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TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM190211
Substrate/Competitorn/a
Meas. Tech.Inhibition Assay
IC50 6.1±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
Name:Histone-lysine N-methyltransferase EZH2
Synonyms:ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6
Type:Protein
Mol. Mass.:85367.84
Organism:Homo sapiens (Human)
Description:Q15910
Residue:746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM190211
n/a
NameBDBM190211
Synonyms:EPZ008990 | US9175331, 47
TypeSmall organic molecule
Emp. Form.C28H39ClN4O3
Mol. Mass.515.087
SMILESCCN([C@H]1CC[C@@H](CC1)N(C)C1COC1)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C |r,wU:3.2,wD:6.9,(-2.67,-3.15,;-1.33,-3.92,;,-3.15,;1.33,-3.92,;2.67,-3.15,;4,-3.92,;4,-5.46,;2.67,-6.23,;1.33,-5.46,;5.33,-6.23,;6.67,-5.46,;5.33,-7.77,;4.25,-8.85,;5.33,-9.94,;6.42,-8.85,;,-1.61,;1.33,-.84,;1.33,.7,;2.67,1.47,;,1.47,;-1.33,.7,;-2.67,1.47,;-4,.7,;-2.67,3.01,;-4,3.78,;-4,5.32,;-5.33,6.09,;-6.67,5.32,;-5.33,7.63,;-4,8.4,;-4,9.94,;-2.67,7.63,;-2.67,6.09,;-1.33,5.32,;-1.33,-.84,;-2.67,-1.61,)|
Structure
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