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Target
Histone-lysine N-methyltransferase EZH1
Ligand
BDBM50075071
Substrate
n/a
Meas. Tech.
ChEMBL_1933811 (CHEMBL4479463)
IC50
69±n/a nM
Citation
 Yang, X; Li, F; Konze, KD; Meslamani, J; Ma, A; Brown, PJ; Zhou, MM; Arrowsmith, CH; Kaniskan, HÜ; Vedadi, M; Jin, J Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors. J Med Chem 59:7617-33 (2016) [PubMed]  Article 
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:
BDBM50075071
Synonyms:
CHEMBL3414619
Type:
Small organic molecule
Emp. Form.:
C33H43N7O2
Mol. Mass.:
569.7402
SMILES:
CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccc(nc1)N1CCN(CC1)C(C)C
Structure:
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