Target
Histone-lysine N-methyltransferase EZH2 [A677G]
Ligand
BDBM190205
Substrate
n/a
Meas. Tech.
Inhibition Assay
IC50
12.7±n/a nM
Citation
 Kuntz, KWKnutson, SKWigle, TJ Inhibitors of human EZH2, and methods of use thereof US Patent  US9175331 Publication Date 11/3/2015
Target
Name:
Histone-lysine N-methyltransferase EZH2 [A677G]
Synonyms:
EZH2 | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (A677G) | KMT6
Type:
Protein
Mol. Mass.:
85381.87
Organism:
Homo sapiens (Human)
Description:
Q15910[A677G]
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDGTRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM190205
Synonyms:
EPZ008493 | US9175331, 36
Type:
Small organic molecule
Emp. Form.:
C22H31N3O3
Mol. Mass.:
385.4998
SMILES:
CCN(CCCOC)c1cccc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C
Structure:
Search PDB for entries with ligand similarity: