Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM378893
Substrate
n/a
Meas. Tech.
EZH2 enzymatic activity
IC50
<0.500±n/a nM
Citation
 Marx, MALee, MRGalemmo, RABobinski, TP EZH2 inhibitors US Patent  US10266542 Publication Date 4/23/2019 
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:
BDBM378893
Synonyms:
5,8-dichloro-2-((7-methyl-5-oxo-5,6-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)methyl)-7-(7-oxa-2-azaspiro[3.5]nonan-2-yl)-3,4-dihydroisoquinolin-1(2H)-one | US10266542, Example 5
Type:
Small organic molecule
Emp. Form.:
C25H28Cl2N4O3
Mol. Mass.:
503.421
SMILES:
Cc1[nH]c(=O)c(CN2CCc3c(Cl)cc(N4CC5(C4)CCOCC5)c(Cl)c3C2=O)c2CCNc12
Structure:
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