tazemetostat
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
UNII: Q40W93WPE1
PubChem: 66558664
Guide to Pharmacology: 7011
ChEMBL: CHEMBL3414621
DrugCentral: 5380
LyCHI: ZKMT6LPDYPMY
Target Activities
EZH2
Histone-lysine N-methyltransferase EZH2
14 Activities
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1 – 10 of 14
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.96 | |||||
IC50 | 9.47 | Bioorg Med Chem Lett, (2020) 30:5:126957 | ||||
IC50 | 9 | Bioorg. Med. Chem. Lett., (2015) 25:17:3644 | ||||
IC50 | 9 | Bioorg. Med. Chem. Lett., (2015) 25:17:3644 | ||||
Ki | 8.6 | J. Med. Chem., (2015) 58:4:1596 | ||||
IC50 | 8.5 | None, (2015) None:None:None | ||||
IC50 | 7.96 | None, (2015) None:None:None | ||||
IC50 | 7.96 | None, (2016) None:None:None | ||||
IC50 | 7.89 | None, (2015) None:None:None | ||||
IC50 | 7.89 | None, (2015) None:None:None | ||||
EED
Polycomb protein EED
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.7 | J Med Chem, (2017) 60:6:2215 | ||||
IC50 | 7.4 | J Med Chem, (2017) 60:6:2215 | ||||
IC50 | 8.7 | |||||
EZH1
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 | ||||