-4-[[4-(3-bromo-4-chloroanilino)pyrido[3,4-d]pyrimidin-6-yl]amino]-4-oxobut-2-enyl]-dimethyl-[(3-methyl-5-nitroimidazol-4-yl)methyl]azanium; Tarloxotinib ion; GTPL9409; CHEMBL4297661; SCHEMBL19733352; PR610; DB14944; TH-4000; Q27279755; 1636938-13-0
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name VATALANIB Phase 2 [30]
Synonyms
212141-54-3; Vatalanib base; N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine; PTK787; Pynasunate; CGP 79787; Vatalanib free base; PTK-787; Vatalanib (free base); Vatalinib; ZK-232934; CGP-79787; ZK222584; PTK/ZK; CHEMBL101253; N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine; UNII-5DX9U76296; CHEBI:90620; YCOYDOIWSSHVCK-UHFFFAOYSA-N; 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazine; 5DX9U76296; NCGC00181350-01; 1-Phthalazinamine,N-(4-chlorophenyl)-4-(4-pyridinylmethyl)-; DSSTox_CID_26919
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 457.7 nM
External Link
 Compound Name BMS-690514 Phase 2 [45]
Synonyms
BMS 690514; BMS690514
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CI-1033 Phase 2 [20]
Synonyms
Canertinib; Canertinib HCl; Canertinib dihydrochloride; Canertinib dihydrochloride [USAN]; CI1033; PD 183805; Canertinib dihydrochloride (USAN); PD-0183805; PD-183805; Canertinib, PD-183805, CI1033, PD183805; N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide dihydrochloride; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide dihydrochloride; N-(4-(3-chloro-4-fluorophenyl)amino)-7-(3-morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide dihydrochloride; N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide; N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl) amino)-7-(3-(4-morpholinyl) propoxy)-6-quinazolinyl)-, dihydrochloride; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-(4-morpholinyl)propoxy)-6-quinazolinyl)-, dihydrochloride
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.11 nM
External Link
 Compound Name CART-EGFR Phase 1/2 [46]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name SN-32793 Phase 1/2 [13]
Synonyms
PR-509; PR-610; SN-32807; Hypoxia-activated irreversible pan-erbb inhibitors, Proacta; Hypoxia-selective multi-kinase inhibitors (NSCLC resistant to reversible tyrosine kinase inhibitor/cancer); Hypoxia-selective multi-kinase inhibitors (lung cancer), Proacta; Hypoxia-selective multi-kinase inhibitors(lung cancer), Proacta/ Yakult Honsha; Hypoxia-selective multi-kinase inhibitors (NSCLC resistant to reversible tyrosine kinase inhibitor/cancer), Proacta/ Yakult Honsha
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name EGFR CART Phase 1/2 [47]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name EMD 55900 Phase 1/2 [40]
Synonyms
27686-84-6; 4,4'-((2R,3S)-2,3-Dimethylbutane-1,4-diyl)bis(benzene-1,2-diol); UNII-7BO8G1BYQU; 1,2-Benzenediol, 4,4'-(2,3-dimethyl-1,4-butanediyl)bis-, (R*,S*)-; EINECS 248-606-6; 7BO8G1BYQU; CHEMBL313972; erythro-nordihydroguaiaretic acid; CHEBI:73468
    Click to Show/Hide
External Link
 Compound Name TAK-186 Phase 1/2 [48]
MOA Inhibitor
External Link
 Compound Name ZN-e4 Phase 1/2 [49]
MOA Inhibitor
External Link
 Compound Name EMB-01 Phase 1/2 [50]
MOA Inhibitor
External Link
 Compound Name Sym015 Phase 1/2 [35]
MOA Antagonist
External Link
 Compound Name BDTX-189 Phase 1/2 [51]
Synonyms
2414572-47-5; EX-A4379
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name AFM24 Phase 1/2 [52]
External Link
 Compound Name Sym013 Phase 1/2 [35]
MOA Antagonist
External Link
 Compound Name S-222611 Phase 1b [53]
MOA Inhibitor
External Link
 Compound Name SYN004 Phase 1 [35]
MOA Inhibitor
External Link
 Compound Name BIBX-1382 Phase 1 [54]
Synonyms
Falnidamol; BIBX 1382; 196612-93-8; BIBX1382; UNII-0MU316797D; CHEMBL258940; FTFRZXFNZVCRSK-UHFFFAOYSA-N; 0MU316797D; N8-(3-Chloro-4-fluorophenyl)-N2-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-2,8-diamine; Bibx 1382bs; Falnidamol [INN]; NCGC00161422-01; AC1OCFIP; BIBX-1382BX; BIBX-1382BS; SCHEMBL158563; GTPL7646; DTXSID0048399; CHEBI:93243; EX-A570; AOB5489; MolPort-039-136-623; ZINC1494443; KS-00001CR9; BCP09515; BDBM50375639; AKOS025396660; API0007916; DB12966; CS-0691; NCGC00161422-03; AS-16894; HY-10322; AK174047
    Click to Show/Hide
MOA Antagonist
Activity IC50 = 3 nM
External Link
 Compound Name IMGN289 Phase 1 [55]
MOA Inhibitor
External Link
 Compound Name AST-1306 Phase 1 [56]
Synonyms
Allitinib; Allitinib tosylate
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name AMG 595 Phase 1 [57]
MOA Modulator
External Link
 Compound Name HER-2/HER-1 vaccine Phase 1 [13]
Synonyms
HER-2/HER-1 vaccine (solid tumors)
    Click to Show/Hide
External Link
 Compound Name EGFR806-specific CAR T cell Phase 1 [58]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name PF-05230907 Phase 1 [59]
MOA Inhibitor
External Link
 Compound Name MR1-1 Phase 1 [60]
Synonyms
MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Anti-EGFR CAR T Phase 1 [61]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name AP32788 Phase 1 [38]
MOA Inhibitor
External Link
 Compound Name CLN-081 Phase 1 [62]
MOA Inhibitor
External Link
 Compound Name LY3164530 Phase 1 [63]
MOA Modulator
External Link
 Compound Name MM-151 Phase 1 [35]
MOA Antagonist
External Link
 Compound Name Cipatinib Phase 1 [32]
Synonyms
HER-1/HER-2 inhibitor (oral, cancer), Jiangsu Hengrui
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Anti-HER3/EGFR DAF Phase 1 [64]
MOA Modulator
External Link
 Compound Name BCA101 Phase 1 [65]
MOA Inhibitor
External Link
 Compound Name CUDC-101 Phase 1 [66]
Synonyms
1012054-59-9; CUDC 101; CUDC101; 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide; UNII-1A7Y9MP123; CHEMBL598797; 1A7Y9MP123; 7-[[4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl]oxy]-N-hydroxyheptanamide; AK174946; 7-((4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl)oxy)-N-hydroxyheptanamide; 7-({4-[(3-ethynylphenyl)amino]-7-methoxyquinazolin-6-yl}oxy)-N-hydroxyheptanamide; 7-((4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)oxy)-N-hydroxyheptanamide; PubChem19149
    Click to Show/Hide
MOA Modulator
Activity IC50 = 2.4 nM
External Link
 Compound Name SI-B001 Phase 1 [67]
External Link
 Compound Name CX-904 Phase 1 [68]
Synonyms
AMG 651
    Click to Show/Hide
External Link
 Compound Name AZD9592 Phase 1 [69]
External Link
 Compound Name D2C7 Phase 1 [70]
External Link
 Compound Name MCLA-158 Phase 1 [71]
MOA Inhibitor
External Link
 Compound Name JNJ-26483327 Phase 1 [72]
Synonyms
MTKI (cancer), J&J; MTKI (cancer), Johnson & Johnson; Multi-targeted kinase inhibitor (cancer), J&J; Multi-targeted kinase inhibitor (cancer), Johnson & Johnson
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyrrolo[2,3-d]pyrimidine derivative 24 Patented [73]
Synonyms
PMID28705083-Compound-22
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PKI166 Discontinued in Phase 2 [74]
Synonyms
PKI-166; CGP-75166; 187724-61-4; NVP-PKI166; CHEMBL1914653; AC1OCFE0; UNII-9RIE5HW38P; 9RIE5HW38P; SCHEMBL177814; GTPL7642; CHEMBL1963502; ZINC23255; AOB1619; PKI-75166; BDBM50358046; NCGC00387215-02; AS-16676; KB-275097; PKI-166, > 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[4,5-e]pyrimidin-6-yl]phenol
    Click to Show/Hide
MOA Modulator
Activity IC50 = 3.7 nM
External Link
 Compound Name RG7160 Discontinued in Phase 2 [75]
MOA Modulator
External Link
 Compound Name PD-153035 Discontinued in Phase 1 [76]
Synonyms
183322-45-4; PD153035 hydrochloride; N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride; PD153035 HCl; PD 153035 HYDROCHLORIDE; PD-153035 hydrochloride; PD153035 (Hydrochloride); Tyrphostin AG 1517; AG 1517 hydrochloride; SU-5271 hydrochloride; UNII-AHJ252P69N; ZM 252868; SU 5271; AG 1517; 4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE; AHJ252P69N; pd 153035; PD153035.HCl; CHEMBL1204168; 6,7-Dimethoxy-4-[N-(3-bromophenyl)amino]quinazoline hydrochloride; C16H15BrClN3O2; 4-Quinazolinamine, N-(3-bromo
    Click to Show/Hide
MOA Modulator
Activity Ki = 0.006 nM
External Link
 Compound Name AZD4769 Discontinued in Phase 1 [77]
Synonyms
Acetic acid, ((4-phenyl-1-(4-(2-quinolinylmethoxy)phenyl)butyl)thio)-; 127481-29-2; L-674573; ((4-Phenyl-1-(4-(2-quinolinylmethoxy)phenyl)butyl)thio)acetic acid; {[4-phenyl-1-(4-(2-quinolinylmethoxy)phenyl)butyl]thio}acetic acid; L 674573; L-674,573; AC1L3YFJ; SCHEMBL9460146; CHEMBL422872; JOIXGLLMSDPZDN-UHFFFAOYSA-N; AZD-4769; 2-[[4-phenyl-1-[4-(2-quinolinylmethoxy)phenyl]butyl]thio]Acetic acid; DA-13018; FT-0734991; AZ-12096971; 2-[4-phenyl-1-[4-(quinolin-2-ylmethoxy)phenyl]butyl]sulfanylacetic
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name TAK165 Discontinued in Phase 1 [20]
Synonyms
Mubritinib; TAK 165; Mubritinib (USAN/INN); 4-[[4-[4-(triazol-1-yl)butyl]phenoxy]methyl]-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 111In-hEGF Preclinical [78]
Synonyms
Indium-111-hEGF; Indium-111-labeled human epithelial growth factor (breast cancer), University of Toronto; 111In-labeledhuman epithelial growth factor (breast cancer), University of Toronto
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name EGFR/IGFR tandem adnectin Preclinical [79]
Synonyms
BMS-964210
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Heparin-EGF-like factor Terminated [80]
Synonyms
HB-EGF, Scios Nova; Heparin-EGF-like factor, Scios Nova
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name CGP-52411 Terminated [81]
Synonyms
DAPH
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 160 nM
External Link
 Compound Name CGP-53353 Terminated [82]
Synonyms
145915-60-2; CGP 53353; DAPH 2; DAPH-7; CGP53353; PKCbetaII/EGFR Inhibitor; 5,6-BIS[(4-FLUOROPHENYL)AMINO]-1H-ISOINDOLE-1,3(2H)-DIONE; CHEMBL7939; CGP 53 353; 4,5-bis(4-Fluoroanilino)-phthalimide; CG53353; 5,6-Bis((4-fluorophenyl)amino)isoindoline-1,3-dione; 5,6-Bis[(4-fluorophenyl)amino]-2H-isoindole-1,3-dione; 4,5-Bis(4-fluoroanilino)phthalimide; 4,5-Bis[4-fluoroanilino]phthalimide; PKCbII/EGFR Inhibitor; AC1O8KXF; 5,6-bis(4-fluoroanilino)isoindole-1,3-dione; MolMap_000016; DAPH-2; CGP-53353, solid; SCHEMBL230492
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 700 nM
External Link
 Compound Name AZD-9935 Terminated [83]
MOA Antagonist
External Link
 Compound Name N4-(3-chlorophenyl)quinazoline-4,6-diamine Investigative [84]
Synonyms
CHEMBL343352; Anilinoquinazoline, 4c; SCHEMBL1262804; AWAYNEMCHILZCF-UHFFFAOYSA-N; ZINC13527446; BDBM50133382; AKOS013915036; 6-amino-4-(3'-chloroanilino)quinazoline; N4-(3-chlorophenyl)-4,6-quinazolinediamine; 6-amino-4[(3-chlorophenyl)amino]quinazoline
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3.38 nM
External Link
 Compound Name 2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile Investigative [85]
Synonyms
Tyrphostin deriv. 29; AC1NS5AC; CHEMBL56132; BDBM4296; ZINC12352646; 2-(Benzoyl)-3-(3,4-dihydroxyphenyl)acrylonitrile; (E)-2-benzoyl-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name 6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline Investigative [86]
Synonyms
CHEMBL250523; BDBM50222432
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name 2-cyano-3-(3,4-dihydroxyphenyl)acrylamide Investigative [85]
Synonyms
Tyrphostin 46; Tyrphostin A46; AG 99; Tyrphostin B40; 122520-85-8; alpha-Cyano-(3,4-dihydroxy)cinnamide; AG-99; 3,4-Dihydroxy-alpha-cyanocinnamamide; UNII-ARL2OF9022; CHEMBL296407; ARL2OF9022; 118409-59-9; Tyrphostin AG 99; (E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide; NSC666250; NSC-666250; 2-Propenamide, 2-cyano-3-(3,4-dihydroxyphenyl)-; (~{E})-3-[3,4-bis(oxidanyl)phenyl]-2-cyano-prop-2-enamide; Tyrphostin AG99; 3,4-Dihydroxy-alpha-cyanocinnamide; NSC 666250; Tocris-0497; Tyrphostin deriv. 40; BiomolKI_000013; AC1NS5AR
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3500 nM
External Link
 Compound Name HM-61713B Investigative [13]
Synonyms
EGFR mutant selective inhibitor (cancer), Hanmi; EMSI (cancer), Hanmi
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Benzyl-quinazolin-4-yl-amine Investigative [87]
Synonyms
N-Benzylquinazolin-4-amine; N-benzyl-N-(4-quinazolinyl)amine; 4-(Benzylamino)quinazoline; 100818-54-0; 4-Benzylaminoquinazoline; AC1LDDI3; benzylquinazolin-4-ylamine; ChemDiv2_003678; N-benzyl-4-quinazolineamine; Oprea1_089836; MLS000701321; N-Benzyl-4-quinazolinamine #; cid_616573; CHEMBL102726; BDBM3256; SCHEMBL7612718; CHEBI:92768; MolPort-001-960-903; FVWANTDQRFSCAL-UHFFFAOYSA-N; HMS2233F15; HMS3373H15; HMS1379H04; ZINC109589; 4-[(phenylmethyl)amino]quinazoline; N-(phenylmethyl)-4-quinazolinamine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6,7-diethoxy-4-styrylquinazoline Investigative [86]
Synonyms
CHEMBL250925
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name AFM-21 Investigative [13]
Synonyms
Anti-EGFR antibody (RECRUIT-TandAb, colon/solid tumors), Affimed
    Click to Show/Hide
External Link
 Compound Name PD182905 Investigative [88]
MOA Inhibitor
External Link
 Compound Name AG 112 Investigative [89]
Synonyms
tyrphostin A48; tyrphostin AG 112; AG-112; AG112
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 125 nM
External Link
 Compound Name 2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile Investigative [90]
Synonyms
(4,5-Dihydroxyindanylidene)malononitrile; Tyrphostin deriv. 17; AC1NS59O; CHEMBL57300; BDBM4286; 133550-13-7; 2-(4,5-dihydroxy-2,3-dihydroinden-1-ylidene)propanedinitrile; 2-(4,5-dihydroxy-2,3-dihydro-1H-inden-1-ylidene)propanedinitrile
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7000 nM
External Link
 Compound Name (3-Bromo-phenyl)-quinazolin-4-yl-amine Investigative [91]
Synonyms
N-(3-bromophenyl)quinazolin-4-amine; CHEMBL290096; AC1LEF72; SCHEMBL2992623; BDBM3264; 4-Anilino quinazoline deriv. 15; ZINC151213; (3-bromophenyl)quinazolin-4-ylamine; N-(3-Bromophenyl)-4-quinazolinamine; AKOS002264782; MCULE-4660970870; 4-Quinazolinamine, N-(3-bromophenyl)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 27 nM
External Link
 Compound Name PD-158780 Investigative [92]
Synonyms
171179-06-9; PD158780; pd 158780; N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine; AC1L1IRV; CHEMBL53753; 4-N-(3-bromophenyl)-6-N-methylpyrido[3,4-d]pyrimidine-4,6-diamine; AK160389; 4-(3-bromoanilino)-6-methylaminopyrido[3,4-d]pyrimidine; 4-[(3-bromophenyl)amino]-6-(methylamino)pyrido[3,4-d]pyrimidine; 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine; Pyrido[3,4-d]pyrimidine-4,6-diamine, N4-(3-bromophenyl)-N6-methyl-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.008 nM
External Link
 Compound Name EGFR inhibitor Investigative [93]
Synonyms
879127-07-8; CHEMBL387187; N-(3-((6-((3-(Trifluoromethyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)cyclopropanecarboxamide; Cyclopropanecarboxylic acid-(3-(6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino)-phenyl)-amide; K00598a; N-{3-[(6-{[3-(trifluoromethyl)phenyl]amino}pyrimidin-4-yl)amino]phenyl}cyclopropanecarboxamide; EGFR Inhibitor 324674; SCHEMBL242230; GTPL5963; CTK8E9808; DTXSID40429554; MolPort-042-665-758; HMS3229E03; BDBM50200394; ZINC13831337; API0010446; CCG-206749; NCGC00167954-01
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 21 nM
External Link
 Compound Name 6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline Investigative [86]
Synonyms
CHEMBL399371
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name LA22-radioimmunoconjugates Investigative [13]
Synonyms
LA22-radioimmunoconjugates (cancer); Lutetium177-DOTA-LA22; LA22-radioimmunoconjugates (cancer), Welson/PekingUniversity; MAb-conjugated radioimmunotherapeutics (cancer), Welson/Peking University; 177Lu-DOTA-LA22; 177Lu-DTPA-LA22
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Investigative [94]
Synonyms
CHEMBL382537
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name ICR 62 Investigative [40]
External Link
 Compound Name Bmab-200 Investigative [13]
Synonyms
Anti-EGFR mAb (cancer), Biocon; Anti-epidermal growth factor receptor monoclonal antibody (cancer), Biocon
    Click to Show/Hide
External Link
 Compound Name HTS-00213 Investigative [95]
Synonyms
CHEMBL461781; AC1MDDFE; MolPort-002-900-007; ZINC1028479; BDBM50292742; MCULE-3257779074; 3-((2,6-dichlorophenoxy)methyl)-5-((4-(4-(trifluoromethyl)phenyl)-4H-1,2,4-triazol-3-ylthio)methyl)-1,2,4-oxadiazole
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 6300 nM
External Link
 Compound Name 6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline Investigative [86]
Synonyms
CHEMBL251123
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine Investigative [92]
Synonyms
CHEMBL300083; 4-N-benzylpyrido[4,3-d]pyrimidine-4,7-diamine; 7-Aminopyrido[4,3-d]pyrimidine 8a; AC1NS3PZ; SCHEMBL6839398; BDBM3331; pyrido[4,3-d]pyrimidine-4,7-diamine,n4-(phenylmethyl)-; ZINC3815364; 171178-89-5; PD-69896; KB-302882
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 578 nM
External Link
 Compound Name Epitinib Investigative [13]
Synonyms
HMPL-813; EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name OSI-75 Investigative [96]
MOA Inhibitor
External Link
 Compound Name (E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin Investigative [97]
Synonyms
CHEMBL213560; SCHEMBL16693054; BDBM50187134
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 710 nM
External Link
 Compound Name HTS-02876 Investigative [95]
Synonyms
AC1MDGL2; CHEMBL460914; MolPort-002-900-576; ZINC1030761; MCULE-7093116609
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile Investigative [90]
Synonyms
133550-11-5; Propanedinitrile, (2,3-dihydro-5,6-dihydroxy-1H-inden-1-ylidene)-; Tyrphostin deriv. 15; ACMC-20muzh; AC1NS59I; SCHEMBL6285970; CHEMBL293584; BDBM4284; CTK0C0328; DTXSID30416170; 2-(5,6-dihydroxy-2,3-dihydroinden-1-ylidene)propanedinitrile; (5,6-Dihydroxyindanylidene)malononitrile; [(2,3-Dihydro-5,6-dihydroxy-1H-inden)-1-ylidene]malononitrile
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name PMID8568816C56 Investigative [98]
Synonyms
PD153035 Analog 56; 171745-13-4; AC1L1EMN; K00042; BDBM3556; GTPL5956; CTK6G1384; DTXSID40274389; MolPort-019-910-218; HMS3229C09; BCP08039; ZINC2572485; IN1496; CCG-206742; QC-8197; ACM171745134; RT-012080; SR-02000000170; SR-02000000170-1; J-010
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.006 nM
External Link
 Compound Name MT-062 Investigative [13]
Synonyms
EGFR inhibitor (melanoma), Medisyn Technologies
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Anti-EGFR mab Investigative [13]
External Link
 Compound Name RG-50810 Investigative [85]
Synonyms
Tyrphostin 23; 118409-57-7; Tyrphostin A23; AG 18; (3,4-Dihydroxybenzylidene)malononitrile; AG-18; Tyrphostin AG18; Tyrphostin RG50810; 2-(3,4-dihydroxybenzylidene)malononitrile; UNII-RV0GCD31OJ; alpha-Cyano-(3,4-dihydroxy)cinnamonitrile; 2-[(3,4-dihydroxyphenyl)methylidene]propanedinitrile; RG 50810; Propanedinitrile,2-[(3,4-dihydroxyphenyl)methylene]-; ag18; (3,4-Dihydroxyphenyl)methylene propanedinitrile; RV0GCD31OJ; C10H6N2O2; NCGC00016043-03; (3,4-dihydroxybenzylidene)propanedinitrile; DSSTox_CID_25215
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11000 nM
External Link
 Compound Name IPS-01003 Investigative [13]
Synonyms
EGFR kinase antagonist (cancer), InnoPharmaScreen
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name RM-6427 Investigative [13]
Synonyms
RM-6428; EGFR tyrosine kinase inhibitors (parasitic infection), Romark
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine Investigative [91]
Synonyms
bpdq; CHEMBL328216; 4-N-(3-bromophenyl)quinazoline-4,6,7-triamine; 4-[(3-Bromophenyl)amino]-6,7-diaminoquinazoline; 169205-87-2; AC1L1DNE; N4-(3-bromophenyl)-4,6,7-Quinazolinetriamine; K00041; SCHEMBL7221302; BDBM3303; 4-Anilinoquinazoline deriv. 54; CTK8F8323; ADXSZLCTQCWMTE-UHFFFAOYSA-N; IN1401; HSCI1_000040; AKOS025149794; 4-(3-bromoanilino)-6,7-diaminoquinazoline; N-(3-Bromophenyl)quinazoline-4,6,7-triamine; 4[ (3-Bromophenyl)aminol-6,7-diaminoquinazoline; J-010514
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.12 nM
External Link
 Compound Name 3-Pyridin-4-yl-quinoline-6,7-diol Investigative [99]
MOA Inhibitor
Activity IC50 = 5000 nM
External Link
 Compound Name AGT-2000 Investigative [13]
Synonyms
Gene therapy (intravenous, brain cancer), ArmaGen
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one Investigative [100]
Synonyms
CHEMBL7827; SCHEMBL3355884; 62845-10-7; CTK2B1467; ZINC23489; DTXSID10445847; BDBM50074745; AKOS030553076; 5,7-Dihydroxy-3-(3-chlorophenyl)-4H-1-benzopyran-4-one; 4H-1-Benzopyran-4-one, 3-(3-chlorophenyl)-5,7-dihydroxy-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 95 nM
External Link
 Compound Name ON-128 Investigative [13]
Synonyms
ON-128060; ON-128 series (cancer); HER1/EGFR inhibitors (cancer), Onconova; Human epidermal growth factor receptor 1/epidermal growth factor receptor inhibitors (cancer), Onconova; ON-128 series (cancer), Onconova
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name FHT-2107 Investigative [13]
Synonyms
EGFR-targeting siRNA agent, ForHumanTech
    Click to Show/Hide
External Link
 Compound Name GI-3000 Investigative [13]
Synonyms
GI-3001; GI-6200; GlioVax-1; EGFR-expressing Saccharomyces cerevisiae-based cancer vaccine (Tarmogen); EGFR-expressing Saccharomyces cerevisiae-based cancer vaccine (Tarmogen), GlobeImmune
    Click to Show/Hide
External Link
 Compound Name 6,7-dimethoxy-N-m-tolylquinazolin-4-amine Investigative [95]
Synonyms
CHEMBL56802; AC1MDC5E; Oprea1_570563; SCHEMBL5482883; ZINC5857; 4-Quinazolinamine,6,7-dimethoxy-N-(3-methylphenyl)-; MolPort-001-734-434; BDBM50102093; MCULE-3929709513; 666839-07-2; (6,7-Dimethoxy-quinazolin-4-yl)-m-tolyl-amine; SR-02000000178; SR-02000000178-1; 6,7-dimethoxy-N-(3-methylphenyl)quinazolin-4-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4.6 nM
External Link
 Compound Name 5,6-Bis-p-tolylamino-isoindole-1,3-dione Investigative [82]
Synonyms
CHEMBL7914; SCHEMBL8834183; BDBM50040920
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4500 nM
External Link
 Compound Name HTS-05058 Investigative [93]
Synonyms
MLS000327715; SMR000180717; 3-(1H-imidazol-5-ylmethylene)-1,3-dihydro-2H-indol-2-one; (3Z)-3-(1H-imidazol-5-ylmethylidene)-1H-indol-2-one; Angiogenesis Inhibitor; 372164-79-9; AC1NWWY9; CHEMBL261692; SCHEMBL2998484; REGID_for_CID_667701; BDBM41079; cid_5714572; REGID_for_CID_5714572; MolPort-002-870-304; MolPort-002-901-109; HMS2463B12; ZINC4693510; AKOS015992864; (3Z)-3-(1H-imidazol-5-ylmethylene)oxindole; 4X-0884; J-011988
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide Investigative [101]
Synonyms
CHEMBL297968; SCHEMBL2994207; FAGJCAQBJKSOOS-UHFFFAOYSA-N; BDBM50077245; N-[4-(3-Methylanilino)quinazoline-7-yl]acrylamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 90 nM
External Link
 Compound Name 4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid Investigative [85]
Synonyms
CHEMBL76958; BDBM50007075; 4-[4-(2-Nitro-vinyl)-phenoxysulfonyl]-benzoic acid; 4-[4-[(E)-2-Nitroethenyl]phenoxysulfonyl]benzoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine Investigative [91]
Synonyms
CHEMBL63786; N-(3-bromophenyl)benzo[g]quinazolin-4-amine; Benzoquinazoline deriv. 23; AC1NS43R; SCHEMBL4348523; BDBM3585; BUVKJPOCMOXSSQ-UHFFFAOYSA-; ZINC3815025; 4-[(3-Bromophenyl)amino]benzo[g]quinazoline; N-(3-Bromophenyl)benzo[g]quinazoline-4-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.003 nM
External Link
 Compound Name ARX-AHD Investigative [13]
Synonyms
Dolastatin-conjugated HER2 antibody (breast cancer), Ambrx
    Click to Show/Hide
External Link
 Compound Name TGF alpha Investigative [13]
Synonyms
TGF alpha (neurological damage)
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name AG 9 Investigative [89]
Synonyms
tyrphostin 1; tyrphostin A1; AG9; AG-9
    Click to Show/Hide
MOA Inhibitor
Activity Ki > 400000 nM
External Link
 Compound Name N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine Investigative [102]
Synonyms
N4-(3-Bromophenyl)quinazoline-4,6-diamine; 169205-78-1; 4-N-(3-bromophenyl)quinazoline-4,6-diamine; CHEMBL52765; AK-25174; N4-(3-bromophenyl)-4,6-quinazolinediamine; 4,6-Quinazolinediamine, N4-(3-bromophenyl)-; C14H11BrN4; nchembio866-comp32; Anilinoquinazoline, 4b; AC1NS3N2; BDBM3294; SCHEMBL1417740; 4-Anilinoquinazoline deriv. 45; KS-00000HMR; CTK4D3225; DTXSID40416141; IZQHULBHKPGOAP-UHFFFAOYSA-N; MolPort-009-198-483; ZINC3815034; BCP18882; ANW-50332; AKOS013915836; 6-amino 4-(3-bromoanilino)quinazoline; GS-4221
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.78 nM
External Link
 Compound Name 4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline Investigative [103]
Synonyms
CHEMBL473320; SCHEMBL5616932
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 131 nM
External Link
 Compound Name Theliatinib Investigative [13]
Synonyms
HMPL-309; Second EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-(3-Bromo-phenylamino)-quinazoline-6,7-diol Investigative [91]
MOA Inhibitor
External Link
 Compound Name 6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline Investigative [86]
Synonyms
CHEMBL250318; BDBM50222435
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 14 nM
External Link
 Compound Name 4-(2-nitroprop-1-enyl)benzene-1,2-diol Investigative [85]
Synonyms
13662-96-9; 1,2-Benzenediol, 4-(2-nitro-1-propenyl)-; AC1MMGH2; Oprea1_551147; CTK0F3796; DTXSID20390758; AKOS017269192
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name EDP-13 Investigative [13]
Synonyms
Epidermal growth factor receptor antagonist (cancer), BiolineRx/Matrix Pharma
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine Investigative [87]
Synonyms
CHEMBL420624; 7-amino-4-[(3-bromophenyl)amino]quinazoline; 4-N-(3-bromophenyl)quinazoline-4,7-diamine; 4-Anilinoquinazoline deriv. 48; AC1NS3NB; BDBM3297; SCHEMBL2986298; GHVBIROTJQDRQB-UHFFFAOYSA-N; ZINC3815072; AKOS014671983; 7-Amino-4-(3-bromoanilino)quinazoline; 7-amino-4(3-bromoanilino)-quinazoline; 7-amino-4-(3-bromoanilino)-quinazoline; 169205-81-6; N-(3-Bromophenyl)quinazoline-4,7-diamine; 7-Amino-4-[(3-bromophenyl)aminolquinazoline; FT-0768311; 7-amino-4-[(3-bromophenyl)-amino]quinazoline
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.1 nM
External Link
 Compound Name (S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate Investigative [85]
Synonyms
Z-L-Ala-chloromethylketone; 41036-43-5; Benzyloxycarbonylalanine chloromethyl ketone; Z-Ala-chloromethyl ketone; AC1NUSRJ; PubChem11548; Benzyloxycarbonyl-ala-chloromethyl ketone; CHEMBL483443; SCHEMBL6437509; DTXSID50194009; ZINC34206665; AKOS027382196; FT-0603930; benzyl N-[(2S)-4-chloro-3-oxobutan-2-yl]carbamate; [(S)-1-Methyl-2-oxo-3-chloropropyl]carbamic acid benzyl ester; Carbamic acid, (3-chloro-1-methyl-2-oxopropyl)-, phenylmethyl ester, (S)-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-(2-nitrovinyl)benzene-1,2-diol Investigative [85]
Synonyms
SL-1; CHEMBL78224; 108074-44-8; SL-1 Pigment; 1,2-Dihydroxy-4-(nitroethenyl)benzene; 4-[(E)-2-nitroethenyl]benzene-1,2-diol; AC1O5R3K; SCHEMBL2052283; SCHEMBL2052285; beta-Nitro-3,4-dihydroxystyrene; LLJASJHXECDHOM-ONEGZZNKSA-N; BDBM50007069; AKOS010878666; 4-(2-Nitro-vinyl)-benzene-1,2-diol; 1,2-Benzenediol, 4-(2-nitroethenyl)-, (E)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 8800 nM
External Link
 Compound Name AG-538 Investigative [85]
Synonyms
Tyrphostin AG 538; AG 538; NSC676485; (E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile; alpha-Cyano-(3,4-dihydroxy)cinnamoyl-(3& -dihydroxyphenyl)ketone; Tyrphostin deriv. 24; Lopac-T-7822; AC1NS5A3; Lopac0_001261; MLS002153408; CHEMBL56393; SCHEMBL2678764; SCHEMBL2678765; BDBM4293; REGID_for_CID_660907; CHEBI:92138; cid_5328760; REGID_for_CID_5328760; HMS3263N04; HMS2233K10; ZINC3871438; 133550-18-2; Tox21_501261; HSCI1_000189; CCG-205335; NSC-676485; LP01261; NCGC00094499-02
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 370 nM
External Link
 Compound Name WZ-3146 Investigative [13]
Synonyms
WZ-4002; WZ-8040; EGFR-T790M kinase inhibitors (lung cancer); EGFR-T790M kinase inhibitors (lung cancer), Gatekeeper Pharmaceuticals
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-methoxy-4-(2-nitrovinyl)phenol Investigative [85]
Synonyms
6178-42-3; 2-Methoxy-4-[(E)-2-nitroethenyl]phenol; 1-(4-HYDROXY-3-METHOXYPHENYL)-2-NITROETHENE; (E)-2-methoxy-4-(2-nitrovinyl)phenol; trans-4-Hydroxy-3-methoxy-beta-nitrostyrene; 2-methoxy-4-[(E)-2-nitrovinyl]phenol; CHEMBL309016; 22568-51-0; AF-467/00017042; 2-methoxy-4-(2-nitroethenyl)phenol; 2-Methoxy-4-(2-nitro-vinyl)-phenol; 4-((1E)-2-nitrovinyl)-2-methoxyphenol; 4-{2-nitrovinyl}-2-methoxyphenol; 4-Hydroxy-3-methoxy-beta-nitrostyrene; AC1LCWDN; PubChem19447; AC1Q1WR9; MLS000574924
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7900 nM
External Link
 Compound Name MG-111 Investigative [104]
Synonyms
134865-04-6; EGF, Hitachi
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 6,7-dimethoxy-4-(2-phenylethynyl)quinazoline Investigative [86]
Synonyms
CHEMBL250315; SCHEMBL6180450; BDBM50222433
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5600 nM
External Link
 Compound Name Anti-EGFR humanized mabs Investigative [13]
Synonyms
Anti-EGFR humanized mAbs (cancer); Anti-EGFR humanized mAbs (cancer), Xencor; Anti-EGFR humanized monoclonal antibodies (cancer), Xencor
    Click to Show/Hide
External Link
 Compound Name 4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline Investigative [86]
Synonyms
CHEMBL250924; BDBM50222419
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 26 nM
External Link
 Compound Name AL-6802 Investigative [13]
Synonyms
EGFR modulators (cancer), Advenchen/Simcere
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name BPIQ-I Investigative [91]
Synonyms
174709-30-9; N-(3-bromophenyl)-3-methyl-3H-imidazo[4,5-g]quinazolin-8-amine; 8-[(3-Bromophenyl)amino]-3-methyl-3H-imidazo[4,5-g]-quinazoline; Imidazoquinazoline deriv. 12; AC1L1DNH; GTPL5939; CHEMBL174426; BDBM3574; SCHEMBL17931472; CTK8E6742; DTXSID60274366; MolPort-044-561-412; HMS3229C05; ZINC2391775; IN1402; HSCI1_000090; AKOS025394452; CCG-206740; ACM174709309; RT-011807; J-011030; BRD-K72211743-001-01-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.025 nM
External Link
 Compound Name mabionHER2 Investigative [13]
Synonyms
Humanized monoclonal antibody (breast cancer), Mabion
    Click to Show/Hide
External Link
 Compound Name 4-(2-nitrovinyl)phenol Investigative [85]
Synonyms
4-Hydroxy-b-nitrostyrene; (E)-4-(2-nitrovinyl)phenol; 4-hydroxy-beta-nitrostyrene; trans-4-Hydroxy-beta-nitrostyrene; 22568-49-6; Phenol, p-(2-nitrovinyl)-; 4-[(E)-2-Nitroethenyl]phenol; 4-[(E)-2-nitrovinyl]phenol; CHEMBL307481; CTJKRKMPTRJAIT-AATRIKPKSA-N; NSC81594; 1-(4-hydroxyphenyl)-2-nitroethene; 4-(2-(Hydroxy(oxido)amino)vinyl)phenol; 4-(2-Nitro-vinyl)-phenol; NSC30299; AC1LCWDH; 4-Hydroxy--nitrostyrene; 4'-hydroxy-beta-nitrostyrene; Phenol,4-(2-nitroethenyl)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10000 nM
External Link
 Compound Name 4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Investigative [94]
Synonyms
CHEMBL200958
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MDP-01 Investigative [13]
Synonyms
Peptabody-EGF (anticancer), Med Discovery
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N4-(3-methylphenyl)-4,6-quinazolinediamine Investigative [105]
Synonyms
CHEMBL336113; Anilinoquinazoline, 4a; 6-amino-4-[(3-methylphenyl)amino]quinazoline; SMA52; SCHEMBL159209; ZINC6328; SMA-52; NFBCSWGEYDCCDW-UHFFFAOYSA-N; BDBM50133384; AKOS013914431; N*4*-m-Tolyl-quinazoline-4,6-diamine; 153436-70-5; 6-amino-4-(3'-methylanilino)quinazoline; 6-amino-4-(3-methylphenylamino)-quinazoline; FT-0765557; 6-amino-4[(3-methylphenyl)amino]quinazoline
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name RX-1792 Investigative [13]
Synonyms
EGF antagonist, Rexahn; RX-0183
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name (3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine Investigative [87]
Synonyms
N-(3-bromophenyl)-5-nitroquinazolin-4-amine; AC1NS3MQ; BDBM3290; CHEMBL116308; 4-Anilinoquinazoline deriv. 41
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 355 nM
External Link
 Compound Name NRC-2694 Investigative [13]
MOA Inhibitor
External Link
 Compound Name Cochliobolic acid Investigative [106]
Synonyms
CHEMBL464721; 185846-15-5; AC1O516J; BDBM50292386; 2-Furancarboxylic acid, tetrahydro-3-hydroxy-5-(17-methyl-13,14-dioxo-1,3,5,7,9,11,15-nonadecaheptaenyl)-, (2alpha,3beta,5alpha(1E,3E,5E,7E,9E,11E,15E))-(partial)-; (2R,3R,5S)-3-hydroxy-5-[(1E,3E,5E,7E,9E,11E,15E)-17-methyl-13,14-dioxononadeca-1,3,5,7,9,11,15-heptaenyl]oxolane-2-carboxylic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1600 nM
External Link
 Compound Name PD-168393 Investigative [107]
Synonyms
PD168393; 194423-15-9; pd 168393; UNII-3R996Y9T0I; 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline; n-{4-[(3-bromophenyl)amino]quinazolin-6-yl}prop-2-enamide; N-[4-(3-bromoanilino)quinazolin-6-yl]prop-2-enamide; CHEMBL285063; 3R996Y9T0I; C17H13BrN4O; N-[4-(3-Bromo-phenylamino)-quinazolin-6-yl]-acrylamide; 2-Propenamide, N-(4-((3-bromophenyl)amino)-6-quinazolinyl)-; 2-Propenamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-; nchembio866-comp2; N-(4-((3-bromophenyl)amino)quinazolin-6-yl)acrylamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.08 nM
External Link
 Compound Name N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Investigative [101]
Synonyms
CHEMBL31815; N-[4-[(3-methyl-phenyl)amino]quinazolin-6-yl]acrylamide; N-[4-[(3-methyl-phenyl)amino]quinazolin-6-yl)acrylamide; SCHEMBL2991796; AWQLTDUXGVCRBV-UHFFFAOYSA-N; BDBM50077244
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.42 nM
External Link
 Compound Name 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Investigative [108]
Synonyms
CHEMBL98798
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 70 nM
External Link
 Compound Name 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Investigative [108]
Synonyms
CHEMBL101581
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2500 nM
External Link
 Compound Name YH013 Investigative [109]
External Link
 Compound Name LAVENDUSTIN A Investigative [110]
Synonyms
125697-92-9; RG14355; UNII-3Y0G32G2RV; CHEMBL103552; 3Y0G32G2RV; C21H19NO6; Lavendustin A, from Streptomyces griseolavendus; Benzoic acid,5-[[(2,5-dihydroxyphenyl)methyl][(2-hydroxyphenyl)methyl]amino]-2-hydroxy-; RG 14355; 5-(((2,5-Dihydroxyphenyl)methyl)((2-hydroxyphenyl)methyl)amino)-2-hydroxybenzoic acid; Benzoic acid, 5-(((2,5-dihydroxyphenyl)methyl)((2-hydroxyphenyl)methyl)amino)-2-hydroxy-; 5-Amino-((N-2,5-dihydroxybenzyl)-N -2-hydroxybenzyl)salicylic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.004 ug.mL-1
External Link
 Compound Name PF 5208766 Investigative [111]
Synonyms
WAY-178357
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Investigative [112]
Synonyms
4-Anilidoquinazoline deriv. 12a; AC1NS5EY; SCHEMBL4355658; BDBM4397
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2700 nM
External Link
 Compound Name N-(4-(phenylamino)quinazolin-6-yl)acrylamide Investigative [107]
Synonyms
CHEMBL1221699; N-[4-(phenylamino)quinazolin-6-yl]prop-2-enamide; nchembio866-comp4; SCHEMBL614989; BDBM50324687; DB08462; N-(4-Anilinoquinazoline-6-yl)acrylamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 1 nM
External Link
 Compound Name AG-213 Investigative [103]
MOA Inhibitor
Activity Ki = 850 nM
External Link
 Compound Name SYM-011 Investigative [13]
Synonyms
Dimercept; Hermodulins; Herstatin; RB-200; RBLX-200; RBLX-242; RBLX-242h; RBLX-642h
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 10-hydroxy-18-methoxybetaenone Investigative [113]
Synonyms
CHEMBL498247; BDBM50269144
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10500 nM
External Link
 Compound Name 4557W Investigative [114]
Synonyms
EGFR/ErbB-2 Inhibitor; 179248-61-4; 4-(4-Benzyloxyanilino)-6,7-dimethoxyquinazoline; SCHEMBL242224; GTPL5964; CHEMBL563845; CTK8E8822; DTXSID40431718; MolPort-018-661-221; HMS3229C21; ZINC1485577; IN1350; HSCI1_000238; AKOS002350936; CCG-206748; RT-012453; J-011438; BRD-K76819286-001-01-0; N-[4-(Benzyloxy)phenyl]-6,7-dimethoxyquinazoline-4-amine; N-[4-(benzyloxy)phenyl]-6,7-dimethoxyquinazolin-4-amine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Tyrphostin ag-1478 Investigative [100]
Synonyms
AG-1478; 153436-53-4; Tyrphostin AG 1478; N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine; 175178-82-2; 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline; AG 1478; AG1478; TYRPHOSTIN; 4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-; UNII-SUH0SEZ9HY; SUH0SEZ9HY; AG-1478 hydrochloride; AG-1478 (Tyrphostin AG-1478); CHEMBL7917; CHEBI:75404; N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine; NSC-693255; AK-63142; N-(3-chlorophenyl)-6,7-dimethoxy-quinazolin-4-amine; BRD6408; BRD-6408; SR-01000076156; NSC693255
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 120 nM
External Link
 Compound Name CL-387785 Investigative [95]
Synonyms
194423-06-8; EKI-785; CL-387785 (EKI-785); CL-387,785; UNII-B4W27J1Z8B; CL-387785(EKI785; WAY-EKI 785); EKB-785; CHEMBL91867; B4W27J1Z8B; N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide; N-(4-((3-bromophenyl)amino)quinazolin-6-yl)but-2-ynamide; CHEBI:90180; C18H13BrN4O; N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}but-2-ynamide; N-[4-[(3-Bromophenyl)amino]quinazolin-6-yl]but-2-ynamide; N-[4-[(3-bromophenyl)amino]-6-quinazolinyl)-2-butynamide; N-{4-[(3-bromophenyl)amino]-6-quinazolinyl}-2-butynamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.37 nM
External Link
 Compound Name HDS-029 Investigative [115]
Synonyms
HDS 029
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.3 nM
External Link
 Compound Name WHI-P154 Investigative [116]
MOA Inhibitor
External Link
 Compound Name PMID24915291C38 Investigative [117]
Synonyms
GTPL8145; PLS-123; BDBM50020476; 1431727-04-6
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7 nM
External Link
 Compound Name HKI-9924129 Investigative [118]
MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name PD-0173956 Investigative [118]
Synonyms
UNII-YR2DP5GJ1Y; YR2DP5GJ1Y; PD173956; PD-173956; AC1NS9BQ; 305820-76-2; SCHEMBL1334768; BDBM6569; CHEMBL574059; Pyrido(2,3-d)pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-2-((4-fluorophenyl)amino)-8-methyl-; 6-(2,6-dichlorophenyl)-2-(4-fluoroanilino)-8-methylpyrido[2,3-d]pyrimidin-7-one; 6-(2,6-dichlorophenyl)-2-[(4-fluorophenyl)amino]-8-methyl-7H,8H-pyrido[2,3-d]pyrimidin-7-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 380 nM
External Link
 Compound Name PD-0166326 Investigative [118]
Synonyms
PD-166326
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 90 nM
External Link
 Compound Name PP121 Investigative [119]
Synonyms
PP-121; PP 121
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 260 nM
External Link
 Compound Name 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [120]
Synonyms
CHEMBL380598; SCHEMBL3148490; HVQJGNALTWNDMX-UHFFFAOYSA-N; BDBM50375058; 2-(1H-Indole-3-yl)-3-phenylmaleimide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Ro-4396686 Investigative [121]
Synonyms
SCHEMBL5809947; CHEMBL606964
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 545 nM
External Link
 Compound Name 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative [120]
Synonyms
1H-Pyrrole-2,5-dione, 3,4-bis(4-methoxyphenyl)-; 108774-82-9; ACMC-20mbs9; CHEMBL381099; CTK0G2626; DTXSID90449388
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative [120]
Synonyms
2,3-diphenylmaleimide; 1H-Pyrrole-2,5-dione, 3,4-diphenyl-; 31295-36-0; AC1MBL6S; SCHEMBL114611; CHEMBL201949; CTK1B9880; 3,4-diphenylpyrrole-2,5-dione; DTXSID70372903; ZINC3847556
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [120]
Synonyms
CHEMBL372076; SCHEMBL3822337
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Osimertinib Approved [14]
Synonyms
Tagrisso
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.421 nM
External Link
 Compound Name PMID27774824-Compound-Figure9Example2down Patented [122]
External Link
 Compound Name Mobocertinib Approved [122]
Synonyms
1847461-43-1; TAK-788; TAK788; AP32788; UNII-39HBQ4A67L; 39HBQ4A67L; propan-2-yl 2-[4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)anilino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Mobocertinib [INN]; Mobocertinib [USAN]; AP-32788; Mobocertinib (TAK788); Mobocertinib(TAK-788); SCHEMBL17373133; GTPL10468; BDBM368374; BCP31045; EX-A3392; US10227342, Example 10; MFCD32669806; NSC825519; s6813; TAK-788;AP32788; WHO 11183; NSC-825519; example 94 [WO2015195228A1]; HY-135815; CS-0114256; TAK-788;TAK 788; AP 32788; 5-Pyrimidinecarboxylic acid, 2-((4-((2-(dimethylamino)ethyl)methylamino)-2-methoxy-5-((1-oxo-2-propen-1-yl)amino)phenyl)amino)-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester; C(C=C)(=O)NC=1C(=CC(=C(C=1)NC1=NC=C(C(=N1)C1=CN(C2=CC=CC=C12)C)C(=O)OC(C)C)OC)N(C)CCN(C)C; Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Isopropyl 2-(5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenylamino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Propan-2-yl 2-(5-(acryloylamino)-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyanilino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
    Click to Show/Hide
External Link
 Compound Name DZD9008 Phase 1/2 [122]
External Link
 Compound Name AC0010 Phase 3 [122]
Synonyms
Avitinib; 1557267-42-1; N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; Avitinib free base; SCHEMBL15453394; KS-00000TON; EX-A783; MolPort-042-663-560; Avitinib(AC0010/AC0010MA); ZINC142081723; AKOS030632728; CS-W008904; N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide; DS-19269; AK543905; 2-Propenamide, N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-
    Click to Show/Hide
External Link
 Compound Name EGFR antisense DNA Phase 1/2 [122]
Synonyms
Antisense therapy, UPCI; EGFR antisense DNA, University of Pittsburgh
    Click to Show/Hide
External Link
 Compound Name CK-101 Phase 1/2 [122]
Synonyms
IDRGFNPZDVBSSE-UHFFFAOYSA-N; 1660963-42-7; RX-518; N-(3-(2-((2,3-Difluoro-4-(4-(2-hydroxyethyl)piperazin-1-yl)phenyl)amino)quinazolin-8-yl)phenyl)acrylamide; EGFR-IN-3; UNII-708TLB8J3Y; 708TLB8J3Y; AK543910; N-[3-[2-[[2,3-difluoro-4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl]amino]quinazolin-8-yl]phenyl]acrylamide; GTPL9863; SCHEMBL16514522; KS-00000TOQ; MolPort-042-663-562; RX518; CK101; EX-A1142; BCP19075; RX 518; ZINC514250913; AKOS030632731; DS-19272; HY-19815; CS-0016788; Example 153 [US20170050936A1]; J-690231; 2-Propena
    Click to Show/Hide
External Link
 Compound Name Pyrotinib Phase 1 [122]
Synonyms
UNII-CJN36EQM0H; SHR-1258; CJN36EQM0H; SHR1258; 1269662-73-8; SCHEMBL9948753; GTPL9662; SADXACCFNXBCFY-IYNHSRRRSA-N; BDBM139991; AKOS032946680; CS-7940; compound 12 [PMID: 28115222]; 2-Propenamide, N-(4-((3-chloro-4-(2-pyridinylmethoxy)phenyl)amino)-3-cyano-7-ethoxy-6-quinolinyl)-3-((2R)-1-methyl-2-pyrrolidinyl)-, (2E)-; HY-104065; US8901140, 5; (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide; (E)-N-[4-[3-chloro-4-(pyridin-2-ylmetho
    Click to Show/Hide
External Link
 Compound Name Anti-EGFRvIII CAR transduced PBL Phase 1/2 [122]
External Link
 Compound Name EGFRvIII CAR Phase 1/2 [122]
External Link
 Compound Name Anti-EGFR V III CAR-T cells Phase 1/2 [122]
External Link
 Compound Name EGFRvIII CAR T cells Phase 1 [122]
External Link
 Compound Name CAR-T cells targeting EGFRviii Phase 1 [122]
External Link
 Compound Name Anti-EGFRvIII CAR T cells Phase 1 [122]
External Link
 Compound Name CART-EGFRvIII T cells Phase 1 [122]
External Link
 Compound Name EGFRvIII-CARs Phase 1 [122]
External Link
 Compound Name CAR-T Cells targeting EGFRvIII Phase 1 [122]
External Link
 Compound Name RG6156 Phase 1 [122]
External Link
 Compound Name AMG 596 Phase 1 [122]
External Link
 Compound Name D2C7 Phase 1 [70]
External Link
References
Ref 1 The m(6)A Methyltransferase METTL3 Promotes Translation in Human Cancer Cells. Mol Cell. 2016 May 5;62(3):335-345. doi: 10.1016/j.molcel.2016.03.021. Epub 2016 Apr 21.
Ref 2 MiR-33a suppresses proliferation of NSCLC cells via targeting METTL3 mRNA. Biochem Biophys Res Commun. 2017 Jan 22;482(4):582-589. doi: 10.1016/j.bbrc.2016.11.077. Epub 2016 Nov 14.
Ref 3 METTL3 induces PLX4032 resistance in melanoma by promoting m(6)A-dependent EGFR translation. Cancer Lett. 2021 Dec 1;522:44-56. doi: 10.1016/j.canlet.2021.09.015. Epub 2021 Sep 13.
Ref 4 ADAR2-mediated editing of miR-214 and miR-122 precursor and antisense RNA transcripts in liver cancers. PLoS One. 2013 Dec 27;8(12):e81922. doi: 10.1371/journal.pone.0081922. eCollection 2013.
Ref 5 Rs884225 polymorphism is associated with primary hypertension by compromising interaction between epithelial growth factor receptor (EGFR) and miR-214. J Cell Mol Med. 2021 Apr;25(8):3714-3723. doi: 10.1111/jcmm.15976. Epub 2021 Feb 26.
Ref 6 Rindopepimut, a 14-mer injectable peptide vaccine against EGFRvIII for the potential treatment of glioblastoma multiforme. Curr Opin Mol Ther. 2010 Dec;12(6):741-54.
Ref 7 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. doi: 10.1517/14728214.11.4.709.
Ref 8 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48. doi: 10.1021/bi900729a.
Ref 9 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
Ref 10 Integration of panitumumab into the treatment of colorectal cancer. Crit Rev Oncol Hematol. 2010 Apr;74(1):16-26. doi: 10.1016/j.critrevonc.2009.06.005. Epub 2009 Jul 17.
Ref 11 Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol Cancer Ther. 2002 May;1(7):507-14.
Ref 12 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
Ref 13 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
Ref 14 AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3.
Ref 15 2017 FDA drug approvals. Nat Rev Drug Discov. 2018 Feb;17(2):81-85. doi: 10.1038/nrd.2018.4. Epub 2018 Jan 19.
Ref 16 Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209. doi: 10.1158/2159-8290.CD-20-0116. Epub 2020 May 15.
Ref 17 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76. doi: 10.1021/jm061031t.
Ref 18 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7. doi: 10.5507/bp.2009.002.
Ref 19 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 20 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 21 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
Ref 22 Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 2011 Aug;73(2):195-202. doi: 10.1016/j.lungcan.2010.11.007. Epub 2010 Dec 8.
Ref 23 Sym004, a novel EGFR antibody mixture, can overcome acquired resistance to cetuximab. Neoplasia. 2013 Oct;15(10):1196-206. doi: 10.1593/neo.131584.
Ref 24 Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Dec;3(12):1404-15.
Ref 25 Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9. doi: 10.1056/NEJMoa1413654.
Ref 26 Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial. J Thorac Oncol. 2020 Dec;15(12):1907-1918. doi: 10.1016/j.jtho.2020.09.001. Epub 2020 Sep 9.
Ref 27 ClinicalTrials.gov (NCT04305795) An Open-label Study Using ASP-1929 Photoimmunotherapy in Combination With Anti-PD1 Therapy in EGFR Expressing Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 28 Clinical pipeline report, company report or official report of Klus Pharma
Ref 29 Clinical pipeline report, company report or official report of Roche (2009).
Ref 30 Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. doi: 10.1016/j.bmc.2007.03.055. Epub 2007 Mar 23.
Ref 31 Characterization of ABT-806, a Humanized Tumor-Specific Anti-EGFR Monoclonal Antibody. Mol Cancer Ther. 2015 May;14(5):1141-51. doi: 10.1158/1535-7163.MCT-14-0820. Epub 2015 Mar 2.
Ref 32 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics. 2005 Aug;86(2):127-41. doi: 10.1016/j.ygeno.2005.04.008.
Ref 33 Phase I dose escalation study of ASP8273, a mutant-selective irreversible EGFR inhibitor, in subjects with EGFR mutation positive NSCLC, Journal of Clinical Oncology, Vol 33, No 15_suppl (May 20 Supplement), 2015: 8083.
Ref 34 Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development. Mar Drugs. 2014 January; 12(1): 255-278.
Ref 35 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 36 Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Cancer Cell. 2008 Apr;13(4):365-73. doi: 10.1016/j.ccr.2008.02.019.
Ref 37 Active antimetastatic immunotherapy in Lewis lung carcinoma with self EGFR extracellular domain protein in VSSP adjuvant. Int J Cancer. 2006 Nov 1;119(9):2190-9.
Ref 38 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 39 Molecular mechanisms of resistance to the EGFR monoclonal antibody cetuximab. Cancer Biol Ther. 2011 May 1;11(9):777-92. doi: 10.4161/cbt.11.9.15050. Epub 2011 May 1.
Ref 40 Monoclonal antibodies to target epidermal growth factor receptor-positive tumors: a new paradigm for cancer therapy. Cancer. 2002 Mar 1;94(5):1593-611. doi: 10.1002/cncr.10372.
Ref 41 EGFR tyrosine kinase inhibitor pelitinib regulates radiation-induced p65-dependent telomerase activation in squamous cell carcinoma. Radiat Res. 2013 Mar;179(3):304-12. doi: 10.1667/RR3028.1. Epub 2013 Feb 4.
Ref 42 BiPar Sciences Co-founder Reunites Management Team At TriAct Therapeutics to Advance Clinical Stage Cancer Programs. TriAct Therapeutics. Sept. 10, 2009.
Ref 43 AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61. doi: 10.1007/s10637-010-9389-3. Epub 2010 Feb 2.
Ref 44 Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes. Clin Cancer Res. 2021 Mar 1;27(5):1463-1475. doi: 10.1158/1078-0432.CCR-20-3555. Epub 2020 Dec 22.
Ref 45 Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93. doi: 10.1002/jps.22099.
Ref 46 ClinicalTrials.gov (NCT01869166) Treatment of Chemotherapy Refractory EGFR(Epidermal Growth Factor Receptor) Positive Advanced Solid Tumors (CART-EGFR)
Ref 47 ClinicalTrials.gov (NCT03152435) EGFR CART Cells for Patients With Metastatic Colorectal Cancer
Ref 48 Regression of EGFR positive established solid tumors in mice with the conditionally active T cell engager TAK-186. J Immunother Cancer. 2022 Jun;10(6):e004336.
Ref 49 Clinical pipeline report, company report or official report of Zentalis Pharmaceuticals.
Ref 50 Clinical pipeline report, company report or official report of EpimAb Biotherapeutics.
Ref 51 Clinical pipeline report, company report or official report of Black Diamond Therapeutics.
Ref 52 Clinical pipeline report, company report or official report of Affimed Therapeutics.
Ref 53 Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 54 Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80. doi: 10.1016/s0959-8049(02)00020-5.
Ref 55 World Antibody-Drug Conjugate Summit, October 15-16, 2013, San Francisco, CA. MAbs. 2014 January 1; 6(1): 18-29.
Ref 56 AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487. doi: 10.1371/journal.pone.0021487. Epub 2011 Jul 18.
Ref 57 AMG 595, an Anti-EGFRvIII Antibody-Drug Conjugate, Induces Potent Antitumor Activity against EGFRvIII-Expressing Glioblastoma. Mol Cancer Ther. 2015 Jul;14(7):1614-24. doi: 10.1158/1535-7163.MCT-14-1078. Epub 2015 Apr 30.
Ref 58 ClinicalTrials.gov (NCT03638167) EGFR806-specific CAR T Cell Locoregional Immunotherapy for EGFR-positive Recurrent or Refractory Pediatric CNS Tumors
Ref 59 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 60 A Phase I Study of Immunotoxin, MR1-1. Duke University report.
Ref 61 ClinicalTrials.gov (NCT02331693) CAR T Cells in Treating Patients With Malignant Gliomas Overexpressing EGFR
Ref 62 TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658. doi: 10.1158/1535-7163.MCT-17-1206. Epub 2018 May 10.
Ref 63 Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
Ref 64 Company report (Biooncology)
Ref 65 ClinicalTrials.gov (NCT04429542) Study of Safety and Tolerability of BCA101 Alone and in Combination With Pembrolizumab in Patients With EGFR-driven Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 66 A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73. doi: 10.1158/1078-0432.CCR-14-2820. Epub 2015 Jan 8.
Ref 67 Clinical pipeline report, company report or official report of SystImmune.
Ref 68 Clinical pipeline report, company report or official report of CytomX
Ref 69 Clinical pipeline report, company report or official report of AstraZeneca
Ref 70 Improved efficacy against malignant brain tumors with EGFRwt/EGFRvIII targeting immunotoxin and checkpoint inhibitor combinations. J Immunother Cancer. 2019 May 29;7(1):142. doi: 10.1186/s40425-019-0614-0.
Ref 71 Clinical pipeline report, company report or official report of Merus.
Ref 72 National Cancer Institute Drug Dictionary (drug id 596693).
Ref 73 Pyrrolo[2,3-d]pyrimidines active as Btk inhibitors. Expert Opin Ther Pat. 2017 Dec;27(12):1305-1318. doi: 10.1080/13543776.2017.1355908. Epub 2017 Jul 20.
Ref 74 Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J Pharmacol Exp Ther. 2013 Jun;345(3):393-403. doi: 10.1124/jpet.113.203497. Epub 2013 Mar 25.
Ref 75 GA201 (RG7160): a novel, humanized, glycoengineered anti-EGFR antibody with enhanced ADCC and superior in vivo efficacy compared with cetuximab. Clin Cancer Res. 2013 Mar 1;19(5):1126-38. doi: 10.1158/1078-0432.CCR-12-0989. Epub 2012 Dec 3.
Ref 76 EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice. Diabetes. 2009 Dec;58(12):2910-9. doi: 10.2337/db08-0506. Epub 2009 Aug 20.
Ref 77 Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 78 A comparison of EGF and MAb 528 labeled with 111In for imaging human breast cancer. J Nucl Med. 2000 May;41(5):903-11.
Ref 79 Clinical pipeline report, company report or official report of Bristol-Myers Squibb.
Ref 80 The heparin-binding domain of heparin-binding EGF-like growth factor can target Pseudomonas exotoxin to kill cells exclusively through heparan sulfate proteoglycans. J Cell Sci. 1994 Sep;107 ( Pt 9):2599-608. doi: 10.1242/jcs.107.9.2599.
Ref 81 Retinoic acid-induced RB (retinoblastoma) hypophosphorylation enhanced by CGP 52411 (4,5-dianilinophthalimide), an EGF family tyrosine kinase receptor inhibitor. Eur J Cell Biol. 1996 Apr;69(4):327-34.
Ref 82 Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. J Med Chem. 1994 Apr 1;37(7):1015-27.
Ref 83 WO patent application no. 2009,0582,67, Benzomorpholine derivatives and methods of use.
Ref 84 Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship. J Med Chem. 2007 May 31;50(11):2605-8. doi: 10.1021/jm070144p. Epub 2007 May 2.
Ref 85 Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60. doi: 10.1021/np50089a001.
Ref 86 Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5863-7. doi: 10.1016/j.bmcl.2007.08.020. Epub 2007 Aug 15.
Ref 87 Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. J Med Chem. 1995 Sep 1;38(18):3482-7. doi: 10.1021/jm00018a008.
Ref 88 Growth factors and their receptors: new targets for prostate cancer therapy. Urology. 2001 Aug;58(2 Suppl 1):114-22. doi: 10.1016/s0090-4295(01)01253-5.
Ref 89 Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52. doi: 10.1021/jm00130a020.
Ref 90 Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991 Jun;34(6):1896-907. doi: 10.1021/jm00110a022.
Ref 91 Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. J Med Chem. 1996 Feb 16;39(4):918-28. doi: 10.1021/jm950692f.
Ref 92 Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor. J Med Chem. 1996 Apr 26;39(9):1823-35. doi: 10.1021/jm9508651.
Ref 93 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. doi: 10.1073/pnas.0708800104. Epub 2007 Dec 11.
Ref 94 Acryloylamino-salicylanilides as EGFR PTK inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):469-72. doi: 10.1016/j.bmcl.2005.06.088. Epub 2005 Nov 3.
Ref 95 Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies. J Med Chem. 2009 Feb 26;52(4):964-75. doi: 10.1021/jm800829v.
Ref 96 Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37. doi: 10.1634/theoncologist.6-6-517.
Ref 97 5-Benzylidene-hydantoins: synthesis and antiproliferative activity on A549 lung cancer cell line. Eur J Med Chem. 2009 Sep;44(9):3471-9. doi: 10.1016/j.ejmech.2009.01.035. Epub 2009 Feb 7.
Ref 98 Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. doi: 10.1021/jm9503613.
Ref 99 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 1994 Aug 19;37(17):2627-9. doi: 10.1021/jm00043a002.
Ref 100 Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. J Med Chem. 1999 Mar 25;42(6):1018-26. doi: 10.1021/jm980551o.
Ref 101 Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. J Med Chem. 1999 May 20;42(10):1803-15. doi: 10.1021/jm9806603.
Ref 102 Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept. J Med Chem. 2003 Dec 4;46(25):5546-51. doi: 10.1021/jm030423m.
Ref 103 Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. Eur J Med Chem. 2008 Jul;43(7):1478-88. doi: 10.1016/j.ejmech.2007.09.018. Epub 2007 Sep 29.
Ref 104 Effects of hEGF (MG111) on gastric mucosal potential difference in rats. Scand J Gastroenterol Suppl. 1989;162:198-201. doi: 10.3109/00365528909091160.
Ref 105 The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR). J Med Chem. 2006 Jun 15;49(12):3544-52. doi: 10.1021/jm0600390.
Ref 106 Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay. J Nat Prod. 1997 Jan;60(1):6-8. doi: 10.1021/np9605293.
Ref 107 Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol. 2007 Apr;3(4):229-38. doi: 10.1038/nchembio866. Epub 2007 Mar 4.
Ref 108 A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997).
Ref 109 Clinical pipeline report, company report or official report of Biocytogen
Ref 110 Novel antiproliferative agents derived from lavendustin A. J Med Chem. 1994 Nov 25;37(24):4079-84. doi: 10.1021/jm00050a005.
Ref 111 Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J Med Chem. 2005 Feb 24;48(4):1107-31. doi: 10.1021/jm040159c.
Ref 112 Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. doi: 10.1016/j.bmcl.2009.10.024. Epub 2009 Oct 9.
Ref 113 Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. J Nat Prod. 2000 Jun;63(6):739-45. doi: 10.1021/np9905259.
Ref 114 Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5. doi: 10.1016/s0960-894x(01)00219-0.
Ref 115 Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. J Med Chem. 2006 Feb 23;49(4):1475-85. doi: 10.1021/jm050936o.
Ref 116 The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. doi: 10.1182/blood-2007-09-115030. Epub 2007 Dec 19.
Ref 117 Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28. doi: 10.1021/jm4017762. Epub 2014 Jun 10.
Ref 118 Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98. doi: 10.1016/s0006-2952(00)00405-6.
Ref 119 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. doi: 10.1038/nchembio.117. Epub 2008 Oct 12.
Ref 120 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81. doi: 10.1021/jm0580297.
Ref 121 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. doi: 10.1016/j.bmcl.2005.12.092. Epub 2006 Feb 3.
Ref 122 TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751.