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Target
Histone-lysine N-methyltransferase EZH2 [A687V]
Ligand
BDBM190215
Substrate
n/a
Meas. Tech.
Inhibition Assay
IC50
22.7±n/a nM
Citation
 Kuntz, KW; Knutson, SK; Wigle, TJ Inhibitors of human EZH2, and methods of use thereof US Patent  US9175331 Publication Date 11/3/2015 
Target
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:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM190215
Synonyms:
EPZ009090 | US9175331, 51
Type:
Small organic molecule
Emp. Form.:
C27H38ClN3O2
Mol. Mass.:
472.063
SMILES:
CCN(C1CCC(CC1)C(C)C)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C |(-5.33,4.23,;-5.33,2.69,;-4,1.93,;-4,.38,;-5.33,-.38,;-5.33,-1.93,;-4,-2.69,;-2.67,-1.93,;-2.67,-.38,;-4,-4.23,;-5.33,-5,;-2.67,-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,;1.33,-2.69,;,-1.93,;-1.33,1.93,;-1.33,.38,)|
Structure:
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