Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 [Y641F] |
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Ligand | BDBM190184 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Inhibition Assay |
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IC50 | 3.4±n/a nM |
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Citation | Kuntz, KW; Knutson, SK; Wigle, TJ Inhibitors of human EZH2, and methods of use thereof US Patent US9175331 Publication Date 11/3/2015 |
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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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BDBM190184 |
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n/a |
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Name | BDBM190184 |
Synonyms: | EPZ006632 | US9175331, 10 |
Type | Small organic molecule |
Emp. Form. | C36H48N5O3 |
Mol. Mass. | 598.798 |
SMILES | CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)nc2=O)c1C)-c1ccc(CN2CCCN(C)CC2)cc1 |
Structure |
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