m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT02171
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[1], [2] | |||
DNA methylation
DNMT3A
METTL3
Direct
Inhibition
m6A modification
EZH2
EZH2
METTL3
Methylation
: m6A sites
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| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | Methyltransferase-like 3 (METTL3) | WRITER | |||
| m6A Target | Histone-lysine N-methyltransferase EZH2 (EZH2) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | DNA methylation (DNAMeth) | ||||
| Epigenetic Regulator | Cysteine methyltransferase DNMT3A (DNMT3A) | WRITER | View Details | ||
| Regulated Target | Methyltransferase-like protein 3 (METTL3) | View Details | |||
| Crosstalk Relationship | DNA methylation → m6A | Inhibition | |||
| Crosstalk Mechanism | DNA methylation directly impacts m6A modification through modulating the expression level of m6A regulator | ||||
| Crosstalk Summary | Methyltransferase-like 3 (METTL3) increased the pri-Let-7b, decreased both the pre-Let-7b and mature Let-7b, attenuating the Let-7b controlling of stem cell renewal. The addition of Metformin increased the bindings of DNA methyltransferase-3a/b (DNMT3A/DNMT3B) to the METTL3 promoter. With the help of the readers of NKAP and HNRNPA2B1, the cluster mediated m6A formation on pri-Let-7b processing increased the mature Let-7b, the key player in suppressing Notch signaling and re-captivating Osimertinib treatment. Simvastatin induces METTL3 down-regulation in lung cancer tissues, which further influences EMT via m6A modification on Histone-lysine N-methyltransferase EZH2 (EZH2) mRNA and thus inhibits the malignant progression of lung cancer. | ||||
| Responsed Disease | Lung cancer | ICD-11: 2C25 | |||
| Responsed Drug | Osimertinib | ||||
| Pathway Response | Notch signaling pathway | hsa04330 | |||
| Cell Process | Epithelial-mesenchymal transition | ||||
In-vitro Model |
NCI-H1975 | Lung adenocarcinoma | Homo sapiens | CVCL_1511 | |
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | ||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Cysteine methyltransferase DNMT3A (DNMT3A) | 8 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| PMID27376512-Compound-Figure3CN | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CG | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 2400 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CM | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure2aExample1 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3000 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-424 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1940 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-427 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 295 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-422 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1430 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-423 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 363 nM | |||
| External Link | ||||
| Histone-lysine N-methyltransferase EZH2 (EZH2) | 74 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Tazemetostat | Approved | [4] | ||
| Synonyms |
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
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| MOA | Inhibitor | |||
| Activity | Ki = 2.5 nM | |||
| External Link | ||||
| DS-3201b | Phase 2 | [5] | ||
| Synonyms |
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
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| MOA | Inhibitor | |||
| External Link | ||||
| CPI-1205 | Phase 1/2 | [6] | ||
| Synonyms |
HPODOLXTMDHLLC-QGZVFWFLSA-N; 1621862-70-1; UNII-455J2479FY; CPI1205; CPI 1205; 455J2479FY; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide; GTPL9115; SCHEMBL17329268; MolPort-044-560-382; KS-000006BA; EX-A1068; s8353; AKOS030628484; ZINC220982768; CS-7648; compound 13 [PMID: 27739677]; HY-100021; J3.556.402K; N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-
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| MOA | Inhibitor | |||
| External Link | ||||
| SHR2554 | Phase 1/2 | [7] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CPI-0209 | Phase 1/2 | [8] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| GSK2816126 | Phase 1 | [9] | ||
| Synonyms |
GSK 126; GSK-126
Click to Show/Hide
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| MOA | Modulator | |||
| Activity | Ki = 0.5 nM | |||
| External Link | ||||
| PF-06821497 | Phase 1 | [10] | ||
| Synonyms |
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
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| MOA | Inhibitor | |||
| External Link | ||||
| DS-3201 | Phase 1 | [6] | ||
| Synonyms |
QTGYNKYZRZATJB-UHFFFAOYSA-N; 701899-63-0; 2-(2-(2-Methyl-1H-imidazol-5-yl)ethyl)isoindoline-1,3-dione; 2-(2-(2-Methyl-1H-imidazol-5-yl)-ethyl)isoindoline-1,3-dione; SCHEMBL7743461; MolPort-035-945-474; MolPort-035-690-353; ZINC98086069; AKOS024459002; AKOS024262663; MCULE-2708350770; FCH4077443; AK158834; AX8292467; ST2403812; 2-[2-(2-methyl-1H-imidazol-5-yl)ethyl]-2,3-dihydro-1H-isoindole-1,3-dione
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| MOA | Inhibitor | |||
| External Link | ||||
| HH2853 | Phase 1 | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-33 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bI | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-35 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-54 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-24 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-27 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-25 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-50 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-47 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2 nM; Ki < 1 nM | |||
| External Link | ||||
| PMID28394193-Compound-21 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-41 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-53 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 80 nM | |||
| External Link | ||||
| PMID28394193-Compound-Figure5aVIII | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-38 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-51 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-31 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 20 nM | |||
| External Link | ||||
| PMID28394193-Compound-42 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-15 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-52 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-32 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| PMID28394193-Compound-23 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-29 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-30 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 16 nM | |||
| External Link | ||||
| PMID28394193-Compound-39 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-49 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-43 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-40 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bIII | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-36 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 316 nM | |||
| External Link | ||||
| PMID28394193-Compound-28 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 32 nM | |||
| External Link | ||||
| PMID28394193-Compound-22 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-18 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-16 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-44 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-20 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-19 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-37 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bII | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-26 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-17 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-34 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID26882240-Compound-1 | Patented | [13] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| EPZ005687 | Investigative | [14] | ||
| Synonyms |
EPZ-005687; EPZ 005687
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| MOA | Inhibitor | |||
| External Link | ||||
| EI1 | Investigative | [15] | ||
| Synonyms |
KB-145943
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| MOA | Inhibitor | |||
| External Link | ||||
| UNC1999 | Investigative | [16] | ||
| Synonyms |
UNC 1999; UNC-1999
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| MOA | Inhibitor | |||
| External Link | ||||
| MS1943 | Investigative | [7] | ||
| Synonyms |
2225938-17-8; SCHEMBL21271666; EX-A3962; s8918; HY-133129; CS-0112146; 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide; 6-(6-(4-(2-(2-(Adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
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| MOA | Degrader | |||
| External Link | ||||
| GSK343 | Investigative | [17] | ||
| Synonyms |
compound 6 [PMID 24900432]; GSK 343
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| MOA | Inhibitor | |||
| Activity | IC50 = 174 nM | |||
| External Link | ||||
| PMID28394193-Compound-11 | Patented | [18] | ||
| External Link | ||||
| PMID28394193-Compound-10 | Patented | [18] | ||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [12] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| 2C25: Lung cancer | 52 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Adagrasib | Approved | [19] | ||
| Synonyms |
2326521-71-3; MRTX-849; UNII-8EOO6HQF8Y; 8EOO6HQF8Y; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; CHEMBL4594350; SCHEMBL20974691; GTPL10888; Kras G12C inhibitor MRTX849; BCP31538; EX-A3258; MRTX 849; MFCD32263433; s8884; compound 20 [PMID: 32250617]; BS-16211; HY-130149; CS-0105265; 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
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| Amivantamab | Approved | [20] | ||
| External Link | ||||
| Mobocertinib | Approved | [21] | ||
| 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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| Sugemalimab | Approved in China | [22] | ||
| External Link | ||||
| Sacituzumab govitecan | Approved | [23] | ||
| Synonyms |
1491917-83-9; 1535963-91-7; 1796566-95-4; CYSTEINYL CL2A-SN-38; DA64T2C2IO; DTXSID401335985; EX-A4354; F82944; GOVITECAN CYSTEINYL CONJUGATE; hRS 7SN38; hRS7-SN38; IMMU 132; IMMU-132; M9BYU8XDQ6; Sacituzumab govitecan; Sacituzumab govitecan [USAN]; sacituzumab-govitecan; Satralizumab linker; SN-38 CYSTEINYL CONJUGATE; UNII-M9BYU8XDQ6
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| Atezolizumab | Approved | [24] | ||
| External Link | ||||
| Tepotinib | Approved | [25] | ||
| Synonyms |
1100598-32-0; EMD 1214063; UNII-1IJV77EI07; Tepotinib (EMD 1214063); EMD1214063; 1IJV77EI07; MSC-2156119J; Benzonitrile, 3-[1,6-dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]-; C29H28N6O2; Tepotinib [INN]; Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]; Benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo
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| Sotorasib | Approved | [26] | ||
| Synonyms |
AMG-510; AMG510; AMG-510 racemate; 2252403-56-6; AMG 510; Kras G12C inhibitor 9; 2296729-00-3; UNII-2B2VM6UC8G; 2B2VM6UC8G; CHEMBL4535757; 2296729-00-3 (racemate); 4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one; Sotorasib [INN]; 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-((2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl)pyrido(2,3-d)pyrimidin-2-one; AMG510 racemate; Sotorasib [USAN]; AMG-510(racemate); Kras mutant-targeting AMG 510; SCHEMBL20560375; GTPL10678; AMG 510 pound>>AMG-510; AMY16918; BCP30452; BCP33368; EX-A3538; BDBM50514402; NSC818433; s8830; WHO 11370; DB15569; NSC-818433; BS-16684; HY-114277; CS-0081316; compound (R)-38 [PMID: 31820981]; (1m)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(propan-2-yl)pyridin-3-yl)-4-((2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl)pyrido(2,3-d)pyrimidin-2(1H)-one; (1S)-4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 2296729-66-1; Pyrido(2,3-d)pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(1-methylethyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl)-
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| Entrectinib | Approved | [27] | ||
| Synonyms |
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
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| Repotrectinib | Approved | [28] | ||
| Synonyms |
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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| MYL-1402O | Phase 3 | [29] | ||
| Synonyms |
bevacizumab biosimilar
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| AB154 | Phase 3 | [30] | ||
| Synonyms |
Domvanalimab
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| Datopotamab deruxtecan | Phase 3 | [31] | ||
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| CS1001 | Phase 3 | [32] | ||
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| JDQ443 | Phase 3 | [33] | ||
| Synonyms |
(S)-JDQ-443; 1-(6-((4S)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one; 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-inda zol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]- 2-Propen-1-one; 1-[6-[(4R)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one; 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one; 1-{6-[(4M)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5- methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2- azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 2653994-08-0; 2653994-10-4; 2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-; AKOS040757949; AT36708; BDBM50579985; CHEMBL5077861; compound 5 [PMID: 35404998]; CS-0226220; CS-0311034; EX-A5693; example 1a [WO2021120890A1]; GLXC-25533; GTPL11715; HY-139612A; JDQ 443; JDQ 443 [WHO-DD]; JDQ443; JDQ-443; MS-29737; NSC846146; NSC-846146; NVP-JDQ443; NVP-JDQ-443; Opnurasib; opnurasib [INN]; -PROPEN-1-ONE, 1-(6-((4R)-4-(5-CHLORO-6-METHYL-1H-INDAZOL-4-YL)-5-METHYL-3-(1-METHYL-1H-INDAZOL-5-YL)-1H-PYRAZOL-1-YL)-2-AZASPIRO(3.3)HEPT-2-YL)-; Q3W0H3V1LQ; SCHEMBL23533580
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| TRS003 | Phase 3 | [34] | ||
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| Tusamitamab ravtansine | Phase 3 | [35] | ||
| Synonyms |
SAR408701
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| RG6058 | Phase 3 | [36] | ||
| Synonyms |
Tiragolumab
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| GSK4069889 | Phase 2 | [37] | ||
| Synonyms |
TSR-022
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| APL-101 | Phase 2 | [38] | ||
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Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
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| SGN-LIV1A | Phase 2 | [39] | ||
| Synonyms |
Ladiratuzumab Vedotin
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| BNT116 | Phase 2 | [40] | ||
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| AZD7789 | Phase 2 | [41] | ||
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| L-DOS47 | Phase 1/2 | [42] | ||
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| NC318 | Phase 2 | [43] | ||
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| Vorolanib | Phase 2 | [44] | ||
| Synonyms |
UNII-YP8G3I74EL; YP8G3I74EL; 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; Vorolanib [INN]; SCHEMBL2439528; CHEMBL4297587; N-((3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; s6843; DB15247; HY-109019; CS-0030517; Q27294638; 1H-Pyrrole-3-carboxamide, N-((3S)-1-((dimethylamino)carbonyl)-3-pyrrolidinyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-
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| Xofigo | Phase 2 | [45] | ||
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| Bintrafusp alfa | Phase 2 | [46] | ||
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| Voyager-V1 | Phase 2 | [47] | ||
| Synonyms |
VSV-IFNBeta-NIS
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| AB-106 | Phase 2 | [48] | ||
| Synonyms |
DS6051b; GTPL11198; AB106
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| RO-5126766 | Phase 2 | [49] | ||
| Synonyms |
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TC-210 | Phase 1/2 | [50] | ||
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| EMB-01 | Phase 1/2 | [51] | ||
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| NM21-1480 | Phase 1/2 | [52] | ||
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| MRx0518 | Phase 1/2 | [53] | ||
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| DZD9008 | Phase 1/2 | [54] | ||
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| BGB-A425 | Phase 1/2 | [55] | ||
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| Rilvegostomig | Phase 1/2 | [56] | ||
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AZD2936
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| IK-007 | Phase 1/2 | [57] | ||
| Synonyms |
grapiprant
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| IBI318 | Phase 1 | [58] | ||
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| GEN-011 | Phase 1 | [59] | ||
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| ENV-105 | Phase 1 | [60] | ||
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Carotuximab
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| AMG 160 | Phase 1 | [61] | ||
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| ADP-A2M10 | Phase 1 | [62] | ||
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| MEDI5752 | Phase 1 | [63] | ||
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| PF-07104091 | Phase 1 | [64] | ||
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| PF-06936308 | Phase 1 | [65] | ||
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| GEM3PSCA | Phase 1 | [66] | ||
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| PF-07257876 | Phase 1 | [67] | ||
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| Cosibelimab | Phase 1 | [68] | ||
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CK-301/TG-1501
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| Gemcitabine | Approved | [69] | ||
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| SMI-4a | Investigative | [70] | ||
| Synonyms |
438190-29-5; SMI 4a; TCS PIM-1 4a; (Z)-SMI-4a; (Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione; (5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione; CHEMBL183906; (5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE; (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione; 327033-36-3; C11H6F3NO2S; (Z)-5-(3-(Trifluoromethyl)benzylidene)-thiazolidine-2,4-dione; (5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione; Pim inhibitor 4a; 3vc4; SMI-4q; TCS PIM-1-4a; 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione; 5-[3-(Trifluoromethyl)benzylidene]thiazolidine-2,4-dione; cc-717; thiazolidine-2,4-dione, 4a; SCHEMBL2541382; SCHEMBL2541388; BDBM26626; AOB6260; EX-A111; SYN1113; BDBM138364; HMS3229J21; 2720AH; HY-16576A; MFCD01152003; s8005; ZINC12576047; AKOS001314163; SMI-4a, >=98% (HPLC); CCG-265027; NCGC00345836-02; NCGC00345836-14; AC-32861; HY-15474; AB0165836; EC-000.2291; J3.561.866J; A11945; W-5256; US8877795, 12; Q27451064; 5-[[3-(trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
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References
: m6A sites