Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 |
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Ligand | BDBM171998 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1558366 (CHEMBL3772958) |
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EC50 | 700±n/a nM |
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Citation | Kuntz, KW; Campbell, JE; Keilhack, H; Pollock, RM; Knutson, SK; Porter-Scott, M; Richon, VM; Sneeringer, CJ; Wigle, TJ; Allain, CJ; Majer, CR; Moyer, MP; Copeland, RA; Chesworth, R The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat. J Med Chem59:1556-64 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase EZH2 |
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Name: | Histone-lysine N-methyltransferase EZH2 |
Synonyms: | ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6 |
Type: | Protein |
Mol. Mass.: | 85367.84 |
Organism: | Homo sapiens (Human) |
Description: | Q15910 |
Residue: | 746 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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BDBM171998 |
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n/a |
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Name | BDBM171998 |
Synonyms: | US10155002, Compound 2 | US9090562, 2 |
Type | Small organic molecule |
Emp. Form. | C33H42N4O3 |
Mol. Mass. | 542.7116 |
SMILES | CN(C1CCCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1 |
Structure |
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