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Assay Detail

CHEMBL5111871

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of EZH2 (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
Lu D, Wang C, Qu L, Yin F, Li S, Luo H, Zhang Y, Liu X, Chen X, Luo Z, Cui N, Kong L, Wang X.
J Med Chem (2022) 65 : 12838 -12859
PubMed 36153841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.51 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414621 TAZEMETOSTAT 4.0 1 7.70
CHEMBL5176169 1 7.58
CHEMBL4532174 1 7.52
CHEMBL5189365 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414621 TAZEMETOSTAT IC50 = 20.0 nM 7.70
CHEMBL5176169 IC50 = 26.0 nM 7.58
CHEMBL4532174 IC50 = 30.0 nM 7.52
CHEMBL5189365 IC50 = 59.0 nM 7.23