m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation

m6A Modification:
Crosstalk ID	M6ACROT03420				[1], [2]
Histone modification H3K27ac Epigenetic Regulator YTHDF2 Direct Enhancement m⁶A modification EGFR EGFR YTHDF2 : m⁶A sites
m6A Regulator	YTH domain-containing family protein 2 (YTHDF2)			READER	Regulator Info
m6A Target	Epidermal growth factor receptor (EGFR)				Targert Gene
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type	Histone modification (HistMod)
Regulated Target	Histone H3 lysine 27 acetylation (H3K27ac)				View Details
Downstream Gene	YTHDF2				View Details
Crosstalk Relationship	Histone modification → m6A			Enhancement
Crosstalk Mechanism	Histone modification directly impacts m6A modification through modulating the level of m6A regulator
Crosstalk Summary	H3K4me3 and Histone H3 lysine 27 acetylation (H3K27ac) modification in the promoter region of YTHDF2 enhanced its expression in HCC, and upregulated YTHDF2 in HCC predicted a worse prognosis.YTHDF2 recognized the m6A modification in the 5'-untranslational region of ETS variant transcription factor 5 (ETV5) mRNA and recruited eukaryotic translation initiation factor 3 subunit B to facilitate its translation. YTHDF2 acts as a tumor suppressor to repress cell proliferation and growth via destabilizing the Epidermal growth factor receptor (EGFR) mRNA in HCC.
Responsed Disease	Liver cancer		ICD-11: 2C12		Disease Info
In-vitro Model	QGY-7703	Endocervical adenocarcinoma	Homo sapiens		CVCL_6715
	BEL-7402	Endocervical adenocarcinoma	Homo sapiens		CVCL_5492
	Hep 3B2.1-7	Childhood hepatocellular carcinoma	Homo sapiens		CVCL_0326
	SMMC-7721	Endocervical adenocarcinoma	Homo sapiens		CVCL_0534
In-vivo Model	5 × 10⁶ of HEP3B and SMMC7721 stable cells were resuspended in 0.1 ml of PBS and subcutaneously injected into the flank of mice.

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	[3]
Synonyms	LY3012211 Click to Show/Hide
MOA	Modulator
External Link	TTD: D03WPP
Compound Name	HEGF		Approved	[4]
MOA	Activator
External Link	TTD: D05GGP
Compound Name	Erlotinib		Approved	[5]
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	CID: 176870 TTD: D07POC DrugBank: DB00530
Compound Name	Gefitinib		Approved	[6]
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	CID: 123631 TTD: D09XZB DrugBank: DB00317
Compound Name	Panitumumab		Approved	[7]
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	TTD: D0HU9H
Compound Name	Cetuximab		Approved	[8]
Synonyms	Erbitux; Cetuximab (genetical recombination); Erbitux (TN); Cetuximab (USAN/INN); Cetuximab (genetical recombination) (JAN); novel EGFR mAb inhibitors Click to Show/Hide
External Link	TTD: D0N5OV
Compound Name	BIBW 2992		Approved	[9]
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	CID: 10184653 TTD: D05UFG DrugBank: DB08916
Compound Name	Nitroglycerin		Approved	[4]
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	CID: 4510 TTD: D07YDE DrugBank: DB00727
Compound Name	Epidermal growth factor		Approved	[10]
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	CID: 56841751 TTD: D08TPS
Compound Name	Osimertinib		Approved	[11]
Synonyms	Tagrisso Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.421 nM
External Link	CID: 71496458 TTD: D0O8GK DrugBank: DB09330
Compound Name	NERATINIB MALEATE		Approved	[12]
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	CID: 67307512 TTD: D0U1ZV
Compound Name	Amivantamab		Approved	[13]
MOA	Inhibitor
External Link	TTD: DQ5X1Z
Compound Name	SKI-758		Approved	[14]
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	CID: 11341869 TTD: D03MNN
Compound Name	Dacomitinib		Approved	[10]
Synonyms	PF-00299804 Click to Show/Hide
MOA	Antagonist
Activity	IC50 = 1.8 nM
External Link	CID: 11511120 TTD: D06XXH DrugBank: DB11963
Compound Name	Lapatinib		Approved	[15]
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	CID: 208908 TTD: D08CDI DrugBank: DB01259
Compound Name	Merimepodib		Approved	[16]
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	CID: 153241 TTD: D0F0ZE DrugBank: DB04862
Compound Name	Vandetanib		Approved	[17]
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	CID: 3081361 TTD: D0G6QF DrugBank: DB05294
Compound Name	Sorafenib		Approved	[18]
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	CID: 216239 TTD: D0W5HK DrugBank: DB00398
Compound Name	Icotinib hydrochloride		Registered	[19]
Synonyms	Conmana; Conmanna; Icotinib; BPI-2009-H Click to Show/Hide
MOA	Antagonist
External Link	CID: 44609731 TTD: D06WRJ
Compound Name	Rindopepimut		Phase 3	[3]
MOA	Modulator
External Link	TTD: D05FRP
Compound Name	SYM-004		Phase 3	[20]
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	TTD: D0CR8H
Compound Name	DE-766		Phase 3	[10]
MOA	Modulator
External Link	TTD: D0FJ1W
Compound Name	EGF816		Phase 3	[21]
MOA	Inhibitor
Activity	IC50 = 160.6 nM
External Link	CID: 72703790 TTD: D0K7FY
Compound Name	CO-1686		Phase 3	[22]
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	CID: 57335384 TTD: D0M4AV DrugBank: DB11907
Compound Name	Zalutumumab		Phase 3	[10]
External Link	TTD: D0R4PW
Compound Name	Almonertinib		Phase 3	[23]
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	CID: 121280087 TTD: DDH8L6
Compound Name	ASP1929		Phase 3	[24]
Synonyms	Cetuximab sarotalocan Click to Show/Hide
MOA	Inhibitor
External Link	TTD: DWK96T
Compound Name	A140		Phase 3	[25]
External Link	TTD: DXZ31K
Compound Name	Bevacizumab + Erlotinib		Phase 3	[26]
MOA	Inhibitor
External Link	TTD: D09BKY
Compound Name	HKI-272		Phase 3	[27]
Synonyms	Neratinib (ERBB2 inhibitor) Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.08 nM
External Link	CID: 9915743 TTD: D0Q9CY DrugBank: DB11828
Compound Name	Indium-111		Phase 2/3	[28]
Synonyms	ABT-806 Click to Show/Hide
External Link	TTD: D0F3KC
Compound Name	Varlitinib		Phase 2/3	[29]
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	CID: 42642648 TTD: D00NYJ DrugBank: DB05944
Compound Name	ASP8273		Phase 2	[30]
MOA	Inhibitor
Activity	IC50 = 8 nM
External Link	CID: 71667668 TTD: D02BYZ DrugBank: DB12036
Compound Name	ABT-414		Phase 2	[31]
External Link	TTD: D06XIT
Compound Name	Depatuxizumab		Phase 2	[32]
MOA	Antagonist
External Link	TTD: D0A6CC
Compound Name	Matuzumab		Phase 2	[33]
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	TTD: D0BZ7V
Compound Name	HER1-VSSP vaccine		Phase 2	[34]
Synonyms	HER1-VSSP vaccine (cancer) Click to Show/Hide
External Link	TTD: D0C3LL
Compound Name	RM-1929		Phase 2	[35]
MOA	Antagonist
External Link	TTD: D0FN4T
Compound Name	CetuGEX		Phase 2	[36]
External Link	TTD: D0K9MC
Compound Name	ABX-EGF		Phase 2	[37]
External Link	TTD: D0P9RG
Compound Name	Pelitinib		Phase 2	[38]
Synonyms	EKB-569; EKI-569; WAY-EKB-569 Click to Show/Hide
MOA	Modulator
Activity	IC50 = 8.02 nM
External Link	CID: 6445562 TTD: D0S3PO DrugBank: DB05524
Compound Name	HM-78136B		Phase 2	[35]
Synonyms	Pan-Her/EGFR inhibitors (cancer), Hanmi Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.218 nM
External Link	CID: 25127713 TTD: D00YER DrugBank: DB12114
Compound Name	Pazopanib + Tyverb/Tykerb		Phase 2	[16]
MOA	Inhibitor
External Link	CID: 10113978 TTD: D03UKJ DrugBank: DB06589
Compound Name	MEHD-7945A		Phase 2	[29]
Synonyms	RG-7597; EGFR/HER3 dual monoclonal antibody, Genentech Click to Show/Hide
MOA	Modulator
External Link	TTD: D09BZJ
Compound Name	TT-100		Phase 2	[39]
Synonyms	TT-100, TriAct; Dual IGF-1/EGFR inhibitor (non-small-cell lung cancer), TriAct Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D0T5JS
Compound Name	BMS-599626		Phase 2	[40]
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	CID: 10437018 TTD: D0U4FF DrugBank: DB12318
Compound Name	Tarloxotinib		Phase 2	[41]
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	CID: 51038316 TTD: DUW81M DrugBank: DB14944
Compound Name	VATALANIB		Phase 2	[27]
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	CID: 151194 TTD: D0P6DJ DrugBank: DB04879
Compound Name	BMS-690514		Phase 2	[42]
Synonyms	BMS 690514; BMS690514 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 11349170 TTD: D0R6UV DrugBank: DB11665
Compound Name	CI-1033		Phase 2	[17]
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	CID: 156414 TTD: D0YB3W DrugBank: DB05424
Compound Name	CART-EGFR		Phase 1/2	[43]
MOA	CAR-T-Cell-Therapy
External Link	TTD: D04DHZ
Compound Name	SN-32793		Phase 1/2	[10]
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	TTD: D05ETC
Compound Name	EGFR CART		Phase 1/2	[44]
MOA	CAR-T-Cell-Therapy
External Link	TTD: D0G1ZU
Compound Name	EMD 55900		Phase 1/2	[37]
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	TTD: D0S8BG
Compound Name	TAK-186		Phase 1/2	[45]
MOA	Inhibitor
External Link	TTD: DC1GH7
Compound Name	ZN-e4		Phase 1/2	[46]
MOA	Inhibitor
External Link	TTD: DF0PR6
Compound Name	EMB-01		Phase 1/2	[47]
MOA	Inhibitor
External Link	TTD: DWQ6J1
Compound Name	Sym015		Phase 1/2	[32]
MOA	Antagonist
External Link	TTD: D0B4OK
Compound Name	BDTX-189		Phase 1/2	[48]
Synonyms	2414572-47-5; EX-A4379 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 154824631 TTD: D9FJ5V
Compound Name	AFM24		Phase 1/2	[49]
External Link	TTD: DK8QG3
Compound Name	Sym013		Phase 1/2	[32]
MOA	Antagonist
External Link	TTD: D0FF2G
Compound Name	S-222611		Phase 1b	[50]
MOA	Inhibitor
External Link	TTD: D0V4XY
Compound Name	SYN004		Phase 1	[32]
MOA	Inhibitor
External Link	TTD: D00KML
Compound Name	BIBX-1382		Phase 1	[51]
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	CID: 6918508 TTD: D00RMC DrugBank: DB12966
Compound Name	IMGN289		Phase 1	[52]
MOA	Inhibitor
External Link	TTD: D04HSH
Compound Name	AST-1306		Phase 1	[53]
Synonyms	Allitinib; Allitinib tosylate Click to Show/Hide
MOA	Modulator
External Link	CID: 24739943 TTD: D04OLK
Compound Name	AMG 595		Phase 1	[54]
MOA	Modulator
External Link	TTD: D05LMC
Compound Name	HER-2/HER-1 vaccine		Phase 1	[10]
Synonyms	HER-2/HER-1 vaccine (solid tumors) Click to Show/Hide
External Link	TTD: D0E7RC
Compound Name	EGFR806-specific CAR T cell		Phase 1	[55]
MOA	CAR-T-Cell-Therapy
External Link	TTD: D0I7ZH
Compound Name	PF-05230907		Phase 1	[56]
MOA	Inhibitor
External Link	TTD: D0JS0W
Compound Name	MR1-1		Phase 1	[57]
Synonyms	MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX Click to Show/Hide
MOA	Modulator
External Link	TTD: D0N3PC
Compound Name	Anti-EGFR CAR T		Phase 1	[58]
MOA	CAR-T-Cell-Therapy
External Link	TTD: D0T0SE
Compound Name	AP32788		Phase 1	[35]
MOA	Inhibitor
External Link	TTD: D0X7BN
Compound Name	CLN-081		Phase 1	[59]
MOA	Inhibitor
External Link	TTD: D68RMI
Compound Name	LY3164530		Phase 1	[60]
MOA	Modulator
External Link	TTD: D01IJM
Compound Name	MM-151		Phase 1	[32]
MOA	Antagonist
External Link	TTD: D01NAP
Compound Name	Cipatinib		Phase 1	[29]
Synonyms	HER-1/HER-2 inhibitor (oral, cancer), Jiangsu Hengrui Click to Show/Hide
MOA	Modulator
External Link	TTD: D08JAN
Compound Name	Anti-HER3/EGFR DAF		Phase 1	[61]
MOA	Modulator
External Link	TTD: D0JW2O
Compound Name	BCA101		Phase 1	[62]
MOA	Inhibitor
External Link	TTD: D0U7XJ
Compound Name	CUDC-101		Phase 1	[63]
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	CID: 24756910 TTD: D0Z4RC DrugBank: DB12174
Compound Name	SI-B001		Phase 1	[64]
External Link	TTD: D6JM8Z
Compound Name	CX-904		Phase 1	[65]
Synonyms	AMG 651 Click to Show/Hide
External Link	TTD: D73FNL
Compound Name	AZD9592		Phase 1	[66]
External Link	TTD: DN47VK
Compound Name	D2C7		Phase 1	[67]
External Link	TTD: DR4ND6
Compound Name	MCLA-158		Phase 1	[68]
MOA	Inhibitor
External Link	TTD: DV8I4Q
Compound Name	JNJ-26483327		Phase 1	[69]
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	TTD: D0U3XL
Compound Name	Pyrrolo[2,3-d]pyrimidine derivative 24		Patented	[70]
Synonyms	PMID28705083-Compound-22 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 90468938 TTD: D0Z2PC
Compound Name	PKI166		Discontinued in Phase 2	[71]
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	CID: 6918403 TTD: D07GFF
Compound Name	RG7160		Discontinued in Phase 2	[72]
MOA	Modulator
External Link	TTD: D0E2CQ
Compound Name	PD-153035		Discontinued in Phase 1	[73]
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	CID: 4705 TTD: D0Q7HO
Compound Name	AZD4769		Discontinued in Phase 1	[74]
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	CID: 124437 TTD: D02RZL
Compound Name	TAK165		Discontinued in Phase 1	[17]
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	CID: 6444692 TTD: D0A9OV DrugBank: DB12682
Compound Name	111In-hEGF		Preclinical	[75]
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	TTD: D0V2FZ
Compound Name	EGFR/IGFR tandem adnectin		Preclinical	[76]
Synonyms	BMS-964210 Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D0TI4U
Compound Name	Heparin-EGF-like factor		Terminated	[77]
Synonyms	HB-EGF, Scios Nova; Heparin-EGF-like factor, Scios Nova Click to Show/Hide
MOA	Modulator
External Link	TTD: D02GFZ
Compound Name	CGP-52411		Terminated	[78]
Synonyms	DAPH Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 160 nM
External Link	CID: 1697 TTD: D03QTP
Compound Name	CGP-53353		Terminated	[79]
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	CID: 6711154 TTD: D0HO1S
Compound Name	AZD-9935		Terminated	[80]
MOA	Antagonist
External Link	TTD: D0Y1YX
Compound Name	N4-(3-chlorophenyl)quinazoline-4,6-diamine		Investigative	[81]
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	CID: 11807783 TTD: D00TJF
Compound Name	2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile		Investigative	[82]
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	CID: 5328763 TTD: D00VZA
Compound Name	6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline		Investigative	[83]
Synonyms	CHEMBL250523; BDBM50222432 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 15 nM
External Link	CID: 44442168 TTD: D00WZG
Compound Name	2-cyano-3-(3,4-dihydroxyphenyl)acrylamide		Investigative	[82]
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	CID: 5328768 TTD: D01NTW
Compound Name	HM-61713B		Investigative	[10]
Synonyms	EGFR mutant selective inhibitor (cancer), Hanmi; EMSI (cancer), Hanmi Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D01SQP
Compound Name	Benzyl-quinazolin-4-yl-amine		Investigative	[84]
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	CID: 6603129 TTD: D01WDI
Compound Name	6,7-diethoxy-4-styrylquinazoline		Investigative	[83]
Synonyms	CHEMBL250925 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 15 nM
External Link	CID: 44442181 TTD: D01WXV
Compound Name	AFM-21		Investigative	[10]
Synonyms	Anti-EGFR antibody (RECRUIT-TandAb, colon/solid tumors), Affimed Click to Show/Hide
External Link	TTD: D02FGG
Compound Name	PD182905		Investigative	[85]
MOA	Inhibitor
External Link	TTD: D02GCE
Compound Name	AG 112		Investigative	[86]
Synonyms	tyrphostin A48; tyrphostin AG 112; AG-112; AG112 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 125 nM
External Link	CID: 5328804 TTD: D02KVB
Compound Name	2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile		Investigative	[87]
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	CID: 5328755 TTD: D02RIG
Compound Name	(3-Bromo-phenyl)-quinazolin-4-yl-amine		Investigative	[88]
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	CID: 735125 TTD: D02ZRO
Compound Name	PD-158780		Investigative	[89]
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	CID: 4707 TTD: D03ATU
Compound Name	EGFR inhibitor		Investigative	[90]
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	CID: 9549299 TTD: D03BJB
Compound Name	6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline		Investigative	[83]
Synonyms	CHEMBL399371 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5 nM
External Link	CID: 44442182 TTD: D03CVQ
Compound Name	LA22-radioimmunoconjugates		Investigative	[10]
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	TTD: D03MTY
Compound Name	5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide		Investigative	[91]
Synonyms	CHEMBL382537 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 11717472 TTD: D03WEN
Compound Name	ICR 62		Investigative	[37]
External Link	TTD: D03ZIW
Compound Name	Bmab-200		Investigative	[10]
Synonyms	Anti-EGFR mAb (cancer), Biocon; Anti-epidermal growth factor receptor monoclonal antibody (cancer), Biocon Click to Show/Hide
External Link	TTD: D04GCH
Compound Name	HTS-00213		Investigative	[92]
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	CID: 2809539 TTD: D04HGN
Compound Name	6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline		Investigative	[83]
Synonyms	CHEMBL251123 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 140 nM
External Link	CID: 44442183 TTD: D04LXG
Compound Name	N4-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine		Investigative	[89]
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	CID: 5328077 TTD: D05ARF
Compound Name	Epitinib		Investigative	[10]
Synonyms	HMPL-813; EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma Click to Show/Hide
MOA	Inhibitor
External Link	CID: 59142777 TTD: D05MEY
Compound Name	OSI-75		Investigative	[93]
MOA	Inhibitor
External Link	TTD: D06QEQ
Compound Name	(E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin		Investigative	[94]
Synonyms	CHEMBL213560; SCHEMBL16693054; BDBM50187134 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 710 nM
External Link	CID: 15984068 TTD: D06UEK
Compound Name	HTS-02876		Investigative	[92]
Synonyms	AC1MDGL2; CHEMBL460914; MolPort-002-900-576; ZINC1030761; MCULE-7093116609 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 2810910 TTD: D07CZM
Compound Name	2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile		Investigative	[87]
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	CID: 5328753 TTD: D07IHD
Compound Name	PMID8568816C56		Investigative	[95]
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	CID: 2857 TTD: D07UYV
Compound Name	MT-062		Investigative	[10]
Synonyms	EGFR inhibitor (melanoma), Medisyn Technologies Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D08RXW
Compound Name	Anti-EGFR mab		Investigative	[10]
External Link	TTD: D09RXX
Compound Name	RG-50810		Investigative	[82]
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	CID: 2052 TTD: D0A0JL
Compound Name	IPS-01003		Investigative	[10]
Synonyms	EGFR kinase antagonist (cancer), InnoPharmaScreen Click to Show/Hide
MOA	Antagonist
External Link	TTD: D0AC7C
Compound Name	RM-6427		Investigative	[10]
Synonyms	RM-6428; EGFR tyrosine kinase inhibitors (parasitic infection), Romark Click to Show/Hide
MOA	Inhibitor
External Link	CID: 9931101 TTD: D0AH2V
Compound Name	N4-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine		Investigative	[88]
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	CID: 2426 TTD: D0B4PH
Compound Name	3-Pyridin-4-yl-quinoline-6,7-diol		Investigative	[96]
MOA	Inhibitor
Activity	IC50 = 5000 nM
External Link	CID: 135469328 TTD: D0B8DE
Compound Name	AGT-2000		Investigative	[10]
Synonyms	Gene therapy (intravenous, brain cancer), ArmaGen Click to Show/Hide
MOA	Modulator
External Link	TTD: D0C5WE
Compound Name	3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one		Investigative	[97]
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	CID: 10850934 TTD: D0C9KC
Compound Name	ON-128		Investigative	[10]
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	TTD: D0CY9O
Compound Name	FHT-2107		Investigative	[10]
Synonyms	EGFR-targeting siRNA agent, ForHumanTech Click to Show/Hide
External Link	TTD: D0D0GS
Compound Name	GI-3000		Investigative	[10]
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	TTD: D0D0YK
Compound Name	6,7-dimethoxy-N-m-tolylquinazolin-4-amine		Investigative	[92]
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	CID: 2808977 TTD: D0DF3Z
Compound Name	5,6-Bis-p-tolylamino-isoindole-1,3-dione		Investigative	[79]
Synonyms	CHEMBL7914; SCHEMBL8834183; BDBM50040920 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 4500 nM
External Link	CID: 10360970 TTD: D0EH6L
Compound Name	HTS-05058		Investigative	[90]
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	CID: 5714572 TTD: D0EP1G
Compound Name	N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide		Investigative	[98]
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	CID: 10494722 TTD: D0F6FZ
Compound Name	4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid		Investigative	[82]
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	CID: 14862522 TTD: D0G4HR
Compound Name	Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine		Investigative	[88]
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	CID: 5328245 TTD: D0G9KD
Compound Name	ARX-AHD		Investigative	[10]
Synonyms	Dolastatin-conjugated HER2 antibody (breast cancer), Ambrx Click to Show/Hide
External Link	TTD: D0GB7F
Compound Name	TGF alpha		Investigative	[10]
Synonyms	TGF alpha (neurological damage) Click to Show/Hide
MOA	Modulator
External Link	TTD: D0H3FX
Compound Name	AG 9		Investigative	[86]
Synonyms	tyrphostin 1; tyrphostin A1; AG9; AG-9 Click to Show/Hide
MOA	Inhibitor
Activity	Ki > 400000 nM
External Link	CID: 2063 TTD: D0H3UI
Compound Name	N4-(3-Bromo-phenyl)-quinazoline-4,6-diamine		Investigative	[99]
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	CID: 5328042 TTD: D0HM5W
Compound Name	4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline		Investigative	[100]
Synonyms	CHEMBL473320; SCHEMBL5616932 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 131 nM
External Link	CID: 11696664 TTD: D0I7RA
Compound Name	Theliatinib		Investigative	[10]
Synonyms	HMPL-309; Second EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma Click to Show/Hide
MOA	Inhibitor
External Link	CID: 54759275 TTD: D0J3EA
Compound Name	4-(3-Bromo-phenylamino)-quinazoline-6,7-diol		Investigative	[88]
MOA	Inhibitor
External Link	CID: 5328050 TTD: D0J9WO
Compound Name	6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline		Investigative	[83]
Synonyms	CHEMBL250318; BDBM50222435 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 14 nM
External Link	CID: 44442165 TTD: D0K2VO
Compound Name	4-(2-nitroprop-1-enyl)benzene-1,2-diol		Investigative	[82]
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	CID: 3260632 TTD: D0K2YY
Compound Name	EDP-13		Investigative	[10]
Synonyms	Epidermal growth factor receptor antagonist (cancer), BiolineRx/Matrix Pharma Click to Show/Hide
MOA	Antagonist
External Link	TTD: D0K3FG
Compound Name	N4-(3-Bromo-phenyl)-quinazoline-4,7-diamine		Investigative	[84]
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	CID: 5328045 TTD: D0K7GD
Compound Name	(S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate		Investigative	[82]
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	CID: 5491980 TTD: D0KN1L
Compound Name	4-(2-nitrovinyl)benzene-1,2-diol		Investigative	[82]
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	CID: 6439158 TTD: D0L3SN
Compound Name	AG-538		Investigative	[82]
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	CID: 5328760 TTD: D0NH7M
Compound Name	WZ-3146		Investigative	[10]
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	CID: 44607360 TTD: D0NJ3Q
Compound Name	2-methoxy-4-(2-nitrovinyl)phenol		Investigative	[82]
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	CID: 638439 TTD: D0O9UR
Compound Name	MG-111		Investigative	[101]
Synonyms	134865-04-6; EGF, Hitachi Click to Show/Hide
MOA	Modulator
External Link	CID: 16143379 TTD: D0P0JW
Compound Name	6,7-dimethoxy-4-(2-phenylethynyl)quinazoline		Investigative	[83]
Synonyms	CHEMBL250315; SCHEMBL6180450; BDBM50222433 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5600 nM
External Link	CID: 18770812 TTD: D0P2GE
Compound Name	Anti-EGFR humanized mabs		Investigative	[10]
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	TTD: D0R2RV
Compound Name	4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline		Investigative	[83]
Synonyms	CHEMBL250924; BDBM50222419 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 26 nM
External Link	CID: 44442180 TTD: D0S9QP
Compound Name	AL-6802		Investigative	[10]
Synonyms	EGFR modulators (cancer), Advenchen/Simcere Click to Show/Hide
MOA	Modulator
External Link	TTD: D0T7OS
Compound Name	BPIQ-I		Investigative	[88]
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	CID: 2427 TTD: D0U6WB
Compound Name	mabionHER2		Investigative	[10]
Synonyms	Humanized monoclonal antibody (breast cancer), Mabion Click to Show/Hide
External Link	TTD: D0V0JV
Compound Name	4-(2-nitrovinyl)phenol		Investigative	[82]
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	CID: 638437 TTD: D0W1BE
Compound Name	4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide		Investigative	[91]
Synonyms	CHEMBL200958 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 44406548 TTD: D0W2PQ
Compound Name	MDP-01		Investigative	[10]
Synonyms	Peptabody-EGF (anticancer), Med Discovery Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D0WD8R
Compound Name	N4-(3-methylphenyl)-4,6-quinazolinediamine		Investigative	[102]
Synonyms	CHEMBL336113; Anilinoquinazoline, 4a; 6-amino-4-[(3-methylphenyl)amino]quinazoline; SMA52; SCHEMBL159209; ZINC6328; SMA-52; NFBCSWGEYDCCDW-UHFFFAOYSA-N; BDBM50133384; AKOS013914431; N4-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	CID: 10220590 TTD: D0X4UE
Compound Name	RX-1792		Investigative	[10]
Synonyms	EGF antagonist, Rexahn; RX-0183 Click to Show/Hide
MOA	Antagonist
External Link	TTD: D0Y1LD
Compound Name	(3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine		Investigative	[84]
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	CID: 5328038 TTD: D0Y2AM
Compound Name	NRC-2694		Investigative	[10]
MOA	Inhibitor
External Link	CID: 16129168 TTD: D0Y6MD
Compound Name	Cochliobolic acid		Investigative	[103]
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	CID: 6450172 TTD: D0ZT9D
Compound Name	PD-168393		Investigative	[104]
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	CID: 4708 TTD: D01VFR DrugBank: DB07662
Compound Name	N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide		Investigative	[98]
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	CID: 9995195 TTD: D01WYI
Compound Name	4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline		Investigative	[105]
Synonyms	CHEMBL98798 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 70 nM
External Link	CID: 44331231 TTD: D03HLH
Compound Name	4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline		Investigative	[105]
Synonyms	CHEMBL101581 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2500 nM
External Link	CID: 44331083 TTD: D05QMN
Compound Name	YH013		Investigative	[106]
External Link	TTD: D0AM9O
Compound Name	LAVENDUSTIN A		Investigative	[107]
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	CID: 3894 TTD: D0D9TU
Compound Name	PF 5208766		Investigative	[108]
Synonyms	WAY-178357 Click to Show/Hide
MOA	Modulator
External Link	TTD: D0J2CP
Compound Name	6-chloro-N-(3-chlorophenyl)quinazolin-4-amine		Investigative	[109]
Synonyms	4-Anilidoquinazoline deriv. 12a; AC1NS5EY; SCHEMBL4355658; BDBM4397 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2700 nM
External Link	CID: 5328819 TTD: D0J5SK
Compound Name	N-(4-(phenylamino)quinazolin-6-yl)acrylamide		Investigative	[104]
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	CID: 10401956 TTD: D0N8TQ DrugBank: DB08462
Compound Name	AG-213		Investigative	[100]
MOA	Inhibitor
Activity	Ki = 850 nM
External Link	CID: 667601 TTD: D0Q3GG
Compound Name	SYM-011		Investigative	[10]
Synonyms	Dimercept; Hermodulins; Herstatin; RB-200; RBLX-200; RBLX-242; RBLX-242h; RBLX-642h Click to Show/Hide
MOA	Modulator
External Link	TTD: D0Q8GX
Compound Name	10-hydroxy-18-methoxybetaenone		Investigative	[110]
Synonyms	CHEMBL498247; BDBM50269144 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 10500 nM
External Link	CID: 10644450 TTD: D0W6CE
Compound Name	4557W		Investigative	[111]
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	CID: 9843206 TTD: D0X4OU
Compound Name	Tyrphostin ag-1478		Investigative	[97]
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	CID: 2051 TTD: D0ZH1U
Compound Name	CL-387785		Investigative	[92]
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	CID: 2776 TTD: D00TZD
Compound Name	HDS-029		Investigative	[112]
Synonyms	HDS 029 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.3 nM
External Link	CID: 11566580 TTD: D05FFT
Compound Name	WHI-P154		Investigative	[113]
MOA	Inhibitor
External Link	CID: 3795 TTD: D0E5IP
Compound Name	PMID24915291C38		Investigative	[114]
Synonyms	GTPL8145; PLS-123; BDBM50020476; 1431727-04-6 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 7 nM
External Link	CID: 71556703 TTD: D06BJG
Compound Name	HKI-9924129		Investigative	[115]
MOA	Inhibitor
Activity	IC50 = 390 nM
External Link	CID: 5311104 TTD: D0D5EW
Compound Name	PD-0173956		Investigative	[115]
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	CID: 5330524 TTD: D0GW4Q
Compound Name	PD-0166326		Investigative	[115]
Synonyms	PD-166326 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 90 nM
External Link	CID: 447700 TTD: D0P3JW DrugBank: DB08339
Compound Name	PP121		Investigative	[116]
Synonyms	PP-121; PP 121 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 260 nM
External Link	CID: 24905142 TTD: D03EHM DrugBank: DB08052
Compound Name	3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione		Investigative	[117]
Synonyms	CHEMBL380598; SCHEMBL3148490; HVQJGNALTWNDMX-UHFFFAOYSA-N; BDBM50375058; 2-(1H-Indole-3-yl)-3-phenylmaleimide Click to Show/Hide
MOA	Inhibitor
External Link	CID: 15422868 TTD: D06AOY
Compound Name	Ro-4396686		Investigative	[118]
Synonyms	SCHEMBL5809947; CHEMBL606964 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 545 nM
External Link	CID: 11396738 TTD: D09XIL
Compound Name	3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione		Investigative	[117]
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	CID: 10946795 TTD: D00NYT
Compound Name	3,4-diphenyl-1H-pyrrole-2,5-dione		Investigative	[117]
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	CID: 2752461 TTD: D0C3WY
Compound Name	3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione		Investigative	[117]
Synonyms	CHEMBL372076; SCHEMBL3822337 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 11572699 TTD: D0EK0G
Compound Name	Osimertinib		Approved	[11]
Synonyms	Tagrisso Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.421 nM
External Link	CID: 71496458 TTD: D0O8GK DrugBank: DB09330
Compound Name	PMID27774824-Compound-Figure9Example2down		Patented	[119]
External Link	TTD: D01DBB
Compound Name	Mobocertinib		Approved	[119]
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	CID: 118607832 TTD: DI4HA7
Compound Name	DZD9008		Phase 1/2	[119]
External Link	TTD: DM8Y2N
Compound Name	AC0010		Phase 3	[119]
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	CID: 72734520 TTD: D0FV3K DrugBank: DB15327
Compound Name	EGFR antisense DNA		Phase 1/2	[119]
Synonyms	Antisense therapy, UPCI; EGFR antisense DNA, University of Pittsburgh Click to Show/Hide
External Link	TTD: D06VFF
Compound Name	CK-101		Phase 1/2	[119]
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	CID: 117909640 TTD: D09BZS
Compound Name	Pyrotinib		Phase 1	[119]
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	CID: 51039030 TTD: D0M8YM DrugBank: DB14993
Compound Name	Anti-EGFRvIII CAR transduced PBL		Phase 1/2	[119]
External Link	TTD: D08RJY
Compound Name	EGFRvIII CAR		Phase 1/2	[119]
External Link	TTD: D0LU4N
Compound Name	Anti-EGFR V III CAR-T cells		Phase 1/2	[119]
External Link	TTD: D0Q4EJ
Compound Name	EGFRvIII CAR T cells		Phase 1	[119]
External Link	TTD: D01LWE
Compound Name	CAR-T cells targeting EGFRviii		Phase 1	[119]
External Link	TTD: D03CMZ
Compound Name	Anti-EGFRvIII CAR T cells		Phase 1	[119]
External Link	TTD: D09OSC
Compound Name	CART-EGFRvIII T cells		Phase 1	[119]
External Link	TTD: D0B5PV
Compound Name	EGFRvIII-CARs		Phase 1	[119]
External Link	TTD: D0PT2M
Compound Name	CAR-T Cells targeting EGFRvIII		Phase 1	[119]
External Link	TTD: D0ZQ6N
Compound Name	RG6156		Phase 1	[119]
External Link	TTD: DF8X5N
Compound Name	AMG 596		Phase 1	[119]
External Link	TTD: DOJ6E8
Compound Name	D2C7		Phase 1	[67]
External Link	TTD: DR4ND6
2C12: Liver cancer		49 Compound(s) Regulating the Disease	Click to Show/Hide the Full List
Compound Name	90Y-loaded resin microspheres		Approved	[120]
External Link	TTD: DGWE36
Compound Name	Thymalfasin		Phase 2	[121]
Synonyms	Zadaxin; 62304-98-7; Thymosin alpha1; Thymosin alpha 1; Thymosin alpha1 (ox); Thymosin alpha1 (human); Thymalfasin [USAN:INN]; UNII-W0B22ISQ1C; Thymosin-alpha-1; 69440-99-9; Thymosin alpha1 (cattle); C129H215N33O55; W0B22ISQ1C; Zadaxin (TN); Thymalfasin alfa 1 Click to Show/Hide
External Link	CID: 16130571 TTD: D0I5KX
Compound Name	Ferumoxides		Approved	[122]
Synonyms	AMI-25; 119683-68-0; Feridex; Feridex IV; Superparamagnetic iron oxide; UNII-G6N3J05W84; Ferumoxides [USAN:USP:BAN]; CCRIS 6722; HSDB 8072; AC1O5DID; G6N3J05W84; iron(2+); iron(3+); Iron oxide crystal is inverse spinel (X-ray data); Fe(II) and Fe(III) are present (Mossbauer Spectroscopy; Physical form is a colloidal particle of nonstoichiometric Click to Show/Hide
External Link	CID: 6432052 TTD: D08QAC DrugBank: DB06215
Compound Name	DTI-015		Approved	[123]
Synonyms	Carmustine; 154-93-8; 1,3-Bis(2-chloroethyl)-1-nitrosourea; BCNU; Carmustin; Nitrumon; Carmubris; Gliadel; BiCNU; Bi CNU; Carmustinum; Bischlorethylnitrosurea; Bischlorethylnitrosourea; Carmustina; Becenun; Becenum; Bischloroethyl nitrosourea; N,N'-BIS(2-CHLOROETHYL)-N-NITROSOUREA; Bis(2-chloroethyl)nitrosourea; Urea, N,N'-bis(2-chloroethyl)-N-nitroso-; Gliadel Wafer; FDA 0345; Bischloroethylnitrosourea; SRI 1720; 1,3-Bis(2-chloroethyl)nitrosourea; BiCNU (TN); Carmustinum [INN-Latin]; Carmustina [INN-Spanish]; DTI 015; NCI-C04773; SK; Injectable carmustine, Direct Therapeutics Click to Show/Hide
External Link	CID: 2578 TTD: D01OXI DrugBank: DB00262
Compound Name	Nofazinlimab		Phase 3	[124]
Synonyms	CS1003; EQ176 Click to Show/Hide
External Link	TTD: DX9GT7
Compound Name	PV-10		Phase 3	[35]
Synonyms	632-69-9; Rose bengal sodium; Rose bengal disodium salt; R105 sodium; Rose-bengal (131 I) natrium; Food Red No 105, sodium salt; EINECS 211-183-3; Food Red Color No 105, sodium salt; Sel disodique de rose bengale iodee (131 I); Rose bengale (131 I) sodique [INN-French]; Rosa bengala sodica (131 I) [INN-Spanish]; Roseum bengalense (131 I) natricum [INN-Latin]; 2,4,5,7-Tetraido(m,p,o',m')tetrachlorofluorescein, disodium salt; Fluorescein, 4,5,6,7-tetrachloro-2',4',5',7'-tetraiodo-, disodium salt; Disodium Click to Show/Hide
External Link	CID: 69438 TTD: D0L2VT
Compound Name	Brivanib		Phase 3	[125]
Synonyms	649735-46-6; BMS-540215; Brivanib (BMS-540215); BMS 540215; UNII-DDU33B674I; Brivanib [USAN]; BMS540215; DDU33B674I; CHEMBL377300; (2R)-1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]propanol; Brivanib (USAN); (2R)-1-[4-[(4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY]-5-METHYL-PYRROLO[2,1-F][1,2,4]TRIAZIN-6-YL]OXYPROPAN-2-OL; (2R)-1-({4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl}oxy)propan-2-ol Click to Show/Hide
External Link	CID: 11234052 TTD: D0HS5V DrugBank: DB11958
Compound Name	JX-594		Phase 3	[126]
Synonyms	Pexastimogene devacirepvec Click to Show/Hide
External Link	TTD: D0HB0V
Compound Name	ABH001		Phase 3	[127]
External Link	TTD: D05LPP
Compound Name	MTC-DOX		Phase 2/3	[128]
Synonyms	MTC-doxorubicin Click to Show/Hide
External Link	TTD: D0W9AI
Compound Name	KD018		Phase 2	[129]
External Link	TTD: D0NB9T
Compound Name	Doxorubicin-eluting beads		Phase 2	[130]
Synonyms	DC Bead (TN) Click to Show/Hide
External Link	TTD: D0M5CD
Compound Name	32-P BioSilicon		Phase 2	[131]
Synonyms	BrachySil Click to Show/Hide
External Link	TTD: D0M1YS
Compound Name	Cixutumumab		Phase 2	[132]
Synonyms	LY3012217 Click to Show/Hide
External Link	TTD: D0E5DP
Compound Name	[131I]-Metuximab		Phase 2	[133]
External Link	TTD: D0E5BW
Compound Name	Darinaparsin		Phase 2	[134]
Synonyms	ZIO-101 Click to Show/Hide
External Link	CID: 11683005 TTD: D03ZME DrugBank: DB06179
Compound Name	Tigatuzumab		Phase 2	[135]
External Link	TTD: D03LTO
Compound Name	CMC-001		Phase 2	[136]
Synonyms	Manganese-based MRI contrast agent (liver tumor imaging), CMC Contrast Click to Show/Hide
External Link	TTD: D00WMJ
Compound Name	OBP-301		Phase 1/2	[137]
External Link	TTD: D0D8ZK
Compound Name	MBO7133		Phase 1/2	[138]
External Link	TTD: D0C3MW
Compound Name	INCB62079		Phase 1/2	[35]
External Link	TTD: D0BE8H
Compound Name	NV-1020		Phase 1/2	[139]
External Link	TTD: D0B6EA
Compound Name	DCVax-Liver		Phase 1/2	[140]
Synonyms	Dendritic cell-based immunotherapy (liver cancer), Northwest Biotherapeutics Click to Show/Hide
External Link	TTD: D00ESH
Compound Name	SRF388		Phase 1	[141]
External Link	TTD: DLY89F
Compound Name	ET140202		Phase 1	[142]
External Link	TTD: D4K2OF
Compound Name	ADP-A2AFP		Phase 1	[143]
External Link	TTD: D31ORV
Compound Name	SM04755		Phase 1	[144]
External Link	TTD: D0P5XM
Compound Name	Anti-CEA CAR-T therapy		Phase 1	[35]
External Link	TTD: D0OP1L
Compound Name	PI-166		Phase 1	[145]
External Link	TTD: D0J2YR
Compound Name	CRS-100		Phase 1	[146]
External Link	TTD: D0B4DL
Compound Name	Autologous ET1402L1-CART cells		Phase 1	[147]
External Link	TTD: D09TGO
Compound Name	Anti-CD133-CAR vector-transduced T cells		Phase 1	[148]
External Link	TTD: D09HRH
Compound Name	MRX34		Phase 1	[149]
External Link	TTD: D08SJY
Compound Name	ALN-VSP		Phase 1	[150]
External Link	TTD: D08JMI
Compound Name	EPCAM-targeted CAR-T cells		Clinical trial	[151]
External Link	TTD: D0T8DD
Compound Name	ADI		Discontinued in Phase 3	[152]
Synonyms	Arginine deiminase Click to Show/Hide
External Link	CID: 46906074 TTD: D0O4EV
Compound Name	GN-1140		Discontinued in Phase 2	[153]
External Link	TTD: D0V4CL
Compound Name	OGT-719		Discontinued in Phase 2	[154]
Synonyms	OGS-719 Click to Show/Hide
External Link	CID: 9838997 TTD: D0C2CH
Compound Name	AFP-Scan		Discontinued in Phase 2	[155]
External Link	TTD: D08CCC
Compound Name	SR1078		Preclinical	[156]
Synonyms	1246525-60-9; SR 1078; SR-1078; N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide; CHEMBL3094387; N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide; N-[4-[2,2,2-Trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)benzamide; SCHEMBL4880524; C17H10F9NO2; DTXSID30591895; BCP09203; EX-A2215; 4063AH; BDBM50444350; s5775; ZINC98052696; AKOS024458390; CS-1045; NCGC00379222-02; AK547149; AS-55921; HY-14422; W-5797; SR-03000001078; SR-03000001078-1; SR-03000001078-2 Click to Show/Hide
External Link	CID: 17980288 TTD: D9D6QN
Compound Name	Occlusin		Preclinical	[157]
Synonyms	Occlusin 50 Injection; Occlusin 500 injection Click to Show/Hide
External Link	TTD: D00INM
Compound Name	HRC-201		Terminated	[158]
Synonyms	Hemoglobin-imaging conjugate (HepSelect), Hemosol Click to Show/Hide
External Link	TTD: D09ZCH
Compound Name	1,2,3,4,5,6-hexabromocyclohexane		Investigative	[159]
Synonyms	1837-91-8; Benzene hexabromide; Cyclohexane, 1,2,3,4,5,6-hexabromo-; Hexabromocyclohexane; JAK2 Inhibitor II; ACMC-1BQJT; SCHEMBL459442; trans-alpha-Benzene hexabromide; CHEMBL444236; DTXSID4052687; CHEBI:93940; NSC7908; HMS3268H22; HMS3413C10; HMS3677C10; NSC-7908; ZINC1586309; ANW-23174; MFCD00059127; s5902; Cyclohexane,2,3,4,5,6-hexabromo-; AKOS015836040; 1,2,3,4,5,6-Hexabromo-cyclohexane; 1,2,3,4,5,6-Hexabromocyclohexane #; NCGC00092358-01; NCGC00092358-02; 1,2,3,4,5,6-hexakis(bromanyl)cyclohexane; A4510; FT-0633875; JAK2 Inhibitor II - CAS 1837-91-8; 1,2,3,4,5,6-Hexabromocyclohexane;NSC7908; A812818; 1,2,3,4,5,6-Hexabrom-cyclohexan (I(2)-Form); J-011778; 1,2,3,4,5,6-Hexabromocyclohexane, >=98% (HPLC); BRD-K06817181-001-01-5; Q27165694 Click to Show/Hide
External Link	CID: 74603 TTD: DLW69V
Compound Name	STP-322		Investigative	[160]
Synonyms	Multi-targeted siRNA therapeutic cocktail (nanoparticle, liver tumor), Sirnaomics Click to Show/Hide
External Link	TTD: D0R8KF
Compound Name	AMB-8LK		Investigative	[160]
Synonyms	Cancer therapy (monoclonal antibody), MAT Biopharma; Y90 anti-ferritin monoclonal antibody (cancer), MAT Biopharma; Yttrium-90 anti-ferritin mAb (cancer), MAT Biopharma; Yttrium-90 anti-ferritin mAb (Hodgkin's disease/pancreatic/liver cancer), MAT Biopharma; 90Y-AMB8LK mAb (cancer), MAT Biopharma; 90Y-AMB8LK monoclonal antibody (cancer), MAT Biopharma; 90Y-labelled anti-ferritin monoclonal antibody (cancer), MAT Biopharma Click to Show/Hide
External Link	TTD: D0P2MD
Compound Name	MiR-34a mimics		Investigative	[160]
Synonyms	MiR-34a mimics (liver cancer) Click to Show/Hide
External Link	TTD: D0M9TD
Compound Name	P53 fusion protein		Investigative	[160]
Synonyms	P53 fusion protein (pancreatic/liver cancer) Click to Show/Hide
External Link	TTD: D06WLG
Compound Name	OP-05		Investigative	[160]
Synonyms	OP-05 program (prodrug, liver tumor); OP-05 program (prodrug, liver tumor), Onco-Pharmakon Click to Show/Hide
External Link	TTD: D02OIP
Compound Name	GR-DD1		Investigative	[160]
Synonyms	Cytotoxin (hepatic metastasis), ERYtech Click to Show/Hide
External Link	TTD: D00QFV

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Correspondence

Prof. Feng ZHU

Prof. Shuiping Liu

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