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TargetHistone-lysine N-methyltransferase EZH2 [A687V]
LigandBDBM190188
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 4±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:
BDBM190188
n/a
NameBDBM190188
Synonyms:EPZ007426 | US9175331, 15
TypeSmall organic molecule
Emp. Form.C28H38N4O2
Mol. Mass.462.6269
SMILESCCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)C#C |r,wU:3.2,wD:6.9,(-5.33,3.47,;-5.33,1.93,;-4,1.15,;-4,-.38,;-2.67,-1.15,;-2.67,-2.69,;-4,-3.47,;-5.33,-2.69,;-5.33,-1.15,;-4,-5,;-2.67,-5.78,;-5.33,-5.78,;-2.67,1.93,;-2.67,3.47,;-1.33,4.23,;,3.47,;,1.93,;1.33,1.15,;2.67,1.93,;1.33,-.38,;2.67,-1.15,;2.67,-2.69,;4,-3.47,;5.33,-2.69,;4,-5,;2.67,-5.78,;2.67,-7.31,;1.33,-5,;1.33,-3.47,;,-2.69,;-1.33,1.15,;-1.33,-.38,;-1.33,5.78,;-1.33,7.31,)|
Structure
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