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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM50246963
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
17.0±n/a nM
Citation
 Collins, MR; Kania, RS; Kumpf, RA; Kung, P; Richter, DT; Sutton, SC; Wythes, MJ Substituted dihydroisoquinolinone compounds US Patent  US10570121 Publication Date 2/25/2020 
Target
Name:
Histone-lysine N-methyltransferase EZH2
Synonyms:
Enhancer of zeste homolog 2 (EZH2) | ENX-1 | Lysine N-methyltransferase 6 | EZH2_HUMAN | EZH2 | KMT6 | Histone-lysine N-methyltransferase EZH2
Type:
Protein
Mol. Mass.:
85367.84
Organism:
Human
Description:
Q15910
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM50246963
Synonyms:
CHEMBL4072040 | US10570121, Example 30
Type:
Small organic molecule
Emp. Form.:
C21H24Cl2N2O3
Mol. Mass.:
422.12
SMILES:
CCC(CO)c1cc(Cl)c2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl
Structure:
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