Target
Histone-lysine N-methyltransferase EZH1
Ligand
BDBM588042
Substrate
n/a
Meas. Tech.
Inhibitory Activity Assay
IC50
12.0±n/a nM
Citation
 Jung, SHHong, DJHwang, JYKim, SHPark, SMMah, SMAhn, YG Dioxoloisoquinolinone derivatives and use thereof US Patent  US11535629 Publication Date 12/27/2022 
Target
Name:
Histone-lysine N-methyltransferase EZH1
Synonyms:
ENX-2 | EZH1 | EZH1_HUMAN | Enhancer of zeste homolog 1 | Enhancer of zeste homolog 1 (EZH1) | Histone-lysine N-methyltransferase EZH1 | KIAA0388
Type:
Protein
Mol. Mass.:
85285.34
Organism:
Homo sapiens (Human)
Description:
Q92800
Residue:
747
Sequence:
MEIPNPPTSKCITYWKRKVKSEYMRLRQLKRLQANMGAKALYVANFAKVQEKTQILNEEWKKLRVQPVQSMKPVSGHPFLKKCTIESIFPGFASQHMLMRSLNTVALVPIMYSWSPLQQNFMVEDETVLCNIPYMGDEVKEEDETFIEELINNYDGKVHGEEEMIPGSVLISDAVFLELVDALNQYSDEEEEGHNDTSDGKQDDSKEDLPVTRKRKRHAIEGNKKSSKKQFPNDMIFSAIASMFPENGVPDDMKERYRELTEMSDPNALPPQCTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNVYKRKNKEIKIEPEPCGTDCFLLLEGAKEYAMLHNPRSKCSGRRRRRHHIVSASCSNASASAVAETKEGDSDRDTGNDWASSSSEANSRCQTPTKQKASPAPPQLCVVEAPSEPVEWTGAEESLFRVFHGTYFNNFCSIARLLGTKTCKQVFQFAVKESLILKLPTDELMNPSQKKKRKHRLWAAHCRKIQLKKDNSSTQVYNYQPCDHPDRPCDSTCPCIMTQNFCEKFCQCNPDCQNRFPGCRCKTQCNTKQCPCYLAVRECDPDLCLTCGASEHWDCKVVSCKNCSIQRGLKKHLLLAPSDVAGWGTFIKESVQKNEFISEYCGELISQDEADRRGKVYDKYMSSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVVMVNGDHRIGIFAKRAIQAGEELFFDYRYSQADALKYVGIERETDVL
  
Inhibitor
Name:
BDBM588042
Synonyms:
6-((4,6-dimethyl-2-oxo-1,2- dihydropyridin-3-yl)methyl)-2-(4- (dimethylamino)bicyclo[2.2.2]octan- 1-yl)-2,4,9-trimethyl-7,8-dihydro- [1,3]dioxolo[4,5-g]isoquinolin- 5(6H)-one isomer A | US11535629, Compound 23
Type:
Small organic molecule
Emp. Form.:
C31H41N3O4
Mol. Mass.:
519.6749
SMILES:
CN(C)C12CCC(CC1)(CC2)C1(C)Oc2c(O1)c(C)c1C(=O)N(Cc3c(C)cc(C)[nH]c3=O)CCc1c2C
Structure:
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