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Target
Histone-lysine N-methyltransferase EZH2 [A677G]
Ligand
BDBM190196
Substrate
n/a
Meas. Tech.
Inhibition Assay
IC50
2.3±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 [A677G]
Synonyms:
EZH2 | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (A677G) | KMT6
Type:
Protein
Mol. Mass.:
85381.87
Organism:
Homo sapiens (Human)
Description:
Q15910[A677G]
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDGTRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM190196
Synonyms:
EPZ008277 | US9175331, 25
Type:
Small organic molecule
Emp. Form.:
C31H38N6O2
Mol. Mass.:
526.6724
SMILES:
CC(C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCN(C)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
Structure:
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