m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03467
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[1], [2] | |||
Histone modification
H3K4me3
SETD1A
IGF2BP2
Direct
Enhancement
m6A modification
TK1
TK1
IGF2BP2
: m6A sites
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| m6A Modification: | |||||
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| m6A Regulator | Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) | READER | |||
| m6A Target | Thymidine kinase, cytosolic (TK1) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone-lysine N-methyltransferase SETD1A (SETD1A) | WRITER | View Details | ||
| Regulated Target | Histone H3 lysine 4 trimethylation (H3K4me3) | View Details | |||
| Downstream Gene | IGF2BP2 | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Enhancement | |||
| Crosstalk Mechanism | histone modification directly impacts m6A modification through modulating the level of m6A regulator | ||||
| Crosstalk Summary | This feeds back upon the IGF2BP2 promoter region by further increasing SETD1A-mediated Histone H3 lysine 4 trimethylation (H3K4me3) level to upregulate IGF2BP2 expression. We demonstrated that this positive feedback loop between IGF2BP2 and SLC7A5 promotes lung cancer radioresistance through the AKT/mTOR pathway. In lung cancer, IGF2BP2 modified m6A to increase the expression of Thymidine kinase, cytosolic (TK1), thus promoting angiogenesis. | ||||
| Responsed Disease | Lung cancer | ICD-11: 2C25 | |||
In-vitro Model |
A-549 | Lung adenocarcinoma | Homo sapiens | CVCL_0023 | |
| NCI-H460 | Lung large cell carcinoma | Homo sapiens | CVCL_0459 | ||
| NCI-H1299 | Lung large cell carcinoma | Homo sapiens | CVCL_0060 | ||
| NHBE (Normal bronchial epithelial cells) | |||||
| In-vivo Model | Suspension of H1299 cells (5.0 × 105) was subcutaneously injected into the right flanks of the mice. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Thymidine kinase, cytosolic (TK1) | 39 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| DEOXYCYTIDINE | Approved | [3] | ||
| Synonyms |
Cytosine deoxyribonucleoside; 2'-dC; bmse000323; ACMC-209rv6; CYTIDINE, 2'-DEOXY-; Cytosine deoxy nucleoside hydrochloride; 4-amino-1-[4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidin-2(1H)-one; Desoxycytidine; 4-amino-1-(2-deoxypentofuranosyl)pyrimidin-2(1H)-one; 4-amino-1-[4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidin-2-one; 3h-deoxycytidine; 4-amino-1-(4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one; 40093-94-5; AC1L19OG; TimTec1_003892; NCIOpen2_004589; Oprea1_817993
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| MOA | Inhibitor | |||
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| Penciclovir | Approved | [4] | ||
| Synonyms |
39809-25-1; Denavir; Penciclovirum; Vectavir; Penciclovirum [INN-Latin]; Pencyclovir; BRL-39123; BRL 39123; Penciclovir [USAN:INN:BAN]; Penciceovir; UNII-359HUE8FJC; CCRIS 9213; PE2
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| MOA | Inhibitor | |||
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| TK-DLI | Preregistration | [5] | ||
| Synonyms |
TBI-0301; Herpes simplex thymidine kinase suicide gene therapy, MolMed/Takara Bio; HSV thymidine kinase gene therapy (GvH, retroviral vector), Istituto Scientifico H San Raffaele; HSV-TK suicide gene therapy, MolMed/Takara Bio; TK cell therapy (haploidentical haematopoietic stem cell transplantation), MolMed/Takara Bio; HSV-TK gene therapy (haematological malignancies), MolMed/Takara Bio; TK-DLI, San Raffaele/MolMed/Takara Bio; TK gene/cell therapy (bone marrow transplantation-associated GvHD prevention), MolMed/Takara Bio; TK-expressing donor T-cells (bone marrow transplantation-associated GvHD prevention), San Raffaele/MolMed; Thymidine kinase expressing donor T-cells (bone marrow transplantation-associated GvHD prevention), San Raffaele/MolMed/Takara
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| MOA | Modulator | |||
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| FV-100 | Phase 3 | [6] | ||
| Synonyms |
CF-1001; CF-1094; CF-1368; CF-1369; CF-1449; CF-1452; CF-1698; CF-1712; CF-1743; CF-1821; CF-1835; CF-1837; CF-1838; CF-1851; CF-2004; CF-2160; CF-2161; CF-2200; BCNAs (antiviral), FermaVir Pharmaceuticals; Bicyclic nucleoside analogs (VZV infection), FermaVir; Bicyclic nucleoside analogs (VZV infection), Inhibitex; Antivirals (nucleoside derivatives), Welsh School of Pharmacy/Rega; BCNAs (antiviral), Rega/Welsh School of Pharmacy; Bicyclic nucleoside analogs (antiviral), Rega/Welsh School of Pharmacy
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| MOA | Inhibitor | |||
| External Link | ||||
| Radiosensitizer gene therapy | Phase 3 | [7] | ||
| Synonyms |
Radiosensitizer gene therapy (prostate cancer)
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| MOA | Inhibitor | |||
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| RP101 | Phase 2/3 | [8] | ||
| Synonyms |
SCHEMBL15589316; CHEMBL3703295; BDBM149820; US8975415,
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| MOA | Inhibitor | |||
| Activity | Ki = 100 nM | |||
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| HQK-1004 | Phase 2 | [9] | ||
| Synonyms |
Arginine butyrate; VX-105; VX-105); Arginine butyrate (hematological malignancies), HemaQuest
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| MOA | Modulator | |||
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| Ad-OC-hsvTK/valacyclovir | Phase 1 | [10] | ||
| Synonyms |
Ad-OC-hsvTK; Gene therapy (prostate cancer), Winship Cancer Institute; Adenovirus osteocalcin-promoter-driven HSV thymidine Kinase, Winship Cancer Institute; Ad-OC-hsvTK/valacyclovir, Winship Cancer Institute
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| MOA | Inhibitor | |||
| External Link | ||||
| Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy | Phase 1 | [11] | ||
| Synonyms |
Thymidine kinase-expressing adenovirus and ganciclovir suicide genetherapy (cancer); Ad5-SSTR/TK-RGD; Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy (cancer), University of Alabama
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| MOA | Modulator | |||
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| Rilapladib | Phase 1 | [12] | ||
| MOA | Inhibitor | |||
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| Sitimagene ceradenovec | Discontinued in Phase 3 | [13] | ||
| Synonyms |
Cerepro; EG-009; HSV thymidine kinase gene therapy, Ark
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| MOA | Modulator | |||
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| 6-Hydroxypropylthymine | Investigative | [4] | ||
| Synonyms |
6-(3-hydroxypropyl)thymine; 6-(3-hydroxypropyl)-5-methylpyrimidine-2,4(1H,3H)-dione; 2,4(1H,3H)-Pyrimidinedione, 6-(3-hydroxypropyl)-5-methyl-; 156569-47-0; AC1L1CEO; SCHEMBL4315838; CHEBI:43299; CTK8A4001; DB04139
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| MOA | Inhibitor | |||
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| 3-(2-propyn-1-yl)thymidine | Investigative | [14] | ||
| Synonyms |
3-Propargylthymidine; SCHEMBL1619074; CHEMBL524872
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| MOA | Inhibitor | |||
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| ITdU | Investigative | [12] | ||
| Synonyms |
3-Hydroxyandrost-5-en-17-one; Diandron, 17-Hormoforin; A-hydroxy-5-androsten-17-one; Spectrum_000661; SpecPlus_000094; Androst-5-en-17-one, 3-hydroxy-, (3.beta.)-; Spectrum3_000116; Spectrum5_000130; Spectrum4_001395; Spectrum2_000359; AC1L18FD; KBioSS_001141; KBioGR_001750; CHEMBL31399; DivK1c_006190; SPBio_000457; SCHEMBL9969169; KBio1_001134; KBio3_000872; KBio2_006277; KBio2_003709; KBio2_001141; CHEBI:95212; MolPort-003-891-893; ALBB-023670; CCG-38634; Androst-5-en-17-one, 3-hydroxy-
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| MOA | Inhibitor | |||
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| 5-Iodo-2'-Deoxyuridine-5'-Monophosphate | Investigative | [4] | ||
| Synonyms |
AC1L52UF; [(2R,3S)-3-hydroxy-5-(5-iodo-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methyl dihydrogen phosphate
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| MOA | Inhibitor | |||
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| 1-[2-(2-triphenylmethoxyethoxy)ethyl]thymine | Investigative | [15] | ||
| Synonyms |
CHEMBL219905
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| MOA | Inhibitor | |||
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| (South)-Methanocarba-Thymidine | Investigative | [4] | ||
| Synonyms |
south-methanocarbathymidine; 1-[(1S,3S,4R,5S)-3-hydroxy-4-(hydroxymethyl)bicyclo[3.1.0]hex-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione; SCT; 1-[(1S,3S,4R,5S)-3-hydroxy-4-(hydroxymethyl)bicyclo[3.1.0]hexan-1-yl]thymine; (1S,3S,4R,5S)-3-hydroxy-4-hydroxymethyl-1-(5-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)bicyclo[3.1.0]hexane; [(S)-Methanocarba-T]; South-Methanocarba-thymine; AC1L9L1U; 2'-exo-Methanocarbathymidine; CHEBI:45586; XRMLXZVSFIBRRJ-PEFMBERDSA-N; DB02921
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| MOA | Inhibitor | |||
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| 6-(Dihydroxy-Isobutyl)-Thymine | Investigative | [4] | ||
| Synonyms |
DHBT; 6-(1,3-dihydroxyisobutyl)thymine; 6-[3-hydroxy-2-(hydroxymethyl)propyl]-5-methylpyrimidine-2,4(1H,3H)-dione; 6-[3-hydroxy-2-(hydroxymethyl)propyl]-5-methyl-2,4(1h,3h)-pyrimidinedione; 6-[3-hydroxy-2-(hydroxymethyl)propyl]thymine; CCV; AC1L1CE0; CTK8A1595; CHEBI:41485; DB02500; 6-[3-hydroxy-2-(hydroxymethyl)propyl]-5-methyl-1H-pyrimidine-2,4-dione
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| MOA | Inhibitor | |||
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| 5-propyl-2'-deoxyuridine | Investigative | [16] | ||
| Synonyms |
27826-74-0; CHEMBL221982; 5-Propyldeoxyuridine; 2'-Deoxy-5-propyluridine; 5-Propyl-dUrd; 5-Propyl-2'-desoxyuridine; AC1L4N4W; 2'-deoxy-5-n-propyluridine; Uridine,2'-deoxy-5-propyl-; Uridine, 2'-deoxy-5-propyl-; SCHEMBL2396529; CTK4G0305; DTXSID30182141; MBERTAKFBYOAHR-IVZWLZJFSA-N; BDBM50375778; 1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-propylpyrimidine-2,4-dione
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| MOA | Inhibitor | |||
| Activity | Ki = 20000 nM | |||
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| L-5-(bromovinyl)deoxyuridine | Investigative | [16] | ||
| Synonyms |
CHEMBL261850; SCHEMBL4314668; BDBM50375781
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| MOA | Inhibitor | |||
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| 9-(4-Hydroxybutyl)-N2-Phenylguanine | Investigative | [4] | ||
| Synonyms |
HBPG; CHEMBL406254; BPG; 6H-Purin-6-one, 1,9-dihydro-9-(4-hydroxybutyl)-2-(phenylamino)-; 161363-19-5; 1QHI; AC1L9LM8; SCHEMBL1506775; SCHEMBL17485742; CTK0A9784; BDBM21866; DTXSID00332272; AKOS030558959; N2-Phenyl-9-(4-hydroxybutyl) guanine; DB02495; 9-(4-Hydroxybuthyl)-N2-Phenylguanine; 2-anilino-9-(4-hydroxybutyl)-1H-purin-6-one; 2-anilino-9-(4-hydroxybutyl)-3H-purin-6-one; 9-(4-hydroxybutyl)-2-(phenylamino)-1,9-dihydro-6H-purin-6-one
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| MOA | Inhibitor | |||
| Activity | Ki = 50 nM | |||
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| L-5-iodo-2'-deoxyuridine | Investigative | [16] | ||
| Synonyms |
CHEMBL408518; URIDINE, 2'-DEOXY-5-IODO-; AC1LAEAG; SCHEMBL51859; XQFRJNBWHJMXHO-XVMARJQXSA-N; ZINC5223557; BDBM50375780; FT-0620507; 5-Iodo-1-(2-deoxy-alpha-D-ribofuranosyl)uracil
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| MOA | Inhibitor | |||
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| 3'-(1,2,3-Triazol-1-yl)-3'-deoxy-beta-D-thymidine | Investigative | [17] | ||
| Synonyms |
3'-(1,2,3-Triazol)dT; 3'-Deoxy-3'-(1,2,3-triazol-1-yl)thymidine; 122370-58-5; CHEMBL1092729; Thymidine,3'-deoxy-3'-(1H-1,2,3-triazol-1-yl)- (9CI); AC1L9Q42; SCHEMBL9965127; CTK4B3087; DTXSID60153586; BDBM50314847; 3'-(1H-1,2,3-Triazol-1-yl)-3'-deoxythymidine; 3''-(1,2,3-Triazol-1-yl)-3''-deoxy-beta-D-thymidine; 1-[(2R,4S,5S)-5-(hydroxymethyl)-4-(triazol-1-yl)tetrahydrofuran-2-yl]-5-methyl-pyrimidine-2,4-dione
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| MOA | Inhibitor | |||
| Activity | IC50 >= 500000 nM | |||
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| BVDU-MP | Investigative | [18] | ||
| Synonyms |
SCHEMBL4287705
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| MOA | Inhibitor | |||
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| 9-Hydroxypropyladenine, S-Isomer | Investigative | [4] | ||
| Synonyms |
(S)-1-(6-Amino-9H-purin-9-yl)propan-2-ol; 14047-27-9; (S)-9-(2-Hydroxypropyl)adenine; (2S)-1-(6-amino-9H-purin-9-yl)propan-2-ol; AC1L9HLO; Tenofovir Related Compound 9; S-9-(2-hydroxypropyl)adenine; SCHEMBL5810639; 9H-Purine-9-ethanol, 6-amino-alpha-methyl-, (alphaS)-; CTK8C2128; DTXSID60332177; MolPort-003-848-032; ZINC2046907; ANW-67863; 6827AA; DB03000; SC-43410; AK-82057; AJ-33425; KB-106920; TX-015702; (2S)-1-(6-aminopurin-9-yl)propan-2-ol; AX8236781; FT-0696938; ST24035731
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| MOA | Inhibitor | |||
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| 2-phenylamino-9-(4-hydroxy-butyl)-6-oxopurine | Investigative | [16] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 5-Bromothienyldeoxyuridine | Investigative | [4] | ||
| Synonyms |
CHEMBL1231486; 5-(5-Bromo-2-thienyl)-2'-deoxyuridine; 5-(5-Bromothien-2-yl)-2'-deoxyuridine; BTD; 134333-70-3; BTDU; Uridine,5-(5-bromo-2-thienyl)-2'-deoxy-; AC1L9K0Y; SCHEMBL1636648; CHEMBL358374; CTK4B9107; BDBM50054768; DB03804; 5-(5-Bromothien-2-yl)-2'-deoxyuridine-; 5-(5-bromothiophen-2-yl)-2'-deoxyuridine; 5-(5-Bromothien-2-yl)-1- (.beta.-D-2-deoxyribofuranos-1-yl)uracil; 5-(5-Bromo-thiophen-2-yl)-1-(4-hydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidine-2,4-dione
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| MOA | Inhibitor | |||
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| 1-[7-(triphenylmethoxy)heptyl]thymine | Investigative | [15] | ||
| Synonyms |
CHEMBL219367; 921587-94-2; CTK3G1843; DTXSID20582671; BDBM50200997; 5-Methyl-1-[7-(triphenylmethoxy)heptyl]pyrimidine-2,4(1H,3H)-dione; 2,4(1H,3H)-Pyrimidinedione, 5-methyl-1-[7-(triphenylmethoxy)heptyl]-
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| MOA | Inhibitor | |||
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| 9-Hydroxypropyladenine, R-Isomer | Investigative | [4] | ||
| Synonyms |
14047-28-0; (R)-9-(2-Hydroxypropyl)adenine; (R)-1-(6-Amino-9H-purin-9-yl)propan-2-ol; (R)-(+)-9-(2-HYDROXYPROPYL)ADENINE; (2R)-1-(6-aminopurin-9-yl)propan-2-ol; UNII-43H6SBP55W; (R)-9-(2-hydroxypropyl) adenine; 9H-Purine-9-ethanol, 6-amino-alpha-methyl-, (alphaR)-; 43H6SBP55W; AK-59150; (2R)-1-(6-Amino-9H-purin-9-yl)propan-2-ol; ARP; W-201193; 9-(2-Hydroxypropyl)adenine, (R)-; PubChem9984; R-9-(2-hydroxypropyl)adenine [WHO-DD]; AC1L9HLR; 9H-Purine-9-ethanol, 6-amino-alpha-methyl-, D-
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| MOA | Inhibitor | |||
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| Edoxudine | Investigative | [16] | ||
| Synonyms |
5-ethyl-1-[4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3-dihydropyrimidine-2,4-d ione; ORF-15817; RWJ-15817; Edurid (Salt/Mix); 1-(2-deoxypentofuranosyl)-5-ethylpyrimidine-2,4(1h,3h)-dione; AC1L1CAR; .beta.-5-Ethyldeoxyuridine; TimTec1_004024; SCHEMBL65580; MLS001360450; AC1Q69H9; 5-ethyl-1-[4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione; .beta.-5-Ethyl-2'-deoxyuridine; XACKNLSZYYIACO-UHFFFAOYSA-N; HMS3056J10; HMS3369L22; HMS1545G20; EDU; AKOS024282522; 5-Ethyl-2'-deoxyuridine; MCULE-3445830855; ST056929
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| MOA | Inhibitor | |||
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| N2-(3-trifluoromethylphenyl)guanine | Investigative | [16] | ||
| MOA | Inhibitor | |||
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| 2'-Deoxyuridine | Investigative | [3] | ||
| Synonyms |
951-78-0; deoxyuridine; Uracil deoxyriboside; 1-((2R,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione; 2-Deoxyuridine; Deoxyribose uracil; 2'-Desoxyuridine; UNII-W78I7AY22C; CCRIS 2832; dURD; EINECS 213-455-7; BRN 0024433; 1-(2-Deoxy-beta-D-ribofuranosyl)uracil; W78I7AY22C; CHEBI:16450; 2 -Deoxyuridine; 1-(2-Deoxy-beta-D-erythro-pentofuranoxyl)uracil; MFCD00006527; AK-54658; 2,4(1H,3H)-Pyrimidinedione, 1-(2-deoxy-beta-D-ribofuranosyl)-; NSC 23615
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| MOA | Inhibitor | |||
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| 1-[5-(triphenylmethoxy)pentyl]thymine | Investigative | [15] | ||
| Synonyms |
CHEMBL216997; 921587-92-0; CTK3G1845; DTXSID10582665; BDBM50201001; 5-Methyl-1-[5-(triphenylmethoxy)pentyl]pyrimidine-2,4(1H,3H)-dione; 2,4(1H,3H)-Pyrimidinedione, 5-methyl-1-[5-(triphenylmethoxy)pentyl]-
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| MOA | Inhibitor | |||
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| Deoxythymidine | Investigative | [4] | ||
| Synonyms |
Thymidine; 50-89-5; 2'-Deoxythymidine; Beta-Thymidine; 5-Methyldeoxyuridine; Thymidin; DThyd; 5-Methyl-2'-deoxyuridine; Thymine-2-deoxyriboside; Thyminedeoxyriboside; Thymine-2-desoxyriboside; 5-Methyldeoxyurindine; dThd; Uridine, 2'-deoxy-5-methyl-; Thymine deoxyriboside; 1-((2R,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione; dT; UNII-VC2W18DGKR; Deoxyribothymidine; AI3-52267; 2'-thymidine; beta-D-Ribofuranoside, thymine-1 2-deoxy-; CCRIS 1283; CHEBI:17748
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM | |||
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| 1-[6-(triphenylmethoxy)hexyl]thymine | Investigative | [15] | ||
| Synonyms |
CHEMBL216998; 921587-93-1; CTK3G1844; DTXSID00658828; BDBM50200990; 5-Methyl-1-[6-(triphenylmethoxy)hexyl]pyrimidine-2,4(1H,3H)-dione; 2,4(1H,3H)-Pyrimidinedione, 5-methyl-1-[6-(triphenylmethoxy)hexyl]-
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| MOA | Inhibitor | |||
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| P1-(5'-Adenosyl)P5-(5'-Thymidyl)Pentaphosphate | Investigative | [8] | ||
| Synonyms |
CHEMBL1236157; T5A; 3tmk; 1mrn; 4TMK; AC1L9KL2; BDBM50366828; DB03280; adenosine 5'-(hexahydrogen pentaphosphate), P"" 5'-ester with thymidine; 103137-88-8; [[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [hydroxy-[hydroxy-[hydroxy-[[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy]phosphoryl]oxyphosphoryl]oxyphosphoryl] hydrogen phosphate
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| MOA | Inhibitor | |||
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| 1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine | Investigative | [15] | ||
| Synonyms |
CHEMBL101135; 5-methyl-1-[(Z)-4-trityloxybut-2-enyl]pyrimidine-2,4-dione; AC1O54TL; 5-Methyl-1-(4-trityloxy-but-2-enyl)-1H-pyrimidine-2,4-dione; SCHEMBL19196301; BDBM50118490; 5-Methyl-1-[(2Z)-4-(trityloxy)but-2-enyl]pyrimidine-2,4(1H,3H)-dione
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| MOA | Inhibitor | |||
| Activity | IC50 = 180 nM | |||
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| Thymidine-5'-Phosphate | Investigative | [4] | ||
| Synonyms |
Thymidine 5'-monophosphate; dTMP(-); thymidine 5'-phosphate(1-); CHEBI:46960; thymidine 5'-(hydrogen phosphate)
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| MOA | Inhibitor | |||
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| 2'-deoxythymidine triphosphate | Investigative | [4] | ||
| Synonyms |
Thymidine-5'-triphosphate; dTTP; thymidine 5'-triphosphate; Deoxy-TTP; Deoxythymidine 5'-triphosphate; 5'-TTP; thymidine 5'-(tetrahydrogen triphosphate); TTP (nucleotide); thymidine triphosphate; pppdT; TTP; UNII-QOP4K539MU; 5-Methyl-dUTP; dThd5'PPP; CHEBI:18077; EINECS 206-669-7; QOP4K539MU; CHEMBL363559; 2'-Deoxythymidine 5'-triphosphate; 18423-43-3; [hydroxy-[[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)tetrahydrofuran-2-yl]methoxy]phosphoryl] phosphono hydrogen phosphate; DEOXYTHYMIDINE_TRIPHOSPHATE
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| MOA | Inhibitor | |||
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| 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] | ||
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| 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] | ||
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| 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] | ||
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| 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] | ||
| Synonyms |
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] | ||
| Synonyms |
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] | ||
| Synonyms |
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