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TargetHistone-lysine N-methyltransferase EZH2 (A677G)
LigandBDBM172176
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 0.8±n/a nM
Citation Kuntz KWKnutson SKWigle TJ Inhibitors of human EZH2, and methods of use thereof US Patent  US9175331 Publication Date 11/3/2015
More Info.:Get all data from this article,  Assay Method
 
Histone-lysine N-methyltransferase EZH2 (A677G)
Name:Histone-lysine N-methyltransferase EZH2 (A677G)
Synonyms:n/a
Type:Protein
Mol. Mass.:85381.87
Organism:Homo sapiens (Human)
Description:Q15910
Residue:746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDGTRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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  Blast E-value cutoff:
BDBM172176
n/a
NameBDBM172176
Synonyms:EPZ009161 | US10155002, Compound 184 | US9090562, 184 | US9175331, 61
TypeSmall organic molecule
Emp. Form.C34H46N6O3
Mol. Mass.586.7674
SMILESCCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc(N(CC)C2CCOCC2)c1C)-c1ccc(nc1)N1CCNCC1
Structure
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