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Assay Detail

CHEMBL3271463

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

Binding
Inhibition of EZH2 in human KARPAS422 cells assessed as global reduction in H3K27me3 level after 4 days by ELISA-based assay
1
Total Activities
1
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

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
Nasveschuk CG, Gagnon A, Garapaty-Rao S, Balasubramanian S, Campbell R, Lee C, Zhao F, Bergeron L, Cummings R, Trojer P, Audia JE, Albrecht BK, Harmange JC.
ACS Med Chem Lett (2014) 5 : 378 -383
PubMed 24900844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.23 4.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3264787 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3264787 IC50 = 58300.0 nM 4.23