| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH2 |
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| Ligand | BDBM50400778 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_879124 (CHEMBL2209069) |
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| IC50 | 174±n/a nM |
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| Citation |  Verma, SK; Tian, X; LaFrance, LV; Duquenne, C; Suarez, DP; Newlander, KA; Romeril, SP; Burgess, JL; Grant, SW; Brackley, JA; Graves, AP; Scherzer, DA; Shu, A; Thompson, C; Ott, HM; Aller, GS; Machutta, CA; Diaz, E; Jiang, Y; Johnson, NW; Knight, SD; Kruger, RG; McCabe, MT; Dhanak, D; Tummino, PJ; Creasy, CL; Miller, WH Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett3:1091-1096 (2012) [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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| BDBM50400778 |
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| n/a |
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| Name | BDBM50400778 |
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| Synonyms: | CHEMBL2204995 |
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| Type | Small organic molecule |
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| Emp. Form. | C31H39N7O2 |
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| Mol. Mass. | 541.6871 |
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| SMILES | CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccnc(c1)N1CCN(C)CC1 |
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| Structure | 
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