| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH1 |
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| Ligand | BDBM50246967 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1677282 (CHEMBL4027425) |
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| Ki | 70±n/a nM |
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| Citation |  Kung, PP; Bingham, P; Brooun, A; Collins, M; Deng, YL; Dinh, D; Fan, C; Gajiwala, KS; Grantner, R; Gukasyan, HJ; Hu, W; Huang, B; Kania, R; Kephart, SE; Krivacic, C; Kumpf, RA; Khamphavong, P; Kraus, M; Liu, W; Maegley, KA; Nguyen, L; Ren, S; Richter, D; Rollins, RA; Sach, N; Sharma, S; Sherrill, J; Spangler, J; Stewart, AE; Sutton, S; Uryu, S; Verhelle, D; Wang, H; Wang, S; Wythes, M; Xin, S; Yamazaki, S; Zhu, H; Zhu, J; Zehnder, L; Edwards, M Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin J Med Chem61:650-665 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Histone-lysine N-methyltransferase EZH1 |
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| Name: | Histone-lysine N-methyltransferase EZH1 |
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| Synonyms: | ENX-2 | EZH1 | EZH1_HUMAN | Enhancer of zeste homolog 1 | Enhancer of zeste homolog 1 (EZH1) | Histone-lysine N-methyltransferase EZH1 | KIAA0388 |
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| Type: | Protein |
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| Mol. Mass.: | 85285.34 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q92800 |
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| Residue: | 747 |
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| Sequence: | MEIPNPPTSKCITYWKRKVKSEYMRLRQLKRLQANMGAKALYVANFAKVQEKTQILNEEW
KKLRVQPVQSMKPVSGHPFLKKCTIESIFPGFASQHMLMRSLNTVALVPIMYSWSPLQQN
FMVEDETVLCNIPYMGDEVKEEDETFIEELINNYDGKVHGEEEMIPGSVLISDAVFLELV
DALNQYSDEEEEGHNDTSDGKQDDSKEDLPVTRKRKRHAIEGNKKSSKKQFPNDMIFSAI
ASMFPENGVPDDMKERYRELTEMSDPNALPPQCTPNIDGPNAKSVQREQSLHSFHTLFCR
RCFKYDCFLHPFHATPNVYKRKNKEIKIEPEPCGTDCFLLLEGAKEYAMLHNPRSKCSGR
RRRRHHIVSASCSNASASAVAETKEGDSDRDTGNDWASSSSEANSRCQTPTKQKASPAPP
QLCVVEAPSEPVEWTGAEESLFRVFHGTYFNNFCSIARLLGTKTCKQVFQFAVKESLILK
LPTDELMNPSQKKKRKHRLWAAHCRKIQLKKDNSSTQVYNYQPCDHPDRPCDSTCPCIMT
QNFCEKFCQCNPDCQNRFPGCRCKTQCNTKQCPCYLAVRECDPDLCLTCGASEHWDCKVV
SCKNCSIQRGLKKHLLLAPSDVAGWGTFIKESVQKNEFISEYCGELISQDEADRRGKVYD
KYMSSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVVMVNGDHRIGIFAKRAIQAG
EELFFDYRYSQADALKYVGIERETDVL
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| BDBM50246967 |
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| n/a |
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| Name | BDBM50246967 |
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| Synonyms: | CHEMBL4080228 | US10570121, Example 81 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H24Cl2N2O5 |
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| Mol. Mass. | 467.342 |
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| SMILES | CO[C@H](C1COC1)c1cc(Cl)c2CCN(Cc3c(OC)cc(C)[nH]c3=O)C(=O)c2c1Cl |r| |
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| Structure | 
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