m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT05367
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[1] | |||
Non-coding RNA
miR-320b
IGF2BP2
lncRNA miRNA circRNA
Direct
Inhibition
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 | Non-coding RNA (ncRNA) | ||||
| Epigenetic Regulator | hsa-miR-320b | microRNA | View Details | ||
| Regulated Target | Insulin like growth factor 2 mRNA binding protein 2 (IGF2BP2) | View Details | |||
| Crosstalk Relationship | ncRNA → m6A | Inhibition | |||
| Crosstalk Mechanism | ncRNAs directly impacts m6A modification through modulating the expression level of m6A regulator | ||||
| Crosstalk Summary | hsa-miR-320b suppresses lung cancer growth and angiogenesis by inhibiting HNF4G, IGF2BP2 and TK1. 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 | [2] | ||
| 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 | [3] | ||
| 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 | |||
| External Link | ||||
| TK-DLI | Preregistration | [4] | ||
| 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 | [5] | ||
| 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 | [6] | ||
| Synonyms |
Radiosensitizer gene therapy (prostate cancer)
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| MOA | Inhibitor | |||
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| RP101 | Phase 2/3 | [7] | ||
| Synonyms |
SCHEMBL15589316; CHEMBL3703295; BDBM149820; US8975415,
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| MOA | Inhibitor | |||
| Activity | Ki = 100 nM | |||
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| HQK-1004 | Phase 2 | [8] | ||
| 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 | [9] | ||
| 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 | [10] | ||
| 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 | |||
| External Link | ||||
| Rilapladib | Phase 1 | [11] | ||
| MOA | Inhibitor | |||
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| Sitimagene ceradenovec | Discontinued in Phase 3 | [12] | ||
| Synonyms |
Cerepro; EG-009; HSV thymidine kinase gene therapy, Ark
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| MOA | Modulator | |||
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| 6-Hydroxypropylthymine | Investigative | [3] | ||
| 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 | |||
| External Link | ||||
| 3-(2-propyn-1-yl)thymidine | Investigative | [13] | ||
| Synonyms |
3-Propargylthymidine; SCHEMBL1619074; CHEMBL524872
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| MOA | Inhibitor | |||
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| ITdU | Investigative | [11] | ||
| 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 | |||
| External Link | ||||
| 5-Iodo-2'-Deoxyuridine-5'-Monophosphate | Investigative | [3] | ||
| 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 | [14] | ||
| Synonyms |
CHEMBL219905
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| MOA | Inhibitor | |||
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| (South)-Methanocarba-Thymidine | Investigative | [3] | ||
| 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 | |||
| External Link | ||||
| 6-(Dihydroxy-Isobutyl)-Thymine | Investigative | [3] | ||
| 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 | [15] | ||
| 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 | [15] | ||
| Synonyms |
CHEMBL261850; SCHEMBL4314668; BDBM50375781
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| MOA | Inhibitor | |||
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| 9-(4-Hydroxybutyl)-N2-Phenylguanine | Investigative | [3] | ||
| 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 | [15] | ||
| 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 | [16] | ||
| 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 | [17] | ||
| Synonyms |
SCHEMBL4287705
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| MOA | Inhibitor | |||
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| 9-Hydroxypropyladenine, S-Isomer | Investigative | [3] | ||
| 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 | [15] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 5-Bromothienyldeoxyuridine | Investigative | [3] | ||
| 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 | [14] | ||
| 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 | [3] | ||
| 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 | [15] | ||
| 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 | [15] | ||
| MOA | Inhibitor | |||
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| 2'-Deoxyuridine | Investigative | [2] | ||
| 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 | [14] | ||
| 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 | [3] | ||
| 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 | [14] | ||
| 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 | [7] | ||
| 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 | [14] | ||
| 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 | [3] | ||
| 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 | [3] | ||
| 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 | [18] | ||
| 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 | [19] | ||
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| Mobocertinib | Approved | [20] | ||
| 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 | [21] | ||
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| Sacituzumab govitecan | Approved | [22] | ||
| 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 | [23] | ||
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| Tepotinib | Approved | [24] | ||
| 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 | [25] | ||
| 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 | [26] | ||
| 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 | [27] | ||
| Synonyms |
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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| MYL-1402O | Phase 3 | [28] | ||
| Synonyms |
bevacizumab biosimilar
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| AB154 | Phase 3 | [29] | ||
| Synonyms |
Domvanalimab
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| Datopotamab deruxtecan | Phase 3 | [30] | ||
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| CS1001 | Phase 3 | [31] | ||
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| JDQ443 | Phase 3 | [32] | ||
| 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 | [33] | ||
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| Tusamitamab ravtansine | Phase 3 | [34] | ||
| Synonyms |
SAR408701
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| RG6058 | Phase 3 | [35] | ||
| Synonyms |
Tiragolumab
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| GSK4069889 | Phase 2 | [36] | ||
| Synonyms |
TSR-022
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| APL-101 | Phase 2 | [37] | ||
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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 | [38] | ||
| Synonyms |
Ladiratuzumab Vedotin
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| BNT116 | Phase 2 | [39] | ||
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| AZD7789 | Phase 2 | [40] | ||
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| L-DOS47 | Phase 1/2 | [41] | ||
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| NC318 | Phase 2 | [42] | ||
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| Vorolanib | Phase 2 | [43] | ||
| 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 | [44] | ||
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| Bintrafusp alfa | Phase 2 | [45] | ||
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| Voyager-V1 | Phase 2 | [46] | ||
| Synonyms |
VSV-IFNBeta-NIS
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| AB-106 | Phase 2 | [47] | ||
| Synonyms |
DS6051b; GTPL11198; AB106
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| RO-5126766 | Phase 2 | [48] | ||
| Synonyms |
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TC-210 | Phase 1/2 | [49] | ||
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| EMB-01 | Phase 1/2 | [50] | ||
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| NM21-1480 | Phase 1/2 | [51] | ||
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| MRx0518 | Phase 1/2 | [52] | ||
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| DZD9008 | Phase 1/2 | [53] | ||
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| BGB-A425 | Phase 1/2 | [54] | ||
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| Rilvegostomig | Phase 1/2 | [55] | ||
| Synonyms |
AZD2936
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| IK-007 | Phase 1/2 | [56] | ||
| Synonyms |
grapiprant
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| IBI318 | Phase 1 | [57] | ||
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| GEN-011 | Phase 1 | [58] | ||
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| ENV-105 | Phase 1 | [59] | ||
| Synonyms |
Carotuximab
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| AMG 160 | Phase 1 | [60] | ||
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| ADP-A2M10 | Phase 1 | [61] | ||
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| MEDI5752 | Phase 1 | [62] | ||
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| PF-07104091 | Phase 1 | [63] | ||
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| PF-06936308 | Phase 1 | [64] | ||
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| GEM3PSCA | Phase 1 | [65] | ||
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| PF-07257876 | Phase 1 | [66] | ||
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| Cosibelimab | Phase 1 | [67] | ||
| Synonyms |
CK-301/TG-1501
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| Gemcitabine | Approved | [68] | ||
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| SMI-4a | Investigative | [69] | ||
| 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