Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25265 | Target Info | |||
| Target Name | Enhancer of zeste homolog 2 (EZH2) | ||||
| Synonyms |
Lysine Nmethyltransferase 6; Lysine N-methyltransferase 6; KMT6; Histonelysine Nmethyltransferase EZH2; Histone-lysine N-methyltransferase EZH2; EZH2; ENX1; ENX-1
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|
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| Target Type | Successful Target | ||||
| Gene Name | EZH2 | ||||
| Biochemical Class | Methyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 33 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]-N-[(1-ethylpyrazol-4-yl)methyl]butanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3397320; BDBM50063679
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]-N-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)methyl]butanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3397326; BDBM50063675
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-ylbenzimidazole-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3770275; BDBM50149699
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-ylindazole-6-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3770192; BDBM50149702
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-ylbenzotriazole-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3769778; BDBM50149700
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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-Cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]indazole-6-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3769731; BDBM50149905
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-Phenoxy-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264749; SCHEMBL6120964; BDBM50010660; ZINC10814875; AKOS034129347; MCULE-6995020502; UPCMLD0ENAT5985517:001; Z30259906
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
4-(2-Cyanophenoxy)-3,5-dimethyl-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264782; SCHEMBL8739407; BDBM50010818
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|
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
4-Benzoyl-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264755; SCHEMBL8738588; BDBM50010666
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| Activity |
IC50 = 57000 nM
|
[3] | |||
| Compound Name |
Ezh2-in-3
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264787; SCHEMBL6120847; BDBM50010823; ZINC140132869; SB19049; DB-128307; J3.544.023B
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| Activity |
IC50 = 58300 nM
|
[3] | |||
| Compound Name |
4-(2-Methoxyphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264766; SCHEMBL8738144; BDBM50010677
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|
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| Activity |
IC50 = 59000 nM
|
[3] | |||
| Compound Name |
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]-N-(cyclopropylmethyl)butanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3397317; BDBM50063682
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|
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| Activity |
IC50 = 60000 nM
|
[1] | |||
| Compound Name |
4-(3-Methylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264763; SCHEMBL8738591; BDBM50010674
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|
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| Activity |
IC50 = 61000 nM
|
[3] | |||
| Compound Name |
3-Chloro-4-(2-cyanophenoxy)-N-[1-(2-hydroxyethyl)-2,2,6,6-tetramethylpiperidin-4-yl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264789; BDBM50010825
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|
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| Activity |
IC50 = 62000 nM
|
[3] | |||
| Compound Name |
3-Chloro-4-(2-cyano-3-pyridazin-4-ylphenoxy)-N-(2,2,6,6-tetramethyloxan-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264791; SCHEMBL6120703; BDBM50010827
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|
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| Activity |
IC50 = 66000 nM
|
[3] | |||
| Compound Name |
3-Chloro-4-(2-cyanophenoxy)-N-(3,3-difluoro-2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264790; BDBM50010826
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-Anilino-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264757; SCHEMBL8739251; BDBM50010668
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(Benzenesulfinyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264753; SCHEMBL8739699; BDBM50010664
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(2-Cyanophenoxy)-2-methoxy-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264773; BDBM50010713
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(1-Phenylcyclopropyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264761; SCHEMBL8739386; BDBM50010672
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(4-Methylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264764; SCHEMBL8738111; BDBM50010675
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(N-Methylanilino)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264758; SCHEMBL6119745; BDBM50010669; 4-(Methyl(phenyl)amino)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-Phenylmethoxy-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264751; SCHEMBL8738695; BDBM50010662
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(1-Phenylethyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264760; SCHEMBL8739708; BDBM50010671
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-Benzyl-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264759; SCHEMBL6120593; BDBM50010670
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-[Hydroxy(phenyl)methyl]-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264756; SCHEMBL8738590; BDBM50010667
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
4-(Benzenesulfonyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3264754; SCHEMBL8738630; BDBM50010665
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|
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| Activity |
IC50 ~ 80000 nM
|
[3] | |||
| Compound Name |
6-Cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-1-propan-2-yl-2,3-dihydroindole-4-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3906288; BDBM50205628
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|
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
6-Cyano-1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-2,3-dihydroindole-4-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3933203; BDBM50205634
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|
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]-N-benzylbutanamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3397318; BDBM50063681
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|
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| Activity |
IC50 = 120000 nM
|
[1] | |||
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,3-dimethoxybenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3905088; ZINC9479672; BDBM50193713; AKOS033041171; MCULE-5883877025; Z109712106
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| Activity |
IC50 ~ 140000 nM
|
[5] | |||
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methoxybenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3923075; ZINC7117963; BDBM50193664; AKOS016817218; MCULE-1595823990; Z109711894
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| Activity |
IC50 ~ 150000 nM
|
[5] | |||
| Compound Name |
CC1=C(C(NC(=C1)C)=O)Cnc(C1=C(C(=CC=C1)OC)F)=O
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3964489; SCHEMBL17026159; BDBM50193659
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|
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| Activity |
IC50 ~ 150000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methylbenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3984466; SCHEMBL13280537; ZINC9512511; BDBM50193716; AKOS001279538; MCULE-9005005720; Z109712074; N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2-methylbenzamide
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| Activity |
IC50 > 200000 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | SAH derived potent and selective EZH2 inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1532-7. | ||||
| REF 2 | The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat. J Med Chem. 2016 Feb 25;59(4):1556-64. | ||||
| REF 3 | Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2. ACS Med Chem Lett. 2014 Jan 14;5(4):378-83. | ||||
| REF 4 | Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR. Bioorg Med Chem Lett. 2017 Jan 15;27(2):217-222. | ||||
| REF 5 | Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. J Med Chem. 2016 Sep 22;59(18):8306-25. | ||||
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