Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T29355 | Target Info | |||
| Target Name | DNA [cytosine-5]-methyltransferase 3A (DNMT3A) | ||||
| Synonyms |
M.HsaIIIA; Dnmt3a; DNA methyltransferase HsaIIIA; DNA MTase HsaIIIA; DNA (cytosine-5)-methyltransferase 3A
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| Target Type | Patented-recorded Target | ||||
| Gene Name | DNMT3A | ||||
| Biochemical Class | Methyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 6 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
GSK343
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Investigative | Compound Info | ||
| Synonyms |
compound 6 [PMID 24900432]; GSK 343
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
1-(2-((((2S,3S,4R,5R)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)ethyl)-3-ethylurea
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Investigative | Compound Info | ||
| Synonyms |
DS-437; CHEMBL3577854; EX-A3697; BDBM50089221; HY-124131; CS-0084441
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
7-[5-(2-Acetamidoethyl)-2-hydroxyphenyl]-3,5,6-trihydroxy-9,10-dioxoanthracene-1,2-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3414632; BDBM50075185
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| Activity |
IC50 = 50000 nM
|
[3] | |||
| Compound Name |
4-({[2-(2-Furylmethyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]carbonyl}amino)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3922548; AN-979/41971108; HMS1599E18; ZINC692812; BDBM50206866; STK276873; AKOS003344826; MCULE-9783439994; SR-01000286985; SR-01000286985-1
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| Activity |
IC50 = 64000 nM
|
[4] | |||
| Compound Name |
N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indazole-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
GSK926; CHEMBL2204998; SCHEMBL2590353; BDBM50400779
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2204997; SCHEMBL12180659; BDBM50400781
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-((2-(1H-Indol-3-yl)ethyl)amino)-3-(9H-carbazol-9-yl)-propan-2-ol
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Investigative | Compound Info | ||
| Synonyms |
DC_05; DC-05; CHEMBL3358015; C25H25N3O; AOB6967; SYN5082; BDBM50031317; AKOS002242638; AKOS016316322; NCGC00402253-02; AS-16448; DC_05, >=98% (HPLC); HY-12746; ST50753266; 1-carbazol-9-yl-3-[(2-indol-3-ylethyl)amino]propan-2-ol; 1-carbazol-9-yl-3-[2-(1H-indol-3-yl)ethylamino]propan-2-ol; 1-(9H-Carbazole-9-yl)-3-[[2-(1H-indole-3-yl)ethyl]amino]-2-propanol
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. | ||||
| REF 2 | Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. | ||||
| REF 3 | Targeting DNA methylation with small molecules: what's next?. J Med Chem. 2015 Mar 26;58(6):2569-83. | ||||
| REF 4 | Discovery of novel DNA methyltransferase 3A inhibitors via structure-based virtual screening and biological assays. Bioorg Med Chem Lett. 2017 Jan 15;27(2):342-346. | ||||
| REF 5 | Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-41. | ||||
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