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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM325938
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
<300±n/a nM
Citation
 Kuntz, KW; Olhava, EJ; Chesworth, R; Duncan, KW Substituted 6,5-fused bicyclic heteroaryl compounds US Patent  US9637472 Publication Date 5/2/2017 
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:
BDBM325938
Synonyms:
US10273223, Compound B-32 | US9637472, Compound B-32
Type:
Small organic molecule
Emp. Form.:
C30H39N7O3
Mol. Mass.:
545.6758
SMILES:
CC(C)n1ncc2c(cc(nc12)C1=CCN(CC1)C(=O)C1CCCN(C)C1)C(=O)NCc1c(C)cc(C)[nH]c1=O |t:14|
Structure:
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