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Target
Histone-lysine N-methyltransferase EZH2 [Y641F]
Ligand
BDBM458816
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
0.300±n/a nM
Citation
 Lu, B; Shen, X; He, M; Liu, D; Zhang, M Benzofuran derivative, preparation method thereof and use thereof in medicine US Patent  US10759787 Publication Date 9/1/2020 
Target
Name:
Histone-lysine N-methyltransferase EZH2 [Y641F]
Synonyms:
EZH2 | EZH2(Y641F) | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (Y641F) | KMT6
Type:
n/a
Mol. Mass.:
85351.84
Organism:
Homo sapiens (Human)
Description:
Q15910[Y641F]
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEFCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM458816
Synonyms:
N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-methyl-6-(methyl(tetrahydro-2H-pyran-4-yl)amino)benzofuran-4-carboxamide | US10759787, Example 23 | US11059811, Example 23
Type:
Small organic molecule
Emp. Form.:
C24H29N3O5
Mol. Mass.:
439.5042
SMILES:
COc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)c(cc2occc12)N(C)C1CCOCC1
Structure:
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