| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH2 |
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| Ligand | BDBM50193716 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1615977 (CHEMBL3858046) |
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| IC50 | >200000±n/a nM |
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| Citation |  Kung, PP; Rui, E; Bergqvist, S; Bingham, P; Braganza, J; Collins, M; Cui, M; Diehl, W; Dinh, D; Fan, C; Fantin, VR; Gukasyan, HJ; Hu, W; Huang, B; Kephart, S; Krivacic, C; Kumpf, RA; Li, G; Maegley, KA; McAlpine, I; Nguyen, L; Ninkovic, S; Ornelas, M; Ryskin, M; Scales, S; Sutton, S; Tatlock, J; Verhelle, D; Wang, F; Wells, P; Wythes, M; Yamazaki, S; Yip, B; Yu, X; Zehnder, L; Zhang, WG; Rollins, RA; Edwards, M 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 Chem59:8306-25 (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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| BDBM50193716 |
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| n/a |
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| Name | BDBM50193716 |
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| Synonyms: | CHEMBL3984466 |
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| Type | Small organic molecule |
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| Emp. Form. | C16H18N2O2 |
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| Mol. Mass. | 270.3263 |
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| SMILES | Cc1cc(C)c(CNC(=O)c2ccccc2C)c(=O)[nH]1 |
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| Structure | 
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