Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 [Y641F] |
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Ligand | BDBM172181 |
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Substrate/Competitor | n/a |
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Meas. Tech. | PRC2 Enzyme Assays |
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IC50 | 1.82±n/a nM |
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Citation | Kuntz, KW; Chesworth, R; Duncan, KW; Keilhack, H; Warholic, N; Klaus, C; Knutson, SK; Wigle, TJ; Seki, M; Shirotori, S; Kawano, S Aryl- or heteroaryl-substituted benzene compounds US Patent US10155002 Publication Date 12/18/2018 |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase EZH2 [Y641F] |
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Name: | Histone-lysine N-methyltransferase EZH2 [Y641F] |
Synonyms: | EZH2 | EZH2(Y641F) | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (Y641F) | KMT6 |
Type: | n/a |
Mol. Mass.: | 85351.84 |
Organism: | Homo sapiens (Human) |
Description: | Q15910[Y641F] |
Residue: | 746 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEFCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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BDBM172181 |
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n/a |
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Name | BDBM172181 |
Synonyms: | US10155002, Compound 189 | US11052093, Compound 189 | US9090562, 189 |
Type | Small organic molecule |
Emp. Form. | C40H57N7O3 |
Mol. Mass. | 683.9257 |
SMILES | CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc(N(CC)C2CCOCC2)c1C)-c1ccc(nc1)N1CCN(CC1)C1CCN(C)CC1 |
Structure |
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