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TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM50075051
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2224729 (CHEMBL5138242)
IC50 54±n/a nM
Citation Talukdar, AMukherjee, ABhattacharya, D Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues. J Med Chem65:1662-1684 (2022) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histone-lysine N-methyltransferase EZH2
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:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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  Blast E-value cutoff:
BDBM50075051
n/a
NameBDBM50075051
Synonyms:CHEMBL3360855 | EPZ005687 | US10273223, Compound C-1 | US9175331, 7 | US9637472, Compound C-1
TypeSmall organic molecule
Emp. Form.C32H37N5O3
Mol. Mass.539.6679
SMILESCc1cc(C)c(CNC(=O)c2cc(cc3n(ncc23)C2CCCC2)-c2ccc(CN3CCOCC3)cc2)c(=O)[nH]1
Structure
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