Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T44916 | Target Info | |||
| Target Name | Embryonic ectoderm development protein (EED) | ||||
| Synonyms |
hEED; WD protein associating with integrin cytoplasmic tails 1; WAIT-1
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| Target Type | Clinical trial Target | ||||
| Gene Name | EED | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Astemizole
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|
Withdrawn from market | Compound Info | ||
| Synonyms |
Alermizol; Astemina; Astemisan; Astemisol; Astemison; Astemizol; Astemizolum; Astesen; Emdar; Esmacen; Fustermizol; Hestazol; Hismanal; Histamen; Histaminos; Histazol; Hubermizol; Kelp; Laridal; Metodih; Metodik; Paralergin; Retolen; Rifedot; Rimbol; Romadin; Simprox; Urdrim; Wareezol; Waruzol; AlacanBrand of Astemizole; Alonga Brand of Astemizole; Astemizol Alonga; Astemizol [German]; Astemizol ratiopharm; Astemizole Alacan Brand; Astemizole Alonga Brand; Astemizole Byk Brand; Astemizole Diba Brand; Astemizole Elfar Brand; Astemizole Esteve Brand; Astemizole Fustery Brand; Astemizole ICN Brand; Astemizole Janssen Brand; Astemizole Lesvi Brand; Astemizole McNeil Brand; Astemizole Medinsa Brand; Astemizole Merck Brand; Astemizole Senosiain Brand; Astemizole Septa Brand; Astemizole Smaller Brand; Astemizole Urbion Brand; Astemizole Vita Brand; Astemizole ratiopharm Brand; Byk Brand of Astemizole; Diba Brand of Astemizole; Elfar Brand of Astemizole; Esteve Brand of Astemizole; Fustery Brand of Astemizole; ICN Brand of Astemizole; Janssen Brand of Astemizole; Lesvi Brand of Astemizole; McNeil Brand of Astemizole; Medinsa Brand of Astemizole; Merck Brand of Astemizole; Ratiopharm Brand of Astemizole; Reig Jofre Brand of Astemizole; Senosiain Brand of Astemizole; Septa Brand of Astemizole; Smaller Brand of Astemizole; Urbion Brand of Astemizole; Vita Brand of Astemizole; R 42512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
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| Activity |
IC50 = 93800 nM
|
[1] | |||
| Compound Name |
(3R,4S)-N,N-Dimethyl-1-[(2-methylimidazo[1,2-a]pyrimidin-3-yl)methyl]-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4105413; BDBM50235628
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| Activity |
Ki ~ 50000 nM
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[2] | |||
| Compound Name |
(3R,4S)-1-(Imidazo[1,2-a]pyridin-7-ylmethyl)-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4087547; BDBM50235646
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
(3R,4S)-1-[(1-Ethyl-3-methylpyrazol-4-yl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082105; BDBM50235634
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
(3R,4S)-N,N-Dimethyl-1-[(1-methylimidazol-2-yl)methyl]-4-(1-methylindol-3-yl)pyrrolidin-3-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4063970; BDBM50235629
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
3-(1-Benzofuran-7-ylmethyl)piperidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082435; BDBM50259904
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| Activity |
IC50 = 95000 nM
|
[3] | |||
| Compound Name |
3-(3-Methoxybenzyl)piperidine
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Investigative | Compound Info | ||
| Synonyms |
3-(3-Methoxy-benzyl)-piperidine; 3-[(3-methoxyphenyl)methyl]piperidine; CHEMBL4101947; SCHEMBL3164096; 3-(3-methoxybenzyl)-piperidine; CTK5E3242; DTXSID20588799; 9441AE; BDBM50259900; MFCD05863593; AKOS011516608; AB22587; FT-0681579; AR-527/43467599
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| Activity |
IC50 = 95000 nM
|
[3] | |||
| Compound Name |
9-Benzyl-5-chloro-7,8,9,10-tetrahydro-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4085277; BDBM50235993
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-[(4-Fluoro-3-methoxyphenyl)methyl]piperidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4063710; BDBM50259911
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| Activity |
IC50 = 119000 nM
|
[3] | |||
| Compound Name |
3-(2-Methoxy-benzyl)-piperidine
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Investigative | Compound Info | ||
| Synonyms |
3-(2-Methoxybenzyl)piperidine; 3-[(2-methoxyphenyl)methyl]piperidine; CHEMBL4087849; SCHEMBL3160580; 3-(2-Methoxybenzyl);piperidine; CTK4I5552; DTXSID90407448; 3032AE; BDBM50259902; MFCD05863594; AKOS009157643; AB22588; BB 0259220; FT-0681580; T6528
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| Activity |
IC50 = 146000 nM
|
[3] | |||
| Compound Name |
3-(1-Benzofuran-7-ylmethyl)piperidine-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4086249; BDBM50259909
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| Activity |
IC50 = 174000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-(4-Methoxybenzyl)piperidine
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|
Investigative | Compound Info | ||
| Synonyms |
3-(4-Methoxy-benzyl)-piperidine; 3-[(4-methoxyphenyl)methyl]piperidine; Piperidine, 3-[(4-methoxyphenyl)methyl]-; CHEMBL4077141; MFCD05863592; F9995-2419; SCHEMBL3163390; 3-(4-Methoxybenzyl)-piperidine; KS-00000DOA; DTXSID50396849; 1997AJ; BDBM50259903; AKOS009157508; AB22585; MCULE-4931710930; AS-31282; SY020823; EN300-86152; K-4357; AR-527/43467598
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| Activity |
IC50 > 500000 nM
|
[3] | |||
| Compound Name |
3-Benzylpiperidine
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|
Investigative | Compound Info | ||
| Synonyms |
3-Benzyl-piperidine; Piperidine, 3-(phenylmethyl)-; Piperidine,3-(phenylmethyl)-; CHEMBL1618229; 3-benzyl piperidine; EINECS 237-088-7; PubChem6850; 3-phenylmethylpiperidine; 3-(Phenylmethyl)piperidine; (racemic) 3-benzylpiperidine; (+/-)-3-Benzyl-piperidine; SCHEMBL1761058; CTK4C0125; KS-00003KRK; DTXSID10929233; HMS1698E08; 3950AD; BDBM50259901; MFCD03426127; SBB010586; AKOS000507669; AKOS016343916; AB14787; FS-2649; MCULE-6410064877; VP80141; NCGC00245432-01; AM807243; DB-008285; BB 0253759; FT-0636926; ST50287661; EN300-70459; Z-5189; AR-527/43467597; F8887-4651
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| Activity |
IC50 > 500000 nM
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[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2. J Med Chem. 2014 Nov 26;57(22):9512-21. | ||||
| REF 2 | SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding. Bioorg Med Chem Lett. 2017 Apr 1;27(7):1576-1583. | ||||
| REF 3 | Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase. J Med Chem. 2017 Jan 12;60(1):415-427. | ||||
| REF 4 | Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. J Med Chem. 2017 Mar 23;60(6):2215-2226. | ||||
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