Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 |
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Ligand | BDBM335716 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Histone Methyl Transferase Assay |
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EC50 | <5000±n/a nM |
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Citation | Kim, KS; Zhang, L; Purandare, AV; Seitz, SP Inhibitors of lysine methyl transferase US Patent US9738630 Publication Date 8/22/2017 |
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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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BDBM335716 |
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n/a |
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Name | BDBM335716 |
Synonyms: | N-((6,8-Difluoro-1-methyl-3-oxo- 2,3-dihydroisoquinolin-4- yl)methyl)-5-(ethyl(tetrahydro- 2H-pyran-4-yl)amino)-4-methyl- 4'-(morpholinomethyl)-[1,1'- biphenyl]-3-carboxamide | US9738630, Example 11 |
Type | Small organic molecule |
Emp. Form. | C37H42F2N4O4 |
Mol. Mass. | 644.7506 |
SMILES | CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c3cc(F)cc(F)c3c(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1 |
Structure |
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