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TargetHistone-lysine N-methyltransferase EZH2 [A687V]
LigandBDBM190195
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 6.5±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 [A687V]
Name:Histone-lysine N-methyltransferase EZH2 [A687V]
Synonyms:EZH2 | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (A687V) | KMT6
Type:Protein
Mol. Mass.:85395.90
Organism:Homo sapiens (Human)
Description:Q15910[A687V]
Residue:746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM190195
n/a
NameBDBM190195
Synonyms:EPZ007790 | US9175331, 23
TypeSmall organic molecule
Emp. Form.C29H44N4O2
Mol. Mass.480.6853
SMILESCCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)C(C)C |r,wU:3.2,wD:6.9,(-5.33,3.85,;-5.33,2.31,;-4,1.54,;-4,,;-2.67,-.77,;-2.67,-2.31,;-4,-3.08,;-5.33,-2.31,;-5.33,-.77,;-4,-4.62,;-2.67,-5.39,;-5.33,-5.39,;-2.67,2.31,;-2.67,3.85,;-1.33,4.62,;,3.85,;,2.31,;1.33,1.54,;2.67,2.31,;1.33,,;2.67,-.77,;2.67,-2.31,;4,-3.08,;5.33,-2.31,;4,-4.62,;2.67,-5.39,;2.67,-6.93,;1.33,-4.62,;1.33,-3.08,;,-2.31,;-1.33,1.54,;-1.33,,;-1.33,6.16,;-2.67,6.93,;,6.93,)|
Structure
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