Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05032
[1]
Non-coding RNA miR-33a METTL3  lncRNA       miRNA   circRNA Direct 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 Non-coding RNA (ncRNA)
Epigenetic Regulator hsa-miR-33a microRNA View Details
Regulated Target Methyltransferase-like protein 3 (METTL3) View Details
Crosstalk Relationship ncRNA  →  m6A Inhibition
Crosstalk Mechanism ncRNAs directly impacts m6A modification through modulating the expression level of m6A regulator
Crosstalk Summary hsa-miR-33a suppresses proliferation of NSCLC cells via targeting METTL3 mRNA.miR-33a was able to depress the expression of Epidermal growth factor receptor (EGFR), TAZ, MAPKAPK2 and DNMT3A at the level of protein
Responsed Disease Non-small cell lung cancer ICD-11: 2C25.Y
Cell Process RNA stability
RNA degradation (hsa03018)
In-vitro Model
A-549 Lung adenocarcinoma Homo sapiens CVCL_0023
NCI-H460 Lung large cell carcinoma Homo sapiens CVCL_0459
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 [2]
Synonyms
LY3012211
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MOA Modulator
External Link
 Compound Name HEGF Approved [3]
MOA Activator
External Link
 Compound Name Erlotinib Approved [4]
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
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MOA Inhibitor
Activity Ki = 0.1 nM
External Link
 Compound Name Gefitinib Approved [5]
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
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MOA Inhibitor
Activity IC50 = 0.1 nM
External Link
 Compound Name Panitumumab Approved [6]
Synonyms
Vectibix; Panitumumab (genetical recombination); Vectibix (TN); Panitumumab (USAN/INN); Panitumumab (genetical recombination) (JAN); Panitumumab (EGFR mAb inhibitor)
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MOA Suppressor
External Link
 Compound Name Cetuximab Approved [7]
Synonyms
Erbitux; Cetuximab (genetical recombination); Erbitux (TN); Cetuximab (USAN/INN); Cetuximab (genetical recombination) (JAN); novel EGFR mAb inhibitors
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External Link
 Compound Name BIBW 2992 Approved [8]
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
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MOA Inhibitor
Activity IC50 = 0.19 nM
External Link
 Compound Name Nitroglycerin Approved [3]
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
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MOA Activator
External Link
 Compound Name Epidermal growth factor Approved [9]
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
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MOA Modulator
External Link
 Compound Name Osimertinib Approved [10]
Synonyms
Tagrisso
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MOA Inhibitor
Activity IC50 = 0.421 nM
External Link
 Compound Name NERATINIB MALEATE Approved [11]
Synonyms
UNII-9RM7XY23ZS; 9RM7XY23ZS; Neratinib maleate [MI]; hki-272 maleate; Nerlynx (TN); SCHEMBL2180998; MolPort-044-561-003; AKOS030524209; DS-19892
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MOA Antagonist
External Link
 Compound Name Amivantamab Approved [12]
MOA Inhibitor
External Link
 Compound Name SKI-758 Approved [13]
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
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MOA Inhibitor
Activity IC50 = 230 nM
External Link
 Compound Name Dacomitinib Approved [9]
Synonyms
PF-00299804
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MOA Antagonist
Activity IC50 = 1.8 nM
External Link
 Compound Name Lapatinib Approved [14]
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)
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MOA Inhibitor
Activity Ki = 3 nM
External Link
 Compound Name Merimepodib Approved [15]
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
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MOA Inhibitor
External Link
 Compound Name Vandetanib Approved [16]
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)
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MOA Inhibitor
Activity IC50 = 200 nM
External Link
 Compound Name Sorafenib Approved [17]
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)
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MOA Inhibitor
Activity IC50 = 43.5 nM
External Link
 Compound Name Icotinib hydrochloride Registered [18]
Synonyms
Conmana; Conmanna; Icotinib; BPI-2009-H
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MOA Antagonist
External Link
 Compound Name Rindopepimut Phase 3 [2]
MOA Modulator
External Link
 Compound Name SYM-004 Phase 3 [19]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
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External Link
 Compound Name DE-766 Phase 3 [9]
MOA Modulator
External Link
 Compound Name EGF816 Phase 3 [20]
MOA Inhibitor
Activity IC50 = 160.6 nM
External Link
 Compound Name CO-1686 Phase 3 [21]
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
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MOA Modulator
Activity IC50 = 1.6 nM
External Link
 Compound Name Zalutumumab Phase 3 [9]
External Link
 Compound Name Almonertinib Phase 3 [22]
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
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MOA Inhibitor
External Link
 Compound Name ASP1929 Phase 3 [23]
Synonyms
Cetuximab sarotalocan
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MOA Inhibitor
External Link
 Compound Name A140 Phase 3 [24]
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [25]
MOA Inhibitor
External Link
 Compound Name HKI-272 Phase 3 [26]
Synonyms
Neratinib (ERBB2 inhibitor)
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MOA Inhibitor
Activity IC50 = 0.08 nM
External Link
 Compound Name Indium-111 Phase 2/3 [27]
Synonyms
ABT-806
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External Link
 Compound Name Varlitinib Phase 2/3 [28]
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
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MOA Modulator
Activity IC50 = 7 nM
External Link
 Compound Name ASP8273 Phase 2 [29]
MOA Inhibitor
Activity IC50 = 8 nM
External Link
 Compound Name ABT-414 Phase 2 [30]
External Link
 Compound Name Depatuxizumab Phase 2 [31]
MOA Antagonist
External Link
 Compound Name Matuzumab Phase 2 [32]
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
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External Link
 Compound Name HER1-VSSP vaccine Phase 2 [33]
Synonyms
HER1-VSSP vaccine (cancer)
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External Link
 Compound Name RM-1929 Phase 2 [34]
MOA Antagonist
External Link
 Compound Name CetuGEX Phase 2 [35]
External Link
 Compound Name ABX-EGF Phase 2 [36]
External Link
 Compound Name Pelitinib Phase 2 [37]
Synonyms
EKB-569; EKI-569; WAY-EKB-569
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MOA Modulator
Activity IC50 = 8.02 nM
External Link
 Compound Name HM-78136B Phase 2 [34]
Synonyms
Pan-Her/EGFR inhibitors (cancer), Hanmi
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MOA Inhibitor
Activity IC50 = 0.218 nM
External Link
 Compound Name Pazopanib + Tyverb/Tykerb Phase 2 [15]
MOA Inhibitor
External Link
 Compound Name MEHD-7945A Phase 2 [28]
Synonyms
RG-7597; EGFR/HER3 dual monoclonal antibody, Genentech
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MOA Modulator
External Link
 Compound Name TT-100 Phase 2 [38]
Synonyms
TT-100, TriAct; Dual IGF-1/EGFR inhibitor (non-small-cell lung cancer), TriAct
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MOA Inhibitor
External Link
 Compound Name BMS-599626 Phase 2 [39]
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
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MOA Inhibitor
Activity IC50 = 32 nM
External Link
 Compound Name Tarloxotinib Phase 2 [40]
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
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MOA Inhibitor
External Link
 Compound Name VATALANIB Phase 2 [26]
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
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MOA Inhibitor
Activity IC50 = 457.7 nM
External Link
 Compound Name BMS-690514 Phase 2 [41]
Synonyms
BMS 690514; BMS690514
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MOA Inhibitor
External Link
 Compound Name CI-1033 Phase 2 [16]
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 [42]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name SN-32793 Phase 1/2 [9]
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 [43]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name EMD 55900 Phase 1/2 [36]
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 [44]
MOA Inhibitor
External Link
 Compound Name ZN-e4 Phase 1/2 [45]
MOA Inhibitor
External Link
 Compound Name EMB-01 Phase 1/2 [46]
MOA Inhibitor
External Link
 Compound Name Sym015 Phase 1/2 [31]
MOA Antagonist
External Link
 Compound Name BDTX-189 Phase 1/2 [47]
Synonyms
2414572-47-5; EX-A4379
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name AFM24 Phase 1/2 [48]
External Link
 Compound Name Sym013 Phase 1/2 [31]
MOA Antagonist
External Link
 Compound Name S-222611 Phase 1b [49]
MOA Inhibitor
External Link
 Compound Name SYN004 Phase 1 [31]
MOA Inhibitor
External Link
 Compound Name BIBX-1382 Phase 1 [50]
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 [51]
MOA Inhibitor
External Link
 Compound Name AST-1306 Phase 1 [52]
Synonyms
Allitinib; Allitinib tosylate
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MOA Modulator
External Link
 Compound Name AMG 595 Phase 1 [53]
MOA Modulator
External Link
 Compound Name HER-2/HER-1 vaccine Phase 1 [9]
Synonyms
HER-2/HER-1 vaccine (solid tumors)
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External Link
 Compound Name EGFR806-specific CAR T cell Phase 1 [54]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name PF-05230907 Phase 1 [55]
MOA Inhibitor
External Link
 Compound Name MR1-1 Phase 1 [56]
Synonyms
MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX
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MOA Modulator
External Link
 Compound Name Anti-EGFR CAR T Phase 1 [57]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name AP32788 Phase 1 [34]
MOA Inhibitor
External Link
 Compound Name CLN-081 Phase 1 [58]
MOA Inhibitor
External Link
 Compound Name LY3164530 Phase 1 [59]
MOA Modulator
External Link
 Compound Name MM-151 Phase 1 [31]
MOA Antagonist
External Link
 Compound Name Cipatinib Phase 1 [28]
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 [60]
MOA Modulator
External Link
 Compound Name BCA101 Phase 1 [61]
MOA Inhibitor
External Link
 Compound Name CUDC-101 Phase 1 [62]
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 [63]
External Link
 Compound Name CX-904 Phase 1 [64]
Synonyms
AMG 651
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External Link
 Compound Name AZD9592 Phase 1 [65]
External Link
 Compound Name D2C7 Phase 1 [66]
External Link
 Compound Name MCLA-158 Phase 1 [67]
MOA Inhibitor
External Link
 Compound Name JNJ-26483327 Phase 1 [68]
Synonyms
MTKI (cancer), J&J; MTKI (cancer), Johnson & Johnson; Multi-targeted kinase inhibitor (cancer), J&J; Multi-targeted kinase inhibitor (cancer), Johnson & Johnson
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MOA Inhibitor
External Link
 Compound Name Pyrrolo[2,3-d]pyrimidine derivative 24 Patented [69]
Synonyms
PMID28705083-Compound-22
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MOA Inhibitor
External Link
 Compound Name PKI166 Discontinued in Phase 2 [70]
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 [71]
MOA Modulator
External Link
 Compound Name PD-153035 Discontinued in Phase 1 [72]
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
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MOA Modulator
Activity Ki = 0.006 nM
External Link
 Compound Name AZD4769 Discontinued in Phase 1 [73]
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
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MOA Inhibitor
External Link
 Compound Name TAK165 Discontinued in Phase 1 [16]
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 [74]
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
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MOA Modulator
External Link
 Compound Name EGFR/IGFR tandem adnectin Preclinical [75]
Synonyms
BMS-964210
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MOA Inhibitor
External Link
 Compound Name Heparin-EGF-like factor Terminated [76]
Synonyms
HB-EGF, Scios Nova; Heparin-EGF-like factor, Scios Nova
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MOA Modulator
External Link
 Compound Name CGP-52411 Terminated [77]
Synonyms
DAPH
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MOA Inhibitor
Activity Ki = 160 nM
External Link
 Compound Name CGP-53353 Terminated [78]
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 [79]
MOA Antagonist
External Link
 Compound Name N4-(3-chlorophenyl)quinazoline-4,6-diamine Investigative [80]
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 [81]
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 [82]
Synonyms
CHEMBL250523; BDBM50222432
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MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name 2-cyano-3-(3,4-dihydroxyphenyl)acrylamide Investigative [81]
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 [9]
Synonyms
EGFR mutant selective inhibitor (cancer), Hanmi; EMSI (cancer), Hanmi
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MOA Inhibitor
External Link
 Compound Name Benzyl-quinazolin-4-yl-amine Investigative [83]
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 [82]
Synonyms
CHEMBL250925
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name AFM-21 Investigative [9]
Synonyms
Anti-EGFR antibody (RECRUIT-TandAb, colon/solid tumors), Affimed
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External Link
 Compound Name PD182905 Investigative [84]
MOA Inhibitor
External Link
 Compound Name AG 112 Investigative [85]
Synonyms
tyrphostin A48; tyrphostin AG 112; AG-112; AG112
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MOA Inhibitor
Activity IC50 = 125 nM
External Link
 Compound Name 2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile Investigative [86]
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
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MOA Inhibitor
Activity IC50 = 7000 nM
External Link
 Compound Name (3-Bromo-phenyl)-quinazolin-4-yl-amine Investigative [87]
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 [88]
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 [89]
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
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MOA Inhibitor
Activity IC50 = 21 nM
External Link
 Compound Name 6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline Investigative [82]
Synonyms
CHEMBL399371
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MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name LA22-radioimmunoconjugates Investigative [9]
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 [90]
Synonyms
CHEMBL382537
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MOA Inhibitor
External Link
 Compound Name ICR 62 Investigative [36]
External Link
 Compound Name Bmab-200 Investigative [9]
Synonyms
Anti-EGFR mAb (cancer), Biocon; Anti-epidermal growth factor receptor monoclonal antibody (cancer), Biocon
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External Link
 Compound Name HTS-00213 Investigative [91]
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 [82]
Synonyms
CHEMBL251123
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MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine Investigative [88]
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 [9]
Synonyms
HMPL-813; EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma
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MOA Inhibitor
External Link
 Compound Name OSI-75 Investigative [92]
MOA Inhibitor
External Link
 Compound Name (E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin Investigative [93]
Synonyms
CHEMBL213560; SCHEMBL16693054; BDBM50187134
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MOA Inhibitor
Activity IC50 = 710 nM
External Link
 Compound Name HTS-02876 Investigative [91]
Synonyms
AC1MDGL2; CHEMBL460914; MolPort-002-900-576; ZINC1030761; MCULE-7093116609
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MOA Inhibitor
External Link
 Compound Name 2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile Investigative [86]
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
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MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name PMID8568816C56 Investigative [94]
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
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MOA Inhibitor
Activity IC50 = 0.006 nM
External Link
 Compound Name MT-062 Investigative [9]
Synonyms
EGFR inhibitor (melanoma), Medisyn Technologies
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MOA Inhibitor
External Link
 Compound Name Anti-EGFR mab Investigative [9]
External Link
 Compound Name RG-50810 Investigative [81]
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
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MOA Inhibitor
Activity Ki = 11000 nM
External Link
 Compound Name IPS-01003 Investigative [9]
Synonyms
EGFR kinase antagonist (cancer), InnoPharmaScreen
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MOA Antagonist
External Link
 Compound Name RM-6427 Investigative [9]
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 [87]
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 [95]
MOA Inhibitor
Activity IC50 = 5000 nM
External Link
 Compound Name AGT-2000 Investigative [9]
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 [96]
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 [9]
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 [9]
Synonyms
EGFR-targeting siRNA agent, ForHumanTech
    Click to Show/Hide
External Link
 Compound Name GI-3000 Investigative [9]
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 [91]
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 [78]
Synonyms
CHEMBL7914; SCHEMBL8834183; BDBM50040920
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4500 nM
External Link
 Compound Name HTS-05058 Investigative [89]
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 [97]
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 [81]
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 [87]
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 [9]
Synonyms
Dolastatin-conjugated HER2 antibody (breast cancer), Ambrx
    Click to Show/Hide
External Link
 Compound Name TGF alpha Investigative [9]
Synonyms
TGF alpha (neurological damage)
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name AG 9 Investigative [85]
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 [98]
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 [99]
Synonyms
CHEMBL473320; SCHEMBL5616932
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 131 nM
External Link
 Compound Name Theliatinib Investigative [9]
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 [87]
MOA Inhibitor
External Link
 Compound Name 6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline Investigative [82]
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 [81]
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 [9]
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 [83]
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 [81]
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 [81]
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 [81]
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 [9]
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 [81]
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 [100]
Synonyms
134865-04-6; EGF, Hitachi
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 6,7-dimethoxy-4-(2-phenylethynyl)quinazoline Investigative [82]
Synonyms
CHEMBL250315; SCHEMBL6180450; BDBM50222433
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5600 nM
External Link
 Compound Name Anti-EGFR humanized mabs Investigative [9]
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 [82]
Synonyms
CHEMBL250924; BDBM50222419
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 26 nM
External Link
 Compound Name AL-6802 Investigative [9]
Synonyms
EGFR modulators (cancer), Advenchen/Simcere
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name BPIQ-I Investigative [87]
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 [9]
Synonyms
Humanized monoclonal antibody (breast cancer), Mabion
    Click to Show/Hide
External Link
 Compound Name 4-(2-nitrovinyl)phenol Investigative [81]
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 [90]
Synonyms
CHEMBL200958
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MDP-01 Investigative [9]
Synonyms
Peptabody-EGF (anticancer), Med Discovery
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N4-(3-methylphenyl)-4,6-quinazolinediamine Investigative [101]
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 [9]
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 [83]
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 [9]
MOA Inhibitor
External Link
 Compound Name Cochliobolic acid Investigative [102]
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 [103]
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 [97]
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 [104]
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 [104]
Synonyms
CHEMBL101581
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2500 nM
External Link
 Compound Name YH013 Investigative [105]
External Link
 Compound Name LAVENDUSTIN A Investigative [106]
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 [107]
Synonyms
WAY-178357
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name 6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Investigative [108]
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 [103]
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 [99]
MOA Inhibitor
Activity Ki = 850 nM
External Link
 Compound Name SYM-011 Investigative [9]
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 [109]
Synonyms
CHEMBL498247; BDBM50269144
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10500 nM
External Link
 Compound Name 4557W Investigative [110]
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 [96]
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 [91]
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 [111]
Synonyms
HDS 029
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.3 nM
External Link
 Compound Name WHI-P154 Investigative [112]
MOA Inhibitor
External Link
 Compound Name PMID24915291C38 Investigative [113]
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 [114]
MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name PD-0173956 Investigative [114]
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 [114]
Synonyms
PD-166326
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MOA Inhibitor
Activity IC50 = 90 nM
External Link
 Compound Name PP121 Investigative [115]
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 [116]
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 [117]
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 [116]
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 [116]
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 [116]
Synonyms
CHEMBL372076; SCHEMBL3822337
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Osimertinib Approved [10]
Synonyms
Tagrisso
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.421 nM
External Link
 Compound Name PMID27774824-Compound-Figure9Example2down Patented [118]
External Link
 Compound Name Mobocertinib Approved [118]
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
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External Link
 Compound Name DZD9008 Phase 1/2 [118]
External Link
 Compound Name AC0010 Phase 3 [118]
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-
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External Link
 Compound Name EGFR antisense DNA Phase 1/2 [118]
Synonyms
Antisense therapy, UPCI; EGFR antisense DNA, University of Pittsburgh
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External Link
 Compound Name CK-101 Phase 1/2 [118]
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
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External Link
 Compound Name Pyrotinib Phase 1 [118]
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
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External Link
 Compound Name Anti-EGFRvIII CAR transduced PBL Phase 1/2 [118]
External Link
 Compound Name EGFRvIII CAR Phase 1/2 [118]
External Link
 Compound Name Anti-EGFR V III CAR-T cells Phase 1/2 [118]
External Link
 Compound Name EGFRvIII CAR T cells Phase 1 [118]
External Link
 Compound Name CAR-T cells targeting EGFRviii Phase 1 [118]
External Link
 Compound Name Anti-EGFRvIII CAR T cells Phase 1 [118]
External Link
 Compound Name CART-EGFRvIII T cells Phase 1 [118]
External Link
 Compound Name EGFRvIII-CARs Phase 1 [118]
External Link
 Compound Name CAR-T Cells targeting EGFRvIII Phase 1 [118]
External Link
 Compound Name RG6156 Phase 1 [118]
External Link
 Compound Name AMG 596 Phase 1 [118]
External Link
 Compound Name D2C7 Phase 1 [66]
External Link
2C25: Lung cancer 52 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Adagrasib Approved [119]
Synonyms
2326521-71-3; MRTX-849; UNII-8EOO6HQF8Y; 8EOO6HQF8Y; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; CHEMBL4594350; SCHEMBL20974691; GTPL10888; Kras G12C inhibitor MRTX849; BCP31538; EX-A3258; MRTX 849; MFCD32263433; s8884; compound 20 [PMID: 32250617]; BS-16211; HY-130149; CS-0105265; 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
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External Link
 Compound Name Amivantamab Approved [120]
External Link
 Compound Name Mobocertinib Approved [121]
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
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External Link
 Compound Name Sugemalimab Approved in China [122]
External Link
 Compound Name Sacituzumab govitecan Approved [123]
Synonyms
1491917-83-9; 1535963-91-7; 1796566-95-4; CYSTEINYL CL2A-SN-38; DA64T2C2IO; DTXSID401335985; EX-A4354; F82944; GOVITECAN CYSTEINYL CONJUGATE; hRS 7SN38; hRS7-SN38; IMMU 132; IMMU-132; M9BYU8XDQ6; Sacituzumab govitecan; Sacituzumab govitecan [USAN]; sacituzumab-govitecan; Satralizumab linker; SN-38 CYSTEINYL CONJUGATE; UNII-M9BYU8XDQ6
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External Link
 Compound Name Atezolizumab Approved [124]
External Link
 Compound Name Tepotinib Approved [125]
Synonyms
1100598-32-0; EMD 1214063; UNII-1IJV77EI07; Tepotinib (EMD 1214063); EMD1214063; 1IJV77EI07; MSC-2156119J; Benzonitrile, 3-[1,6-dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]-; C29H28N6O2; Tepotinib [INN]; Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]; Benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo
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External Link
 Compound Name Sotorasib Approved [126]
Synonyms
AMG-510; AMG510; AMG-510 racemate; 2252403-56-6; AMG 510; Kras G12C inhibitor 9; 2296729-00-3; UNII-2B2VM6UC8G; 2B2VM6UC8G; CHEMBL4535757; 2296729-00-3 (racemate); 4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one; Sotorasib [INN]; 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-((2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl)pyrido(2,3-d)pyrimidin-2-one; AMG510 racemate; Sotorasib [USAN]; AMG-510(racemate); Kras mutant-targeting AMG 510; SCHEMBL20560375; GTPL10678; AMG 510 pound>>AMG-510; AMY16918; BCP30452; BCP33368; EX-A3538; BDBM50514402; NSC818433; s8830; WHO 11370; DB15569; NSC-818433; BS-16684; HY-114277; CS-0081316; compound (R)-38 [PMID: 31820981]; (1m)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(propan-2-yl)pyridin-3-yl)-4-((2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl)pyrido(2,3-d)pyrimidin-2(1H)-one; (1S)-4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 2296729-66-1; Pyrido(2,3-d)pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(1-methylethyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl)-
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External Link
 Compound Name Entrectinib Approved [127]
Synonyms
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
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External Link
 Compound Name Repotrectinib Approved [128]
Synonyms
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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External Link
 Compound Name MYL-1402O Phase 3 [129]
Synonyms
bevacizumab biosimilar
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External Link
 Compound Name AB154 Phase 3 [130]
Synonyms
Domvanalimab
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External Link
 Compound Name Datopotamab deruxtecan Phase 3 [131]
External Link
 Compound Name CS1001 Phase 3 [132]
External Link
 Compound Name JDQ443 Phase 3 [133]
Synonyms
(S)-JDQ-443; 1-(6-((4S)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one; 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-inda zol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]- 2-Propen-1-one; 1-[6-[(4R)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one; 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one; 1-{6-[(4M)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5- methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2- azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 2653994-08-0; 2653994-10-4; 2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-; AKOS040757949; AT36708; BDBM50579985; CHEMBL5077861; compound 5 [PMID: 35404998]; CS-0226220; CS-0311034; EX-A5693; example 1a [WO2021120890A1]; GLXC-25533; GTPL11715; HY-139612A; JDQ 443; JDQ 443 [WHO-DD]; JDQ443; JDQ-443; MS-29737; NSC846146; NSC-846146; NVP-JDQ443; NVP-JDQ-443; Opnurasib; opnurasib [INN]; -PROPEN-1-ONE, 1-(6-((4R)-4-(5-CHLORO-6-METHYL-1H-INDAZOL-4-YL)-5-METHYL-3-(1-METHYL-1H-INDAZOL-5-YL)-1H-PYRAZOL-1-YL)-2-AZASPIRO(3.3)HEPT-2-YL)-; Q3W0H3V1LQ; SCHEMBL23533580
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External Link
 Compound Name TRS003 Phase 3 [134]
External Link
 Compound Name Tusamitamab ravtansine Phase 3 [135]
Synonyms
SAR408701
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External Link
 Compound Name RG6058 Phase 3 [136]
Synonyms
Tiragolumab
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External Link
 Compound Name GSK4069889 Phase 2 [137]
Synonyms
TSR-022
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External Link
 Compound Name APL-101 Phase 2 [138]
Synonyms
Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
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 Compound Name SGN-LIV1A Phase 2 [139]
Synonyms
Ladiratuzumab Vedotin
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External Link
 Compound Name BNT116 Phase 2 [140]
External Link
 Compound Name AZD7789 Phase 2 [141]
External Link
 Compound Name L-DOS47 Phase 1/2 [142]
External Link
 Compound Name NC318 Phase 2 [143]
External Link
 Compound Name Vorolanib Phase 2 [144]
Synonyms
UNII-YP8G3I74EL; YP8G3I74EL; 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; Vorolanib [INN]; SCHEMBL2439528; CHEMBL4297587; N-((3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; s6843; DB15247; HY-109019; CS-0030517; Q27294638; 1H-Pyrrole-3-carboxamide, N-((3S)-1-((dimethylamino)carbonyl)-3-pyrrolidinyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-
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External Link
 Compound Name Xofigo Phase 2 [145]
External Link
 Compound Name Bintrafusp alfa Phase 2 [146]
External Link
 Compound Name Voyager-V1 Phase 2 [147]
Synonyms
VSV-IFNBeta-NIS
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 Compound Name AB-106 Phase 2 [148]
Synonyms
DS6051b; GTPL11198; AB106
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 Compound Name RO-5126766 Phase 2 [149]
Synonyms
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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 Compound Name TC-210 Phase 1/2 [150]
External Link
 Compound Name EMB-01 Phase 1/2 [151]
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 Compound Name NM21-1480 Phase 1/2 [152]
External Link
 Compound Name MRx0518 Phase 1/2 [153]
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 Compound Name DZD9008 Phase 1/2 [154]
External Link
 Compound Name BGB-A425 Phase 1/2 [155]
External Link
 Compound Name Rilvegostomig Phase 1/2 [156]
Synonyms
AZD2936
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External Link
 Compound Name IK-007 Phase 1/2 [157]
Synonyms
grapiprant
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External Link
 Compound Name IBI318 Phase 1 [158]
External Link
 Compound Name GEN-011 Phase 1 [159]
External Link
 Compound Name ENV-105 Phase 1 [160]
Synonyms
Carotuximab
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External Link
 Compound Name AMG 160 Phase 1 [161]
External Link
 Compound Name ADP-A2M10 Phase 1 [162]
External Link
 Compound Name MEDI5752 Phase 1 [163]
External Link
 Compound Name PF-07104091 Phase 1 [164]
External Link
 Compound Name PF-06936308 Phase 1 [165]
External Link
 Compound Name GEM3PSCA Phase 1 [166]
External Link
 Compound Name PF-07257876 Phase 1 [167]
External Link
 Compound Name Cosibelimab Phase 1 [168]
Synonyms
CK-301/TG-1501
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External Link
 Compound Name Gemcitabine Approved [169]
External Link
 Compound Name SMI-4a Investigative [170]
Synonyms
438190-29-5; SMI 4a; TCS PIM-1 4a; (Z)-SMI-4a; (Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione; (5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione; CHEMBL183906; (5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE; (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione; 327033-36-3; C11H6F3NO2S; (Z)-5-(3-(Trifluoromethyl)benzylidene)-thiazolidine-2,4-dione; (5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione; Pim inhibitor 4a; 3vc4; SMI-4q; TCS PIM-1-4a; 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione; 5-[3-(Trifluoromethyl)benzylidene]thiazolidine-2,4-dione; cc-717; thiazolidine-2,4-dione, 4a; SCHEMBL2541382; SCHEMBL2541388; BDBM26626; AOB6260; EX-A111; SYN1113; BDBM138364; HMS3229J21; 2720AH; HY-16576A; MFCD01152003; s8005; ZINC12576047; AKOS001314163; SMI-4a, >=98% (HPLC); CCG-265027; NCGC00345836-02; NCGC00345836-14; AC-32861; HY-15474; AB0165836; EC-000.2291; J3.561.866J; A11945; W-5256; US8877795, 12; Q27451064; 5-[[3-(trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
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