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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM326120
Substrate
n/a
Meas. Tech.
Wild-Type PRC2 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  US10273223 Publication Date 4/30/2019 
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:
BDBM326120
Synonyms:
US10273223, Compound D-18 | US9637472, Compound D-18
Type:
Small organic molecule
Emp. Form.:
C31H41N7O3
Mol. Mass.:
559.7023
SMILES:
Cc1cc(C)c(CNC(=O)c2cc(cc3n(ncc23)C2CCCC2)N2CCN(CC2)C(=O)C2CCNCC2)c(=O)[nH]1
Structure:
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