Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 |
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Ligand | BDBM50193660 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1615982 (CHEMBL3858051) |
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IC50 | 1187±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 |
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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BDBM50193660 |
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n/a |
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Name | BDBM50193660 |
Synonyms: | CHEMBL3928387 |
Type | Small organic molecule |
Emp. Form. | C20H23ClN2O3 |
Mol. Mass. | 374.861 |
SMILES | CC(C)Oc1ccc2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl |
Structure |
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