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TargetHistone-lysine N-methyltransferase EZH2 [A687V]
LigandBDBM190189
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 7.1±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:
BDBM190189
n/a
NameBDBM190189
Synonyms:EPZ007478 | US9175331, 17
TypeSmall organic molecule
Emp. Form.C29H41ClN4O2
Mol. Mass.513.114
SMILESCCN([C@H]1CC[C@@H](CC1)N(C)C1CCC1)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C |r,wU:3.2,wD:6.9,(-6.67,.32,;-5.33,-.45,;-4,.32,;-2.67,-.45,;-1.33,.32,;,-.45,;,-1.99,;-1.33,-2.76,;-2.67,-1.99,;1.33,-2.76,;2.67,-1.99,;1.33,-4.3,;.24,-5.39,;1.33,-6.48,;2.42,-5.39,;-4,1.86,;-5.33,2.63,;-5.33,4.17,;-6.67,4.94,;-4,4.94,;-2.67,4.17,;-1.33,4.94,;-1.33,6.48,;,4.17,;1.33,4.94,;2.67,4.17,;4,4.94,;4,6.48,;5.33,4.17,;5.33,2.63,;6.67,1.86,;4,1.86,;2.67,2.63,;1.33,1.86,;-2.67,2.63,;-1.33,1.86,)|
Structure
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