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TargetHistone-lysine N-methyltransferase EZH2 [A687V]
LigandBDBM190222
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 43.6±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:
BDBM190222
n/a
NameBDBM190222
Synonyms:EPZ009157 | US9175331, 59
TypeSmall organic molecule
Emp. Form.C29H39ClN4O3
Mol. Mass.527.098
SMILESCCN([C@H]1CC[C@H](CC1)C(=O)N1CCCC1)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C |r,wU:3.2,6.9,(-2.67,-3.05,;-1.33,-3.82,;,-3.05,;1.33,-3.82,;2.67,-3.05,;4,-3.82,;4,-5.36,;2.67,-6.13,;1.33,-5.36,;5.33,-6.13,;6.67,-5.36,;5.33,-7.67,;4.09,-8.58,;4.56,-10.04,;6.1,-10.04,;6.58,-8.58,;,-1.51,;1.33,-.74,;1.33,.8,;2.67,1.57,;,1.57,;-1.33,.8,;-2.67,1.57,;-4,.8,;-2.67,3.11,;-4,3.88,;-4,5.42,;-5.33,6.19,;-6.67,5.42,;-5.33,7.73,;-4,8.5,;-4,10.04,;-2.67,7.73,;-2.67,6.19,;-1.33,5.42,;-1.33,-.74,;-2.67,-1.51,)|
Structure
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