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TargetHistone-lysine N-methyltransferase EZH2 [A687V]
LigandBDBM190186
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 6.8±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 [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:
BDBM190186
n/a
NameBDBM190186
Synonyms:EPZ007209 | US9175331, 12
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)n(C)c2=O)c1C |r,wU:3.2,wD:6.9,(-5.33,4.23,;-5.33,2.69,;-4,1.93,;-4,.38,;-2.67,-.38,;-2.67,-1.93,;-4,-2.69,;-5.33,-1.93,;-5.33,-.38,;-4,-4.23,;-2.67,-5,;-5.33,-5,;-2.67,2.69,;-2.67,4.23,;-1.33,5,;-1.33,6.54,;,4.23,;,2.69,;1.33,1.93,;2.67,2.69,;1.33,.38,;2.67,-.38,;2.67,-1.93,;4,-2.69,;5.33,-1.93,;4,-4.23,;2.67,-5,;2.67,-6.54,;1.33,-4.23,;,-5,;1.33,-2.69,;,-1.93,;-1.33,1.93,;-1.33,.38,)|
Structure
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