Pharos : Ligand Details

Tazemetostat is an inhibitor of the methyltransferase, EZH2, and some EZH2 gain-of-function mutations including Y646X and A687V. Tazemetostat also inhibited EZH1 with a half-maximal inhibitory concentration (IC50) of 392 nM, approximately 36 times higher than the IC50 for inhibition of EZH2

Ligand Summary

Ligand Structure

Synonyms & Links

UNII: Q40W93WPE1

PubChem: 66558664

Guide to Pharmacology: 7011

ChEMBL: CHEMBL3414621

DrugCentral: 5380

LyCHI: ZKMT6LPDYPMY

Target Activities

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EZH2

Tclin

Histone-lysine N-methyltransferase EZH2

15 Activities

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1 – 10 of 15

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
EC50	6.7	J. Med. Chem., (2016) 59:4:1556	26769278

IC50	7.7	Bioorg. Med. Chem. Lett., (2015) 25:17:3644	26189078

IC50	7.89	None, (2015) None:None:None

IC50	7.89	None, (2015) None:None:None

IC50	7.89	None, (2015) None:None:None

IC50	7.89	None, (2016) None:None:None

IC50	7.96	None, (2015) None:None:None

IC50	7.96	None, (2015) None:None:None

IC50	7.96	None, (2016) None:None:None

IC50	8.5	None, (2015) None:None:None

EZH1

Tchem

Histone-lysine N-methyltransferase EZH1

1 Activities

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1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.41	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf