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Target
Histone-lysine N-methyltransferase EZH2 [2-746,Y641N]
Ligand
BDBM435640
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
3.50±n/a nM
Citation
 Collins, MR; Kania, RS; Kumpf, RA; Kung, P; Richter, DT; Sutton, SC; Wythes, MJ Substituted dihydroisoquinolinone compounds US Patent  US10570121 Publication Date 2/25/2020 
Target
Name:
Histone-lysine N-methyltransferase EZH2 [2-746,Y641N]
Synonyms:
EZH2 | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (Y641N) | KMT6
Type:
Enzyme Catalytic Domain
Mol. Mass.:
85187.58
Organism:
Homo sapiens (Human)
Description:
Q15910 Y641N
Residue:
745
Sequence:
GQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISENCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM435640
Synonyms:
US10570121, Example 146 | US10570121, Example 147
Type:
Small organic molecule
Emp. Form.:
C25H31BrClN3O3
Mol. Mass.:
536.889
SMILES:
COC(C1CCN(C)CC1)c1cc(Br)c2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl
Structure:
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