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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM50205628
Substrate
n/a
Meas. Tech.
ChEMBL_1628509 (CHEMBL3871094)
IC50
88±n/a nM
Citation
 Ansari, A; Satalkar, S; Patil, V; Shete, AS; Kaur, S; Gupta, A; Singh, S; Raja, M; Severance, DL; Bernales, S; Chakravarty, S; Hung, DT; Pham, SM; Herrera, FJ; Rai, R Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR. Bioorg Med Chem Lett 27:217-222 (2017) [PubMed]  Article 
Target
Name:
Histone-lysine N-methyltransferase EZH2
Synonyms:
ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6
Type:
Protein
Mol. Mass.:
85367.84
Organism:
Homo sapiens (Human)
Description:
Q15910
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM50205628
Synonyms:
CHEMBL3906288
Type:
Small organic molecule
Emp. Form.:
C22H26N4O2
Mol. Mass.:
378.4674
SMILES:
CC(C)N1CC(C)c2c1cc(cc2C(=O)NCc1c(C)cc(C)[nH]c1=O)C#N
Structure:
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