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TargetHistone-lysine N-methyltransferase EZH2 (A677G)
LigandBDBM190199
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 1.5±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:
BDBM190199
n/a
NameBDBM190199
Synonyms:EPZ008286 | US9175331, 29
TypeSmall organic molecule
Emp. Form.C31H42N4O2
Mol. Mass.502.6908
SMILESCCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)C#CC1CC1 |r,wU:3.2,wD:6.9,(-2,5.67,;-3.33,4.9,;-3.33,3.36,;-4.67,2.59,;-4.67,1.05,;-6,.28,;-7.34,1.05,;-7.34,2.59,;-6,3.36,;-8.67,.28,;-10,1.05,;-8.67,-1.26,;-2,2.59,;-2,1.05,;-.67,.28,;.67,1.05,;.67,2.59,;2,3.36,;2,4.9,;3.33,2.59,;4.67,3.36,;6,2.59,;7.34,3.36,;7.34,4.9,;8.67,2.59,;8.67,1.05,;10,.28,;7.34,.28,;6,1.05,;4.67,.28,;-.67,3.36,;-.67,4.9,;-.67,-1.26,;-.67,-2.8,;-.67,-4.34,;-1.44,-5.67,;.1,-5.67,)|
Structure
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