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TargetHistone-lysine N-methyltransferase EZH2 (A677G)
LigandBDBM190201
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 1.3±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:
BDBM190201
n/a
NameBDBM190201
Synonyms:EPZ008336 | US9175331, 31
TypeSmall organic molecule
Emp. Form.C27H39ClN4O2
Mol. Mass.487.077
SMILESCCN([C@@H]1CC[C@@H](CC1)N(C)C)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1CC |r,wD:3.2,6.9,(-5.33,.77,;-5.33,-.77,;-4,-1.54,;-4,-3.08,;-2.67,-3.85,;-2.67,-5.39,;-4,-6.16,;-5.33,-5.39,;-5.33,-3.85,;-4,-7.7,;-2.67,-8.47,;-5.33,-8.47,;-2.67,-.77,;-1.33,-1.54,;,-.77,;1.33,-1.54,;,.77,;-1.33,1.54,;-1.33,3.08,;-2.67,3.85,;,3.85,;,5.39,;1.33,6.16,;1.33,7.7,;,8.47,;2.67,8.47,;4,7.7,;5.33,8.47,;4,6.16,;2.67,5.39,;2.67,3.85,;-2.67,.77,;-4,1.54,;-4,3.08,)|
Structure
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