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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM172038
Substrate
n/a
Meas. Tech.
ChEMBL_2079561 (CHEMBL4735352)
IC50
4.0±n/a nM
Citation
 Martin, MC; Zeng, G; Yu, J; Schiltz, GE Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer. J Med Chem 63:15344-15370 (2020) [PubMed]  Article 
Target
Name:
Histone-lysine N-methyltransferase EZH2
Synonyms:
2.1.1.356 | Ezh2 | Histone-lysine N-methyltransferase EZH2 | Synonyms=LOC312299
Type:
PROTEIN
Mol. Mass.:
85254.24
Organism:
Rattus norvegicus
Description:
ChEMBL_120176
Residue:
746
Sequence:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKTMFSSNRQKILERTETLNQEWKQRRIQPVHIMTSVSSLRGTRECSVTSDLDFPAQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPDEREEKQKDLDDSRDDKETCPPRKFPADKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTISVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPVPTEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
  
Inhibitor
Name:
BDBM172038
Synonyms:
US10155002, Compound 44 | US10647700, Compound EPZ6438 | US11052093, Compound 143 | US11535629, Compound Control A | US9090562, 143 | US9090562, 44 | US9394283, 1
Type:
Small organic molecule
Emp. Form.:
C34H44N4O4
Mol. Mass.:
572.7376
SMILES:
CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1
Structure:
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