Reaction Details |
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Target | Polycomb protein EED |
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Ligand | BDBM24226 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1437166 (CHEMBL3382328) |
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Ki | 23010±n/a nM |
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Citation | Kong, X; Chen, L; Jiao, L; Jiang, X; Lian, F; Lu, J; Zhu, K; Du, D; Liu, J; Ding, H; Zhang, N; Shen, J; Zheng, M; Chen, K; Liu, X; Jiang, H; Luo, C Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2. J Med Chem57:9512-21 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Polycomb protein EED |
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Name: | Polycomb protein EED |
Synonyms: | EED | EED_HUMAN | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1 | hEED |
Type: | Protein |
Mol. Mass.: | 50201.68 |
Organism: | Homo sapiens (Human) |
Description: | O75530 |
Residue: | 441 |
Sequence: | MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTP
NAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNR
VTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITM
QCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVL
SADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFS
TRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQ
CDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSR
DSSILIAVCDDASIWRWDRLR
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BDBM24226 |
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n/a |
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Name | BDBM24226 |
Synonyms: | 1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine | ASTEMIZOLE | Astemizole, [O-Methyl-3H] | CHEMBL296419 | Hismanal | Histaminos | [3H]-ASTEMIZOLE | [3H]Astemizole | cid_2247 | med.21724, Compound Astemizole |
Type | Radiolabeled ligand |
Emp. Form. | C28H31FN4O |
Mol. Mass. | 458.5703 |
SMILES | COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 |
Structure |
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