m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT05378
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[1] | |||
m6A modification
MIR7-1
MIR7-1
ALKBH5
Demethylation
: m6A sites
Direct
Inhibition
Non-coding RNA
miR-7
EGFR
lncRNA miRNA circRNA
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| m6A Modification: | |||||
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| m6A Regulator | RNA demethylase ALKBH5 (ALKBH5) | ERASER | |||
| m6A Target | microRNA 7-1 (MIR7-1) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Non-coding RNA (ncRNA) | ||||
| Epigenetic Regulator | MicroRNA 7-1 (MIR7-1) | microRNA | View Details | ||
| Regulated Target | Epidermal growth factor receptor (EGFR) | View Details | |||
| Crosstalk Relationship | m6A → ncRNA | Inhibition | |||
| Crosstalk Mechanism | m6A regulators directly modulate the functionality of ncRNAs through specific targeting ncRNA | ||||
| Crosstalk Summary | ALKBH5 is a tumor-promoting gene in epithelial ovarian cancer, which is involved in the mTOR pathway and microRNA 7-1 (MIR7-1)-Beclin1 complex. ALKBH5 activated Epidermal growth factor receptor (EGFR)-PIK3CA-AKT-mTOR signaling pathway. ALKBH5 inhibited autophagy of epithelial ovarian cancer through microRNA 7-1 (MIR7-1) and BCL-2. | ||||
| Responsed Disease | Ovarian cancer | ICD-11: 2C73 | |||
| Pathway Response | PI3K-Akt signaling pathway | hsa04151 | |||
| mTOR signaling pathway | hsa04150 | ||||
| Autophagy | hsa04140 | ||||
In-vitro Model |
A2780 | Ovarian endometrioid adenocarcinoma | Homo sapiens | CVCL_0134 | |
| SK-OV-3 | Ovarian serous cystadenocarcinoma | Homo sapiens | CVCL_0532 | ||
| OVCAR-3 | Ovarian serous adenocarcinoma | Homo sapiens | CVCL_0465 | ||
| CoC1 | Ovarian adenocarcinoma | Homo sapiens | CVCL_6891 | ||
| In-vivo Model | SKOV3 or A2780 cells were infected with the indicated lentiviral vectors and injected (5 × 106 cells/mouse in 200 uL volume) subcutaneously into the left armpit of 6-week-old BALB/c nude mice. After 21 days, the animals were sacrificed to confirm the presence of tumors and weigh the established tumors. | ||||
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 | ||
| Necitumumab | Approved | [2] | ||
| Synonyms |
LY3012211
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| MOA | Modulator | |||
| External Link | ||||
| HEGF | Approved | [3] | ||
| MOA | Activator | |||
| External Link | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| 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 | |||
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| Osimertinib | Approved | [10] | ||
| Synonyms |
Tagrisso
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.421 nM | |||
| External Link | ||||
| 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 | ||||
| Amivantamab | Approved | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| Dacomitinib | Approved | [9] | ||
| Synonyms |
PF-00299804
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| MOA | Antagonist | |||
| Activity | IC50 = 1.8 nM | |||
| External Link | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| 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 | ||||
| Icotinib hydrochloride | Registered | [18] | ||
| Synonyms |
Conmana; Conmanna; Icotinib; BPI-2009-H
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| MOA | Antagonist | |||
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| Rindopepimut | Phase 3 | [2] | ||
| MOA | Modulator | |||
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| 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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| DE-766 | Phase 3 | [9] | ||
| MOA | Modulator | |||
| External Link | ||||
| EGF816 | Phase 3 | [20] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 160.6 nM | |||
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| 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 | |||
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| Zalutumumab | Phase 3 | [9] | ||
| External Link | ||||
| 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 | |||
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| ASP1929 | Phase 3 | [23] | ||
| Synonyms |
Cetuximab sarotalocan
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| MOA | Inhibitor | |||
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| A140 | Phase 3 | [24] | ||
| External Link | ||||
| Bevacizumab + Erlotinib | Phase 3 | [25] | ||
| MOA | Inhibitor | |||
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| HKI-272 | Phase 3 | [26] | ||
| Synonyms |
Neratinib (ERBB2 inhibitor)
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.08 nM | |||
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| Indium-111 | Phase 2/3 | [27] | ||
| Synonyms |
ABT-806
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| 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 | |||
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| ASP8273 | Phase 2 | [29] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
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| ABT-414 | Phase 2 | [30] | ||
| External Link | ||||
| Depatuxizumab | Phase 2 | [31] | ||
| MOA | Antagonist | |||
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| 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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| HER1-VSSP vaccine | Phase 2 | [33] | ||
| Synonyms |
HER1-VSSP vaccine (cancer)
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| RM-1929 | Phase 2 | [34] | ||
| MOA | Antagonist | |||
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| CetuGEX | Phase 2 | [35] | ||
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| ABX-EGF | Phase 2 | [36] | ||
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| Pelitinib | Phase 2 | [37] | ||
| Synonyms |
EKB-569; EKI-569; WAY-EKB-569
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| MOA | Modulator | |||
| Activity | IC50 = 8.02 nM | |||
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| HM-78136B | Phase 2 | [34] | ||
| Synonyms |
Pan-Her/EGFR inhibitors (cancer), Hanmi
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.218 nM | |||
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| Pazopanib + Tyverb/Tykerb | Phase 2 | [15] | ||
| MOA | Inhibitor | |||
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| MEHD-7945A | Phase 2 | [28] | ||
| Synonyms |
RG-7597; EGFR/HER3 dual monoclonal antibody, Genentech
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| MOA | Modulator | |||
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| 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 | |||
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| 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 | ||||
| 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 | ||||
| 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 | ||||
| BMS-690514 | Phase 2 | [41] | ||
| Synonyms |
BMS 690514; BMS690514
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | Ki = 0.11 nM | |||
| External Link | ||||
| CART-EGFR | Phase 1/2 | [42] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| EGFR CART | Phase 1/2 | [43] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| 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
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| External Link | ||||
| TAK-186 | Phase 1/2 | [44] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| ZN-e4 | Phase 1/2 | [45] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| EMB-01 | Phase 1/2 | [46] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Sym015 | Phase 1/2 | [31] | ||
| MOA | Antagonist | |||
| External Link | ||||
| BDTX-189 | Phase 1/2 | [47] | ||
| Synonyms |
2414572-47-5; EX-A4379
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| MOA | Inhibitor | |||
| External Link | ||||
| AFM24 | Phase 1/2 | [48] | ||
| External Link | ||||
| Sym013 | Phase 1/2 | [31] | ||
| MOA | Antagonist | |||
| External Link | ||||
| S-222611 | Phase 1b | [49] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| SYN004 | Phase 1 | [31] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Antagonist | |||
| Activity | IC50 = 3 nM | |||
| External Link | ||||
| IMGN289 | Phase 1 | [51] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AST-1306 | Phase 1 | [52] | ||
| Synonyms |
Allitinib; Allitinib tosylate
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| MOA | Modulator | |||
| External Link | ||||
| AMG 595 | Phase 1 | [53] | ||
| MOA | Modulator | |||
| External Link | ||||
| HER-2/HER-1 vaccine | Phase 1 | [9] | ||
| Synonyms |
HER-2/HER-1 vaccine (solid tumors)
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| External Link | ||||
| EGFR806-specific CAR T cell | Phase 1 | [54] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| PF-05230907 | Phase 1 | [55] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| Anti-EGFR CAR T | Phase 1 | [57] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| AP32788 | Phase 1 | [34] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CLN-081 | Phase 1 | [58] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| LY3164530 | Phase 1 | [59] | ||
| MOA | Modulator | |||
| External Link | ||||
| MM-151 | Phase 1 | [31] | ||
| MOA | Antagonist | |||
| External Link | ||||
| Cipatinib | Phase 1 | [28] | ||
| Synonyms |
HER-1/HER-2 inhibitor (oral, cancer), Jiangsu Hengrui
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| MOA | Modulator | |||
| External Link | ||||
| Anti-HER3/EGFR DAF | Phase 1 | [60] | ||
| MOA | Modulator | |||
| External Link | ||||
| BCA101 | Phase 1 | [61] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Modulator | |||
| Activity | IC50 = 2.4 nM | |||
| External Link | ||||
| SI-B001 | Phase 1 | [63] | ||
| External Link | ||||
| CX-904 | Phase 1 | [64] | ||
| Synonyms |
AMG 651
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| External Link | ||||
| AZD9592 | Phase 1 | [65] | ||
| External Link | ||||
| D2C7 | Phase 1 | [66] | ||
| External Link | ||||
| MCLA-158 | Phase 1 | [67] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| Pyrrolo[2,3-d]pyrimidine derivative 24 | Patented | [69] | ||
| Synonyms |
PMID28705083-Compound-22
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Modulator | |||
| Activity | IC50 = 3.7 nM | |||
| External Link | ||||
| RG7160 | Discontinued in Phase 2 | [71] | ||
| MOA | Modulator | |||
| External Link | ||||
| 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 | ||||
| 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 | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| EGFR/IGFR tandem adnectin | Preclinical | [75] | ||
| Synonyms |
BMS-964210
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| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| CGP-52411 | Terminated | [77] | ||
| Synonyms |
DAPH
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| MOA | Inhibitor | |||
| Activity | Ki = 160 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 700 nM | |||
| External Link | ||||
| AZD-9935 | Terminated | [79] | ||
| MOA | Antagonist | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 3.38 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 1000 nM | |||
| External Link | ||||
| 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 | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | Ki = 3500 nM | |||
| External Link | ||||
| HM-61713B | Investigative | [9] | ||
| Synonyms |
EGFR mutant selective inhibitor (cancer), Hanmi; EMSI (cancer), Hanmi
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 6,7-diethoxy-4-styrylquinazoline | Investigative | [82] | ||
| Synonyms |
CHEMBL250925
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| MOA | Inhibitor | |||
| Activity | IC50 = 15 nM | |||
| External Link | ||||
| AFM-21 | Investigative | [9] | ||
| Synonyms |
Anti-EGFR antibody (RECRUIT-TandAb, colon/solid tumors), Affimed
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| External Link | ||||
| PD182905 | Investigative | [84] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| 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 | ||||
| (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)-
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| MOA | Inhibitor | |||
| Activity | IC50 = 27 nM | |||
| External Link | ||||
| 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-
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.008 nM | |||
| External Link | ||||
| 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 | ||||
| 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 | ||||
| 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
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| MOA | Modulator | |||
| External Link | ||||
| 5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide | Investigative | [90] | ||
| Synonyms |
CHEMBL382537
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| ICR 62 | Investigative | [36] | ||
| External Link | ||||
| Bmab-200 | Investigative | [9] | ||
| Synonyms |
Anti-EGFR mAb (cancer), Biocon; Anti-epidermal growth factor receptor monoclonal antibody (cancer), Biocon
Click to Show/Hide
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| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 6300 nM | |||
| External Link | ||||
| 6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline | Investigative | [82] | ||
| Synonyms |
CHEMBL251123
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 140 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 578 nM | |||
| External Link | ||||
| Epitinib | Investigative | [9] | ||
| Synonyms |
HMPL-813; EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| OSI-75 | Investigative | [92] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| (E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin | Investigative | [93] | ||
| Synonyms |
CHEMBL213560; SCHEMBL16693054; BDBM50187134
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 710 nM | |||
| External Link | ||||
| HTS-02876 | Investigative | [91] | ||
| Synonyms |
AC1MDGL2; CHEMBL460914; MolPort-002-900-576; ZINC1030761; MCULE-7093116609
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| 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 | ||||
| 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
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.006 nM | |||
| External Link | ||||
| MT-062 | Investigative | [9] | ||
| Synonyms |
EGFR inhibitor (melanoma), Medisyn Technologies
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| MOA | Inhibitor | |||
| External Link | ||||
| Anti-EGFR mab | Investigative | [9] | ||
| External Link | ||||
| 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
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 11000 nM | |||
| External Link | ||||
| IPS-01003 | Investigative | [9] | ||
| Synonyms |
EGFR kinase antagonist (cancer), InnoPharmaScreen
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| MOA | Antagonist | |||
| External Link | ||||
| RM-6427 | Investigative | [9] | ||
| Synonyms |
RM-6428; EGFR tyrosine kinase inhibitors (parasitic infection), Romark
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.12 nM | |||
| External Link | ||||
| 3-Pyridin-4-yl-quinoline-6,7-diol | Investigative | [95] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5000 nM | |||
| External Link | ||||
| AGT-2000 | Investigative | [9] | ||
| Synonyms |
Gene therapy (intravenous, brain cancer), ArmaGen
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| MOA | Modulator | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 95 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| FHT-2107 | Investigative | [9] | ||
| Synonyms |
EGFR-targeting siRNA agent, ForHumanTech
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| External Link | ||||
| 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
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| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 4.6 nM | |||
| External Link | ||||
| 5,6-Bis-p-tolylamino-isoindole-1,3-dione | Investigative | [78] | ||
| Synonyms |
CHEMBL7914; SCHEMBL8834183; BDBM50040920
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 4500 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 90 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 1000 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.003 nM | |||
| External Link | ||||
| ARX-AHD | Investigative | [9] | ||
| Synonyms |
Dolastatin-conjugated HER2 antibody (breast cancer), Ambrx
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| External Link | ||||
| TGF alpha | Investigative | [9] | ||
| Synonyms |
TGF alpha (neurological damage)
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| MOA | Modulator | |||
| External Link | ||||
| AG 9 | Investigative | [85] | ||
| Synonyms |
tyrphostin 1; tyrphostin A1; AG9; AG-9
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| MOA | Inhibitor | |||
| Activity | Ki > 400000 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.78 nM | |||
| External Link | ||||
| 4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline | Investigative | [99] | ||
| Synonyms |
CHEMBL473320; SCHEMBL5616932
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 131 nM | |||
| External Link | ||||
| Theliatinib | Investigative | [9] | ||
| Synonyms |
HMPL-309; Second EGFR tyrosine kinase inhibitor (cancer), Hutchison Medipharma
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-(3-Bromo-phenylamino)-quinazoline-6,7-diol | Investigative | [87] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline | Investigative | [82] | ||
| Synonyms |
CHEMBL250318; BDBM50222435
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| MOA | Inhibitor | |||
| Activity | IC50 = 14 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| EDP-13 | Investigative | [9] | ||
| Synonyms |
Epidermal growth factor receptor antagonist (cancer), BiolineRx/Matrix Pharma
Click to Show/Hide
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| MOA | Antagonist | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.1 nM | |||
| External Link | ||||
| (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
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 8800 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 370 nM | |||
| External Link | ||||
| WZ-3146 | Investigative | [9] | ||
| Synonyms |
WZ-4002; WZ-8040; EGFR-T790M kinase inhibitors (lung cancer); EGFR-T790M kinase inhibitors (lung cancer), Gatekeeper Pharmaceuticals
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 7900 nM | |||
| External Link | ||||
| MG-111 | Investigative | [100] | ||
| Synonyms |
134865-04-6; EGF, Hitachi
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| MOA | Modulator | |||
| External Link | ||||
| 6,7-dimethoxy-4-(2-phenylethynyl)quinazoline | Investigative | [82] | ||
| Synonyms |
CHEMBL250315; SCHEMBL6180450; BDBM50222433
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 5600 nM | |||
| External Link | ||||
| 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
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| External Link | ||||
| 4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline | Investigative | [82] | ||
| Synonyms |
CHEMBL250924; BDBM50222419
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM | |||
| External Link | ||||
| AL-6802 | Investigative | [9] | ||
| Synonyms |
EGFR modulators (cancer), Advenchen/Simcere
Click to Show/Hide
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| MOA | Modulator | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.025 nM | |||
| External Link | ||||
| mabionHER2 | Investigative | [9] | ||
| Synonyms |
Humanized monoclonal antibody (breast cancer), Mabion
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| External Link | ||||
| 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
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 10000 nM | |||
| External Link | ||||
| 4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide | Investigative | [90] | ||
| Synonyms |
CHEMBL200958
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| MDP-01 | Investigative | [9] | ||
| Synonyms |
Peptabody-EGF (anticancer), Med Discovery
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 1000 nM | |||
| External Link | ||||
| RX-1792 | Investigative | [9] | ||
| Synonyms |
EGF antagonist, Rexahn; RX-0183
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| MOA | Antagonist | |||
| External Link | ||||
| (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
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| MOA | Inhibitor | |||
| Activity | IC50 = 355 nM | |||
| External Link | ||||
| NRC-2694 | Investigative | [9] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 1600 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.08 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.42 nM | |||
| External Link | ||||
| 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline | Investigative | [104] | ||
| Synonyms |
CHEMBL98798
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| MOA | Inhibitor | |||
| Activity | IC50 = 70 nM | |||
| External Link | ||||
| 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline | Investigative | [104] | ||
| Synonyms |
CHEMBL101581
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| MOA | Inhibitor | |||
| Activity | IC50 = 2500 nM | |||
| External Link | ||||
| YH013 | Investigative | [105] | ||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.004 ug.mL-1 | |||
| External Link | ||||
| PF 5208766 | Investigative | [107] | ||
| Synonyms |
WAY-178357
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| MOA | Modulator | |||
| External Link | ||||
| 6-chloro-N-(3-chlorophenyl)quinazolin-4-amine | Investigative | [108] | ||
| Synonyms |
4-Anilidoquinazoline deriv. 12a; AC1NS5EY; SCHEMBL4355658; BDBM4397
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| MOA | Inhibitor | |||
| Activity | IC50 = 2700 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
| External Link | ||||
| AG-213 | Investigative | [99] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 850 nM | |||
| External Link | ||||
| SYM-011 | Investigative | [9] | ||
| Synonyms |
Dimercept; Hermodulins; Herstatin; RB-200; RBLX-200; RBLX-242; RBLX-242h; RBLX-642h
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| MOA | Modulator | |||
| External Link | ||||
| 10-hydroxy-18-methoxybetaenone | Investigative | [109] | ||
| Synonyms |
CHEMBL498247; BDBM50269144
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| MOA | Inhibitor | |||
| Activity | IC50 = 10500 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 120 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.37 nM | |||
| External Link | ||||
| HDS-029 | Investigative | [111] | ||
| Synonyms |
HDS 029
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.3 nM | |||
| External Link | ||||
| WHI-P154 | Investigative | [112] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID24915291C38 | Investigative | [113] | ||
| Synonyms |
GTPL8145; PLS-123; BDBM50020476; 1431727-04-6
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| MOA | Inhibitor | |||
| Activity | IC50 = 7 nM | |||
| External Link | ||||
| HKI-9924129 | Investigative | [114] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 390 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 380 nM | |||
| External Link | ||||
| PD-0166326 | Investigative | [114] | ||
| Synonyms |
PD-166326
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| MOA | Inhibitor | |||
| Activity | IC50 = 90 nM | |||
| External Link | ||||
| PP121 | Investigative | [115] | ||
| Synonyms |
PP-121; PP 121
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| MOA | Inhibitor | |||
| Activity | IC50 = 260 nM | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| Ro-4396686 | Investigative | [117] | ||
| Synonyms |
SCHEMBL5809947; CHEMBL606964
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| MOA | Inhibitor | |||
| Activity | IC50 = 545 nM | |||
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| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione | Investigative | [116] | ||
| Synonyms |
CHEMBL372076; SCHEMBL3822337
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| MOA | Inhibitor | |||
| External Link | ||||
| Osimertinib | Approved | [10] | ||
| Synonyms |
Tagrisso
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.421 nM | |||
| External Link | ||||
| PMID27774824-Compound-Figure9Example2down | Patented | [118] | ||
| External Link | ||||
| 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 | ||||
| DZD9008 | Phase 1/2 | [118] | ||
| External Link | ||||
| 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 | ||||
| EGFR antisense DNA | Phase 1/2 | [118] | ||
| Synonyms |
Antisense therapy, UPCI; EGFR antisense DNA, University of Pittsburgh
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| External Link | ||||
| 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 | ||||
| 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 | ||||
| Anti-EGFRvIII CAR transduced PBL | Phase 1/2 | [118] | ||
| External Link | ||||
| EGFRvIII CAR | Phase 1/2 | [118] | ||
| External Link | ||||
| Anti-EGFR V III CAR-T cells | Phase 1/2 | [118] | ||
| External Link | ||||
| EGFRvIII CAR T cells | Phase 1 | [118] | ||
| External Link | ||||
| CAR-T cells targeting EGFRviii | Phase 1 | [118] | ||
| External Link | ||||
| Anti-EGFRvIII CAR T cells | Phase 1 | [118] | ||
| External Link | ||||
| CART-EGFRvIII T cells | Phase 1 | [118] | ||
| External Link | ||||
| EGFRvIII-CARs | Phase 1 | [118] | ||
| External Link | ||||
| CAR-T Cells targeting EGFRvIII | Phase 1 | [118] | ||
| External Link | ||||
| RG6156 | Phase 1 | [118] | ||
| External Link | ||||
| AMG 596 | Phase 1 | [118] | ||
| External Link | ||||
| D2C7 | Phase 1 | [66] | ||
| External Link | ||||
| 2C73: Ovarian cancer | 198 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Atezolizumab | Approved | [34] | ||
| External Link | ||||
| Carboplatin | Approved | [119] | ||
| Synonyms |
Azanide; Carbopaltin; Carboplatine; Carboplatino; Carboplatinum; Cbdca; Ercar; Paraplatin; Carboplatine [French]; Carboplatino [Spanish]; Carboplatinum [Latin]; C 2538; JM 8; Carboplatin (USAN); IUPAC: Azane; JM-8; Paraplatin (TN); Paraplatin, Carboplatin; Paraplatin-AQ; Cis-Diammine(cyclobutanedicarboxylato)platinumII; Platinum(+2) Cation; Carboplatin (JAN/USP/INN); Carboplatin [USAN:INN:BAN:JAN]; Cyclobutane-1,1-dicarboxylate; Cyclobutane-1,1-dicarboxylic acid; Diammine-1,1-cyclobutane dicarboxylate platinum II; Cis-Diamine[1,1-cyclobutanedicarboxylato]platinum(II); Cis-Diammine(1,1-cyclobutanedicarboxylato) platinum; Cis-Diammine(1,1-cyclobutanedicarboxylato)platinum; Cis-Diammine[1,1-cyclobutane-dicarboxylato] platinum; Diammine(1,1-cyclobutanedicarboxylato)platinum (II); Platinum, {diammine[1,1-cyclobut; Cis-(1,1-Cyclobutanedicarboxylato)diammineplatinum(II); Cis-Diamine(1,1-cyclobutanedicarboxylato)platinum(II); Cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II); Platinum(II), (1, 1-cyclobutanedicar; Diammine[cyclobutane-1,1-dicarboxylato(2-)-k2O1,O1]platinum; Diammine(cyclobutane-1,1-dicarboxylato(2-)-O,O')platinum; Platinum, diammine(1,1-cyclobutanedicarboxylato(2-)-O,O')-, (SP-4-2); (SP-4-2)-diammine[cyclobutane-1,1-dicarboxylato(2-)-kappa(2)O,O']platinum; 1,1-Cyclobutanedicarboxylate diammine platinum (II); 1,1-Cyclobutanedicarboxylate diammine platinum(II)
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| Lurbinectedin | Phase 3 | [120] | ||
| Synonyms |
UNII-2CN60TN6ZS; 497871-47-3; 2CN60TN6ZS; Lurbinectedin [INN]; SCHEMBL16152477; DTXSID30198065; DB12674; CS-6323; HY-16293; J3.652.626B
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| External Link | ||||
| Mirvetuximab soravtansine | Approved | [34] | ||
| Synonyms |
ZOHXWSHGANNQGO-QRVRWUFNSA-N; DB12489
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| External Link | ||||
| Lenvatinib | Approved | [121] | ||
| Synonyms |
E 7080; E-7080, E7080; 4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxy-quinoline-6-carboxamide
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| External Link | ||||
| Catumaxomab | Phase 2 | [122] | ||
| External Link | ||||
| Avelumab | Approved | [34] | ||
| External Link | ||||
| Olaparib | Approved | [34] | ||
| Synonyms |
AZD 2281; AZD2281; AZD-2281; Acylpiperazine analogue, 47; KU-0059436; KU-59436; Olaparib, KU-0059436, AZD2281,KU0059436, AZD2281; 4-[(3-{[4-Cyclopropylcarbonyl)piperazin-4-yl]carbonyl}-4-fluorophenyl)methyl]phtalazin-1(2H)-one; 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one
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| External Link | ||||
| Cabozantinib | Approved | [123] | ||
| Synonyms |
Cabometyx; Cometriq
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| External Link | ||||
| Taxol | Approved | [55] | ||
| Synonyms |
C47H51NO14; weekly paclitaxel; Micellar Paclitaxel; Paclitaxel [USAN:INN:BAN]; SCHEMBL15000506; Benzenepropanoic acid, beta-(benzoylamino)-alpha-hydroxy-, 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester, (2aR-(2aalpha,4beta,4abeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-
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| Tisotumab vedotin | Phase 2 | [124] | ||
| External Link | ||||
| KU-0058948 | Approved | [125] | ||
| Synonyms |
CHEMBL380648; 4-[3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one; 4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; Homopiperazine analogue, 14; SCHEMBL864319; BDBM27533; HGEPGGJUGUMFHT-UHFFFAOYSA-N; ZINC3821234; DB08058; NCGC00386677-01; KU-58948; FT-0670691; TL80090044; 4-[3-([1,4]diazepane-1-carbonyl)-4 -fluorobenzyl]-2H-phthalazin-1-one; 4-[3-([1,4]diazepane-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one
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| MVax | Approved | [126] | ||
| Synonyms |
MVax (TN)
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| Intedanib | Phase 2 | [127] | ||
| Synonyms |
Nintedanib; Vargatef; 656247-17-5; BIBF-1120; BIBF 1120; 928326-83-4; BIBF1120; Nintedanib (BIBF 1120); OFEV; UNII-G6HRD2P839; (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate; G6HRD2P839; CHEBI:85164; 1160294-26-7; Methyl (3z)-3-{[(4-{methyl[(4-Methylpiperazin-1-Yl)acetyl]amino}phenyl)amino](Phenyl)methylidene}-2-Oxo-2,3-Dihydro-1h-Indole-6-Carboxylate
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| Fluzone QIV | Approved | [126] | ||
| Synonyms |
Seasonal influenza vaccine (quadrivalent)
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| Pembrolizumab | Approved | [34] | ||
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| Plicamycin | Approved | [128] | ||
| Synonyms |
A-2371; NSC24559; PA-144; MTM A; AC1O3EQZ; CHEMBL413720; SCHEMBL14066059; NSC-24559; AKOS030213136; EC-7071; CCG-208236; NCGC00160390-01; NCI60_004287; AB01273958-01
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| Bevacizumab | Approved | [34] | ||
| Synonyms |
Bevacizumab (ophthalmic slow-release tissue tablet)
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| Trabectedin | Approved | [34] | ||
| Synonyms |
Ecteinascidin; Ecteinascidin-743; Et-743; Yondelis (TN)
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| Topotecan | Approved | [129] | ||
| Synonyms |
Hycamptamine; Hycamptin; Hycamtamine; Topotecane; Topotecanum; Topotecan lactone; SKF 104864; SKF-S 104864; TOPOTECAN, HYCAMTIN; Topotecan (BAN); Topotecan [INN:BAN]; Topotecane [INN-French]; Topotecanum [INN-Latin]; Topotecan Monohydrochloride, (S)-Isomer; (4S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; (S)-10-((Dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione; (S)-10-[(DIMETHYLAMINO)METHYL]-4-ETHYL-4,9-DIHYDROXY-1H-PYRANO[3',4':6,7]INOLIZINO[1,2-B]-QUINOLINE-3,14(4H,12H)-DIONE; (S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]-quinoline-3,14(4H,12H)-dione; (S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 9-Dimethylaminomethyl-10-hydroxycamptothecin
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| Altretamine | Approved | [130] | ||
| Synonyms |
Altretamina; Altretaminum; HEXAMETHYLMELAMINE; HMM; HTM; HXM; Hemel; Hexalen; Hexastat; Hexinawas; Altretamine Bellon Brand; Altretamine Chiesi Brand; Altretamine Wassermann Brand; Bellon Brand of Altretamine; Chiesi Brand of Altretamine; MGI Pharma Brand of Altretamine; Rhone Poulenc Rorer Brand of Altretamine; Wassermann Brand of Altretamine; A 8723; ENT 50852; NC 195; Altretamina [INN-Spanish]; Altretaminum [INN-Latin]; Hexalen (TN); Hexalen, Altretamine; KB-913; Rhone-Poulenc Rorer Brand of Altretamine; Altretamine (USP/INN); Altretamine [USAN:INN:BAN]; No-s-triazine; N,N,N',N',N'',N''-hexamethyl-1,3,5-triazine-2,4,6-triamine; N~2~,N~2~,N~4~,N~4~,N~6~,N~6~-Hexamethyl-1,3,5-triazine-2,4,6-triamine; 2,4, 6-Tris(dimethylamino)-1,3,5-triazine; 2,4,6-Tris(dimethylami; 2,4,6-Tris(dimethylamino)-1,3,5-triazine; 2,4,6-Tris(dimethylamino-s-triazine; 2-N,2-N,4-N,4-N,6-N,6-N-hexamethyl-1,3,5-triazine-2,4,6-triamine
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| Rucaparib | Approved | [131] | ||
| Synonyms |
283173-50-2; Rubraca; AG-14447; UNII-8237F3U7EH; 8237F3U7EH; AK317822; 8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one; 8-FLUORO-2-(4-((METHYLAMINO)METHYL)PHENYL)-4,5-DIHYDRO-1H-AZEPINO[5,4,3-CD]INDOL-6(3H)-ONE; 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-; 8-fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one
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| Melphalan flufenamide | Approved | [132] | ||
| Synonyms |
J-1; Dipeptide-conjugated melphalan prodrug (iv formulation, ovary tumor), Oncopeptides
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| Nivolumab | Approved | [34] | ||
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| Ofranergene obadenovec | Phase 3 | [133] | ||
| Synonyms |
VB-111
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| Batiraxcept | Phase 3 | [134] | ||
| Synonyms |
AVB-S6-500
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| Trebananib | Phase 3 | [135] | ||
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| Nemvaleukin alfa | Phase 3 | [136] | ||
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| RRx-001 | Phase 2 | [34] | ||
| Synonyms |
925206-65-1; 2-BROMO-1-(3,3-DINITROAZETIDIN-1-YL)ETHAN-1-ONE; UNII-7RPW6SU9SC; 2-Bromo-1-(3,3-dinitroazetidin-1-yl)ethanone; 7RPW6SU9SC; RRx001; Ethanone, 2-bromo-1-(3,3-dinitro-1-azetidinyl)-; SCHEMBL2249018; CHEMBL3526802; MolPort-044-559-098; EX-A2006; BCP19228; 1-bromoacetyl-3,3-dinitroazetidine; ZINC34805177; s8405; DB12060; CS-5286; HY-16438; AS-53015
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| Picoplatin | Phase 3 | [137] | ||
| Synonyms |
AMD 473; JM-473; ZD0473; (SP-4-3)-Amminedichloro(2-methylpyridine)platinium; Platinum, amminedichloro(2-methylpyridine)-, (SP-4-3)-; Picoplatin [INN:BAN]; UNII-B5TAN0L720; ZD 0473; AC1L42P3; B5TAN0L720; DB04874; Amminedichloro(2-methylpyridine)platinium; AN-30599; LS-184068; J-011604; azane; 2-methylpyridine; dichloride
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| VB-111 | Phase 3 | [34] | ||
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| Upifitamab rilsodotin | Phase 3 | [138] | ||
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| ABT-888 | Phase 3 | [34] | ||
| Synonyms |
Veliparib; 912444-00-9; ABT 888; ABT-888 (Veliparib); Veliparib (ABT-888); ABT888; UNII-01O4K0631N; 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide; CHEBI:62880; 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide; (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide; 01O4K0631N; 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-; (2r)-2-(7-Carbamoyl-1h-Benzimidazol-2-Yl)-2-Methylpyrrolidinium; Veliparib dihydrochloride
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| Rubraca rucaparib | Phase 3 | [34] | ||
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| Masitinib | Phase 3 | [34] | ||
| Synonyms |
790299-79-5; AB1010; Masatinib; Masitinib (AB1010); Masivet; AB-1010; AB 1010; UNII-M59NC4E26P; Masitinib [INN]; M59NC4E26P; 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide; CHEMBL1908391; CHEBI:63450; Masitinib (INN); N-(4-Methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide; Q-201339; C28H30N6OS; N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
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| Galinpepimut-S | Phase 3 | [139] | ||
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| SNDX-275 | Phase 3 | [34] | ||
| Synonyms |
Entinostat; Histone Deacetylase Inhibitor I; IN1470; MS 275; SNDX 275; MS 27-275; Ms-275; Entinostat (USAN/INN); MS-27-275; Pyridin-3-ylmethyl 4-(2-aminophenylcarbamoyl)benzylcarbamate; Pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate; Pyridin-3-ylmethyl {4-[(2-aminophenyl)carbamoyl]benzyl}carbamate; Pyridin-3-ylmethyl{4-[(2-aminophenyl)carbamoyl]benzyl}carbamate; Carbamic acid, [[4-[[(2-aminophenyl)amino]carbonyl]phenyl] methyl]-, 3-pyridinylmethyl ester; Carbamic acid, [[4-[[(2-aminophenyl)carbaonyl]phenyl]methyl]-, 3-pyridinylmethyl ester; Entinostat, SNDX-275, MS-27-275, MS-275; N-(2-Aminophenyl)-4-[N-(pyridin-3-yl-methoxycarbonyl)aminomethyl]benzamide; N-(2-aminophenyl)-4-(N-(pyridin-3-ylmethoxycarbonyl)aminomethyl)benzamide; Carbamic acid, ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3-pyridinylmethyl ester; 3-Pyridinylmethyl ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)carbamate
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| acelarin | Phase 2 | [34] | ||
| Synonyms |
NUC-1031
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| Glufosfamide | Phase 3 | [121] | ||
| Synonyms |
Glucosylifostamide mustard; D 19575; D-19575; Glc-IPM; Glucosyl-ifosfamide mustard; Beta-D-Glucopyranose 1-(N,N'-bis(2-chloroethyl)phosphorodiamidate; Beta-D-Glucopyranose, 1-(N,N'-bis(2-chloroethyl)phosphorodiamidate); (2S,3R,4S,5S,6R)-2-bis(2-chloroethylamino)phosphoryloxy-6-(hydroxymethyl)oxane-3,4,5-triol
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| PM1183 | Phase 3 | [55] | ||
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| Amonafide | Phase 3 | [140] | ||
| Synonyms |
Quinamed (TN)
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| Etirinotecan pegol | Phase 2 | [55] | ||
| Synonyms |
NKTR-102
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| INCB24360 | Phase 2 | [34] | ||
| Synonyms |
Epacadostat
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| AL3818 | Phase 1/2 | [34] | ||
| Synonyms |
Anlotinib; 1058156-90-3; UNII-GKF8S4C432; GKF8S4C432; AL-3818; SCHEMBL2063386; GTPL9601; KSMZEXLVHXZPEF-UHFFFAOYSA-N; MolPort-044-567-604; ZINC117924202; AKOS030526233; DB11885; CS-5396; AL 3818; HY-19716; 1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinolin-7-yl]oxymethyl]cyclopropan-1-amine; 1-((4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropan-amine; Cyclopropanamine, 1-(((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxy-7-quinolinyl)oxy)methyl)-
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| Sapacitabine | Phase 3 | [34] | ||
| Synonyms |
CYC682
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| Pelareorep | Phase 2 | [55] | ||
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| Opdivo + Yervoynivolumab + ipilimumab | Phase 1/2 | [34] | ||
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| Epothilon | Phase 3 | [121] | ||
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| Oregovomab | Phase 3 | [141] | ||
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| Farletuzumab | Phase 3 | [142] | ||
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| DCVax-Ovarian | Phase 3 | [34] | ||
| Synonyms |
DCVax-L; Dendritic cell-based immunotherapy (ovarian cancer), Northwest Biotherapeutics
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| MK-8109 | Phase 3 | [143] | ||
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| Karenitecin | Phase 3 | [144] | ||
| Synonyms |
Karenitecin (TN)
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| TRC105 | Phase 2 | [145] | ||
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| SNS-595 | Phase 3 | [121] | ||
| Synonyms |
Voreloxin; Vosaroxin; AG 7352; SNS 595; SPC 595; AG 7352 (TN); AG-7352; SNS 595 (TN); SPC 595 (TN); SPC-595; Voreloxin (TN); Voreloxin (USAN); SNS-595 (TN); 1,4-Dihydro-7-(3-methoxy-4-methylamino-1-pyrrolidinyl)-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid
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| MK-4827 | Phase 3 | [146] | ||
| Synonyms |
1038915-60-4; (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide; UNII-HMC2H89N35; HMC2H89N35; CHEMBL1094636; 2-{4-[(3s)-piperidin-3-yl]phenyl}-2h-indazole-7-carboxamide; MK4827; MK 4827; Niraparib [USAN:INN]; 2-{4-[(3S)-piperidin-3-yl]phenyl}indazole-7-carboxamide; 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide; MK 4827 (Base); Niraparib (USAN); Zejula (TN); MK-4827(Niraparib); SCHEMBL1421875; GTPL8275; CTK8B9123; EX-A290; DTXSID50146129; MolPort-023-219-142; ZINC43206370; BDBM50316226
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| EC20 | Phase 3 | [147] | ||
| Synonyms |
Technetium Tc-99m etarfolatide
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| Abagovomab | Phase 2/3 | [148] | ||
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| Mecbotamab vedotin | Phase 2 | [149] | ||
| Synonyms |
HTBA3011; HTBA3012
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| GEN-1 | Phase 2 | [34] | ||
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| Stenoparib | Phase 2 | [150] | ||
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| DKN-01 | Phase 2 | [34] | ||
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| EP-100 | Phase 2 | [34] | ||
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| EP0057 | Phase 2 | [151] | ||
| Synonyms |
CRLX101
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| BNT141 | Phase 2 | [152] | ||
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| TJ004309 | Phase 2 | [153] | ||
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| Maveropepimut-S | Phase 2 | [154] | ||
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| PF-07901801 | Phase 2 | [155] | ||
| Synonyms |
maplirpacept
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| SPL-108 | Phase 2 | [34] | ||
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| VS-6063 | Phase 2 | [34] | ||
| Synonyms |
Defactinib hydrochloride; 1073160-26-5; Defactinib (hydrochloride); UNII-L2S469LM49; Defactinib hydrochloride [USAN]; L2S469LM49; Defactinib hydrochloride (USAN); Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-, hydrochloride; Defactinib HCl; Benzamide, N-methyl-4-((4-(((3-(methyl(methylsulfonyl)amino)-2-pyrazinyl)methyl)amino)-5-(trifluoromethyl)-2-pyrimidinyl)amino)-, hydrochloride (1:1); Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsu
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| PTX-200 | Phase 2 | [34] | ||
| Synonyms |
Plant-derived antiparkinsonian, Phytrix
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| Mirvetuximab soratansine | Phase 2 | [55] | ||
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| Ovapuldencel-T | Phase 2 | [34] | ||
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| MUC-1 cancer vaccine | Phase 2 | [156] | ||
| Synonyms |
CVac (TN)
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| FANG vaccine | Phase 3 | [157] | ||
| Synonyms |
FANG (TN)
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| Ispinesib | Phase 2 | [158] | ||
| Synonyms |
SB-715992; Ispinesib (SB-715992 /CK0238273); SB-715992, CK0238273,Ispinesib; N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxoquinazolin-2-yl)-2-methylpropyl]-4-methylbenzamide
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| EGEN-001 | Phase 2 | [159] | ||
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| CRLX101 | Phase 2 | [34] | ||
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| Folate binding protein vaccine | Phase 2 | [160] | ||
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| RO-5126766 | Phase 2 | [161] | ||
| Synonyms |
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TPIV200 | Phase 2 | [139] | ||
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| BBI503 | Phase 2 | [162] | ||
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| Varlilumab | Phase 2 | [34] | ||
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| Kevetrin | Phase 2 | [34] | ||
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| OTL38 | Phase 2 | [55] | ||
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| NanoPac | Phase 2 | [34] | ||
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| Sagopilone | Phase 2 | [163] | ||
| Synonyms |
ZK-EPO; 305841-29-6; UNII-KY72JU32FO; KY72JU32FO; DE-03757; ZK-219477; EPO-477; SH-Y03757A; ZK epothilone; Sagopilone [USAN:INN]; Sagopilone (USAN/INN); SCHEMBL423579; CHEMBL2304041; SH Y03757A; Bay 86-5302; ZINC3964449; DB12391; SH-Y-03757; BAY-86-5302; AN-28960; DE 03757; ZK 219477; D09721; 841S296; (1S,3S,7S,10R,11S,12S,16R)-10-allyl-7,11-dihydroxy-8,8,12,16-tetramethyl-3-(2-methyl-1,3-benzothiazol-5-yl)-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione
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| PMID27841036-Compound-37 | Phase 2 | [164] | ||
| Synonyms |
2X-121
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| BGB-290 | Phase 2 | [165] | ||
| Synonyms |
Pamiparib
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| TLPLDC | Phase 2 | [139] | ||
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| Anetumab ravtansine | Phase 2 | [34] | ||
| Synonyms |
Mesothelin-ADC
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| OGX-427 | Phase 2 | [166] | ||
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| ZW25 | Phase 1 | [34] | ||
| Synonyms |
Zanidatamab
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| CDX-1401 | Phase 2 | [34] | ||
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| CA4P | Phase 2 | [55] | ||
| Synonyms |
Fosbretabulin disodium; 168555-66-6; Combretastatin A4 disodium phosphate; CA4DP; Fosbretabulin (disodium); Zybrestat; UNII-702RHR475O; Combretastatin A4 Phosphate Disodium Salt; Fosbretabulin disodium [USAN]; 702RHR475O; Combretastatin A-4 phosphate; Fosbretabulin disodium (USAN); CHEMBL289351; Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium; AC1OCF9S; Fosbretabulin Disodium Salt; CA-4P; CA 4P; SCHEMBL321426; C18H19O8P.2Na; MolPort-006-823-175; ACT03122; 3559AH; s7204; AKOS027327946; BCP9000542; CS-1484; NSC-752293; Fosbr
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| Dendritic cell vaccine | Phase 2 | [167] | ||
| Synonyms |
Dendritic cell vaccine, University of Bonn; Human telomerase reverse transcriptase (hTERT)-pulsed dendritic cells (cancer), University of Bonn
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| LY2606368 | Phase 2 | [34] | ||
| Synonyms |
prexasertib; 1234015-52-1; UNII-820NH671E6; LY-2606368; 820NH671E6; Prexasertib [USAN]; 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile; 5-({5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl}amino)pyrazine-2-carbonitrile; 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile; SCHEMBL1975451; GTPL9549; SCHEMBL19457660; SCHEMBL18989301; CHEMBL3544911; EX-A758; DOTGPNHGTYJDEP-UHFFFAOYSA-N; AOB87325; ZINC95837013
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| GSK3377794 | Phase 2 | [34] | ||
| External Link | ||||
| Melphalan | Approved | [168] | ||
| External Link | ||||
| MEDI-546 | Phase 2 | [169] | ||
| External Link | ||||
| RG-7599 | Phase 2 | [170] | ||
| Synonyms |
DNIB-0600A; Antibody-drug conjugate (NSCLC/ovarian cancer), Genentech
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| EP-201 | Phase 2 | [139] | ||
| Synonyms |
Chissonox 201; Unox epoxide 201; Unox 201; Epoxide-201; EP 201; 141-37-7; CCRIS 279; NSC 61273; BRN 0246264; MLS002638023; CHEBI:82463; 3,4-epoxy-6-methylcyclohexylmethyl-3,4-epoxy-6-methylcyclohexanecarboxylate; Epoxide 201; 6-Methyl-3,4-epoxycyclohexylmethyl 6-methyl-3,4-epoxycyclohexane carboxylate; 3,4-Epoxy-6-methylcyclohexylmethyl-3,4-epoxy-6-methylcyclohexane carboxylate; 3,4-Epoxy-6-methylcyclohexylmethyl-3',4'-epoxy-6'-methylcyclohexane carboxylate; 3,4-Epoxy-6-methylcyclohexylmethyl 3,4-epoxy-6-methylcyclohexanec
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| APR-246 | Phase 2 | [34] | ||
| Synonyms |
Eprenetapopt
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| Tigatuzumab | Phase 2 | [171] | ||
| External Link | ||||
| CRS-207 | Phase 2 | [139] | ||
| External Link | ||||
| MK-1775 | Phase 2 | [172] | ||
| Synonyms |
955365-80-7; Adavosertib; MK1775; MK 1775; UNII-K2T6HJX3I3; AZD 1775; AZD-1775; AZD1775; 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-(4-(4-methylpiperazin-1-yl)phenylamino)-1H-pyrazolo[3,4-d]pyrimidin-3(2H)-one; K2T6HJX3I3; 1-[6-(2-hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one; 2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1H-pyrazolo[3,4-d]pyrimidin-3(2H)-one; AK-99219
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| External Link | ||||
| CP-547632 | Phase 2 | [173] | ||
| Synonyms |
BFF; CP 547632; CP-547,632; 3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide
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| Motolimid | Phase 2 | [55] | ||
| External Link | ||||
| TC-210 | Phase 1/2 | [174] | ||
| External Link | ||||
| REGN5668 | Phase 1/2 | [175] | ||
| External Link | ||||
| TC-510 | Phase 1/2 | [176] | ||
| External Link | ||||
| XMT-1592 | Phase 1/2 | [177] | ||
| External Link | ||||
| GL-ONC1 | Phase 2 | [178] | ||
| Synonyms |
olvimulogene nanivacirepvec
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| LY2940680 | Phase 1/2 | [34] | ||
| Synonyms |
1258861-20-9; Taladegib; LY-2940680; UNII-QY8BWX1LJ5; 4-Fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide; QY8BWX1LJ5; Taladegib (LY2940680); LY 2940680; 4-fluoro-n-methyl-n-(1-(4-(1-methyl-1h-pyrazol-5-yl)-1-phthalazinyl)-4-piperidinyl)-2-(trifluoromethyl)benzamide; 4-Fluoro-N-Methyl-N-{1-[4-(1-Methyl-1h-Pyrazol-5-Yl)phthalazin-1-Yl]piperidin-4-Yl}-2-(Trifluoromethyl)benzamide; Taladegib [USAN:INN]
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| External Link | ||||
| Her-2/neu vaccine | Phase 1/2 | [179] | ||
| External Link | ||||
| NY-ESO-TCR | Phase 1/2 | [31] | ||
| External Link | ||||
| GALE-302 | Phase 1/2 | [34] | ||
| External Link | ||||
| DPX-survivac cancer vaccine | Phase 1/2 | [180] | ||
| External Link | ||||
| REGN4018 | Phase 1/2 | [181] | ||
| External Link | ||||
| GALE-301 + GALE-302 | Phase 1/2 | [139] | ||
| External Link | ||||
| Anti-C-met CAR-T cells | Phase 1/2 | [182] | ||
| External Link | ||||
| CDX-014 | Phase 1/2 | [34] | ||
| External Link | ||||
| O-Vax | Phase 1/2 | [183] | ||
| Synonyms |
AC vaccine (ovarian cancer), AVAX
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| External Link | ||||
| Anti-HER2 CAR-T | Phase 1/2 | [184] | ||
| External Link | ||||
| NT-501 CNTF | Phase 1/2 | [185] | ||
| External Link | ||||
| Phenoxodiol | Phase 1/2 | [186] | ||
| Synonyms |
Dehydroequol; Idronoxil; Haginin E; NV 06; NV-06; Idronoxil (USAN/INN); 2H-1-benzopyran-7-0,1,3-(4-hydroxyphenyl); 3-(4-Hydroxyphenyl)-2H-1-benzopyran-7-ol; 3-(4-Hydroxyphenyl)-2H-chromen-7-ol; 7-hydroxy-3-hydroxyphenyl-1H-benzopyran
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| External Link | ||||
| GALE-301 | Phase 2 | [139] | ||
| External Link | ||||
| IL-2/gene-modified lymphocytes | Phase 1/2 | [187] | ||
| External Link | ||||
| Ovarian dendritic cell-based vaccine | Phase 1/2 | [188] | ||
| External Link | ||||
| Anti-mesothelin CAR transduced PBL | Phase 1/2 | [189] | ||
| External Link | ||||
| ONCOS-102 | Phase 1/2 | [34] | ||
| Synonyms |
CGTG-102
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| BNT115 | Phase 1 | [190] | ||
| External Link | ||||
| MEDI3617 | Phase 1 | [191] | ||
| External Link | ||||
| SL-172154 | Phase 1 | [192] | ||
| External Link | ||||
| INKmune | Phase 1 | [193] | ||
| External Link | ||||
| DeTIL-0255 | Phase 1 | [194] | ||
| External Link | ||||
| DS-6000 | Phase 1 | [195] | ||
| External Link | ||||
| MCY-M11 | Phase 1 | [196] | ||
| External Link | ||||
| IMT1012 | Phase 1 | [197] | ||
| External Link | ||||
| mRNA-2416 | Phase 1 | [198] | ||
| Synonyms |
mRNA-OX40L
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| TG4050 | Phase 1 | [199] | ||
| External Link | ||||
| GRN-300 | Phase 1 | [200] | ||
| External Link | ||||
| ITIL-306 | Phase 1 | [201] | ||
| External Link | ||||
| STRO-002 | Phase 1 | [202] | ||
| External Link | ||||
| Ipafricept | Phase 1 | [203] | ||
| External Link | ||||
| IMT-1012 immunotherapeutic vaccine | Phase 1 | [204] | ||
| External Link | ||||
| STM 434 | Phase 1 | [55] | ||
| External Link | ||||
| Mibefradil | Withdrawn from market | [205] | ||
| Synonyms |
Mibefradil (Cytostatic Checkpoint Therapy, ovarian cancer); Mibefradil (Cytostatic Checkpoint Therapy, ovarian cancer), Tau Therapeutics; Calcium T-channel inhibitor (Cytostatic Checkpoint Therapy, ovarian cancer), Tau Therapeutics
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| RG7882 | Phase 1 | [206] | ||
| External Link | ||||
| MOv19-BBz CAR T cells | Phase 1 | [207] | ||
| External Link | ||||
| SC-003 | Phase 1 | [34] | ||
| External Link | ||||
| KHK-2866 | Phase 1 | [208] | ||
| External Link | ||||
| PUMVC3-hIGFBP-2 | Phase 1 | [209] | ||
| Synonyms |
IGFBP-2 DNA plasmid vaccine (intradermal, ovarian cancer); IGFBP-2 DNA plasmid vaccine (intradermal, ovarian cancer), Fred Hutchinson
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| Anti-hCD70 CAR transduced PBL | Phase 1 | [210] | ||
| External Link | ||||
| Prolanta | Phase 1 | [34] | ||
| External Link | ||||
| JCAR020 | Phase 1 | [31] | ||
| External Link | ||||
| COTI-2 | Phase 1 | [34] | ||
| Synonyms |
UNII-2BTA1O65BR; 2BTA1O65BR; 1039455-84-9; ZINC114475331; CS-8156; HY-19896; 1-Piperazinecarbothioic acid, 4-(2-pyridinyl)-, 2-(6,7-dihydro-8(5H)-quinolinylidene)hydrazide
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| Anti-meso-CAR vector transduced T cells | Phase 1 | [211] | ||
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| Cantrixil | Phase 1 | [34] | ||
| Synonyms |
UNII-5DVS457HEG; 5DVS457HEG; SCHEMBL19410294; TRX-E-002-1; cis-4-(p-hydroxyphenyl)-7,4'-dihydroxy-3',5'-dimethoxy-8-methylisoflavan; (+)-cis-4-(Para-hydroxyphenyl)-7,4-dihydroxy-3,5-dimethoxy-8-methylisoflavan; 1803036-93-2
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| Iboctadekin + Doxil | Phase 1 | [212] | ||
| External Link | ||||
| FATE-NK100 | Phase 1 | [34] | ||
| External Link | ||||
| Iboctadekin | Phase 1 | [213] | ||
| External Link | ||||
| Anti-CD133-CAR vector-transduced T cells | Phase 1 | [214] | ||
| External Link | ||||
| Hu-CART meso cells | Phase 1 | [215] | ||
| External Link | ||||
| PTC596 | Phase 1 | [34] | ||
| External Link | ||||
| SOR-C13 | Phase 1 | [216] | ||
| External Link | ||||
| AE-O | Phase 1 | [217] | ||
| Synonyms |
Ovarian vaccine, Generex
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| E 7974 | Phase 1 | [121] | ||
| Synonyms |
26510-52-1; ethyl 3-oxo-3-(pyridin-2-yl)propanoate; Ethyl picolinoylacetate; ethyl 3-oxo-3-(2-pyridyl)propionate; ethyl 3-oxo-3-pyridin-2-ylpropanoate; ethyl 3-oxo-3-(2-pyridinyl)propanoate; 3-Oxo-3-(2-pyridyl)propionic acid ethyl ester; Ethyl picolinoylacetate, 95%; ethyl 3-oxo-3-(2-pyridyl)propanoate; PubChem11088; ethyl-2-pyridoyl acetate; AC1MC5MX; AC1Q34ND; SCHEMBL601821; CHEMBL2035673; CTK4F8033; DTXSID30371376; MolPort-001-769-152; FQHXWZMJALFSJJ-UHFFFAOYSA-N; ZINC153764; Ethyl picolinoylacetate, AldrichCPR; STL131872
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| DMUC-5754A | Phase 1 | [218] | ||
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| Alvespimycin hydrochloride | Phase 1 | [219] | ||
| Synonyms |
Alvespimycin hydrochloride (USAN); 17-DMAG; 17-Desmethoxy-17-N,N-dimethylaminoethylamino-geldanamycin, HCl; 17-N,N-Dimethylaminoethylamino-17-demethoxy-geldanamycin, HCl; 17DMAG; 17DMAG, Alvespimycin, KOS-1022, NSC 707545, 17-DMAG
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| Navicixizumab | Phase 1 | [31] | ||
| External Link | ||||
| AR-A014418 | Patented | [220] | ||
| Synonyms |
487021-52-3; GSK-3beta Inhibitor VIII; 1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea; 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea; A Inhibitor VIII; N-(4-METHOXYBENZYL)-N'-(5-NITRO-1,3-THIAZOL-2-YL)UREA; UNII-87KSH90Q6D; AR-AO 14418; SN 4521; AR-A 014418; CHEMBL259850; 87KSH90Q6D; N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea; AK175829; C12H12N4O4S; N-(4-Methoxybenzyl)-N& -(5-nitro-1,3-thiazol-2-yl)urea; AR 014418; GSK 3be
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| R1549 | Discontinued in Phase 3 | [221] | ||
| External Link | ||||
| Tanomastat | Discontinued in Phase 3 | [222] | ||
| Synonyms |
Tanomastat (USAN/INN); (2S)-4-[4-(4-chlorophenyl)phenyl]-4-oxo-2-(phenylsulfanylmethyl)butanoic acid
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| IDM-1 | Discontinued in Phase 3 | [223] | ||
| Synonyms |
Osidem
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| Lurtotecan | Discontinued in Phase 2 | [224] | ||
| Synonyms |
OSI-211; Lurtotecan [INN]; 149882-10-0; UNII-4J1L80T08I; OSI 211; NX 211; GG 211; Gi 147211; 4J1L80T08I; C28H30N4O6; CHEMBL341028; 11H-1,4-Dioxino(2,3-g)pyrano(3',4':6,7)indolizino(1,2-b)quinoline-9,12(8H,14H)-dione, 8-ethyl-2,3-dihydro-8-hydroxy-15-((4-methyl-1-piperazinyl)methyl)-, (8S)-; GI-147211C; lurtotecan liposome; AC1L1U8C; SCHEMBL19208; CHEMBL305666; DTXSID30164422; GG-211; ZINC22010625; NX-211; GW-211; BDBM50036130; DB12222; LS-173358; Lurtotecan dihydrochloride; GI 147211C; GG-147211C; GI-147211; GI-147211A; GL-147211C; Liposomal lurtotecan
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| AGS-8M4 | Discontinued in Phase 2 | [225] | ||
| Synonyms |
AGS-8 MAb, Agensys, AGS8M4, ASP-6183
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| Biricodar | Discontinued in Phase 2 | [226] | ||
| Synonyms |
Incel; Biricodar [INN]; Vx 710; Incel (TN); 1,7-dipyridin-3-ylheptan-4-yl (2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
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| Onyvax-O | Discontinued in Phase 1 | [227] | ||
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| RG7458 | Discontinued in Phase 1 | [228] | ||
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| RG7600 | Discontinued in Phase 1 | [229] | ||
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| S-8184 | Preclinical | [230] | ||
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| 111In-OC-125 F(ab1/2)-DTPA | Terminated | [231] | ||
| Synonyms |
Indimacis 125; Indium-111-OC-125 F(ab1/2)-DTPA
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| HumaRAD-OV | Investigative | [232] | ||
| Synonyms |
HumaRAD88BV59; KSB-310
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| FOLIGO 002 | Investigative | [232] | ||
| External Link | ||||
| HS-210 | Investigative | [232] | ||
| Synonyms |
HS-01; Endoplasmin modulator (ovary tumor, HeatShock/fusion protein/antigen), Heat Biologics; Gp-96-Ig + unspecified tumorantigen secreting live cell vaccine (ovary tumor, HeatShock), Heat Biologics
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| CGEN-991 | Investigative | [232] | ||
| Synonyms |
Anti-CGEN-991 antibody (ovarian cancer); CGEN-991 (ovarian cancer), Compugen; Anti-CGEN-991 antibody (ovarian cancer), Compugen
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| FabOvar | Investigative | [232] | ||
| Synonyms |
Alpha-folate receptor-targeting I131-labeled mAb fragment (ip, ovarian carcinoma), Advanced Accelerator Applications; Alpha-folate receptor-targeting I131-labeled mAb fragment (ip, ovarian carcinoma), Dompe
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| ALVAC-CEA/hB7.1 | Investigative | [232] | ||
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| MX-35 | Investigative | [232] | ||
| Synonyms |
Monoclonal antibody (ovarian cancer), Recepta
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| 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Investigative | [233] | ||
| Synonyms |
CHEMBL1082330; BDBM50320180
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| ET-006 | Investigative | [232] | ||
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| AB-3D3 | Investigative | [232] | ||
| Synonyms |
AB-0447a; KAAG1-targeting mAb (ovarian cancer), Alethia; KAAG1-targeting monoclonal antibody (ovarian cancer), Alethia; Kidney associated antigen 1-targeting mAb (ovarian cancer), Alethia; Kidney associated antigen 1-targeting monoclonal antibody (ovarian cancer), Alethia; AB-0447-targeting monoclonal antibodies (cancer), Alethia
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| RAP-701 | Investigative | [232] | ||
| Synonyms |
Small stabilized receptor active peptide (ovarian cancer), RAPID Pharmaceuticals
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| Anti-folate receptor 1 humanized mab | Investigative | [232] | ||
| Synonyms |
Anti-folate receptor 1 humanized mAb (cancer)
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| Disorazol Z-LHRH conjugates | Investigative | [232] | ||
| Synonyms |
Disorazol Z-LHRH conjugates (ovarian cancer)
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| Anti-CGEN-153 mab | Investigative | [232] | ||
| Synonyms |
CGEN-153; Anti-CGEN-153 mAb (ovarian cancer); CGEN-153 (Ovarian cancer), Compugen; Anti-CGEN-153 mAb (ovarian cancer), Compugen
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| OGX-427 + Paclitaxel | Investigative | [234] | ||
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References
: m6A sites