Target
Histone-lysine N-methyltransferase EZH2 [Y641F]
Ligand
BDBM516873
Substrate
n/a
Meas. Tech.
In Vitro Methyltransferase Activity Assay
IC50
7.00±n/a nM
Citation
 Peng, JLiu, YWang, LFang, ZFei, ZChen, XLan, J 4,5,6-trisubstituted indazole derivatives, and preparation method and pharmaceutical use thereof US Patent  US11104664 Publication Date 8/31/2021 
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:
BDBM516873
Synonyms:
US11104664, Compound P-47
Type:
Small organic molecule
Emp. Form.:
C24H36N4O3
Mol. Mass.:
428.5676
SMILES:
CCN(C1CCC(CC1)N1CC(C1)OC)c1c(CC)c(cc2n(C)ncc12)C(=O)OC |(6.6,-3.33,;5.27,-2.56,;3.93,-3.33,;3.93,-4.87,;2.6,-5.64,;2.6,-7.18,;3.93,-7.95,;5.27,-7.18,;5.27,-5.64,;3.93,-9.49,;2.84,-10.58,;3.93,-11.67,;5.02,-10.58,;3.93,-13.21,;2.6,-13.98,;2.6,-2.56,;2.6,-1.02,;3.93,-.25,;5.27,-1.02,;1.27,-.25,;-.07,-1.02,;-.07,-2.56,;-1.21,-3.59,;-2.72,-3.27,;-.59,-5,;.94,-4.84,;1.27,-3.33,;1.27,1.29,;-.07,2.06,;2.6,2.06,;3.93,1.29,)|
Structure:
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