| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH2 |
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| Ligand | BDBM50149638 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1558364 (CHEMBL3772956) |
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| IC50 | 900±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 |
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| Synonyms: | ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6 |
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| Type: | Protein |
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| Mol. Mass.: | 85367.84 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q15910 |
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| Residue: | 746 |
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| Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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| BDBM50149638 |
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| n/a |
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| Name | BDBM50149638 |
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| Synonyms: | CHEMBL3770418 | US10273223, Compound B-88 | US9637472, Compound B-88 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H20BrN5O2 |
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| Mol. Mass. | 418.288 |
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| SMILES | CC(C)n1ncc2c(cc(Br)nc12)C(=O)NCc1c(C)cc(C)[nH]c1=O |
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| Structure | 
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