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TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM50562994
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2081276 (CHEMBL4737067)
Ki 2.0±n/a nM
Citation Kung, PPFan, CGukasyan, HJHuang, BKephart, SKraus, MLee, JHSutton, SCYamazaki, SZehnder, L Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug. J Med Chem64:1725-1732 (2021) [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:
BDBM50562994
n/a
NameBDBM50562994
Synonyms:CHEMBL4740532
TypeSmall organic molecule
Emp. Form.C21H21BrClN5O2
Mol. Mass.490.781
SMILESCc1nnn(C)c1-c1cc(Br)c2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl |(30.21,-10.38,;29.89,-11.89,;30.92,-13.04,;30.16,-14.37,;28.65,-14.05,;27.51,-15.09,;28.48,-12.52,;27.14,-11.76,;25.8,-12.53,;24.47,-11.76,;23.14,-12.52,;24.48,-10.22,;23.14,-9.45,;23.14,-7.92,;24.48,-7.16,;24.48,-5.61,;23.14,-4.84,;23.14,-3.29,;24.47,-2.52,;21.8,-2.53,;20.47,-3.3,;19.13,-2.53,;20.47,-4.84,;21.8,-5.62,;21.8,-7.16,;25.82,-7.91,;27.15,-7.14,;25.81,-9.45,;27.14,-10.22,;28.46,-9.45,)|
Structure
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