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Assay Detail

CHEMBL4735331

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

Binding
Inhibition of human full length N-terminal Flag tagged EZH2 Y641F mutant using dimethylated H3K27 as the substrate incubated for 120 mins by quadrupole mass spectrometry coupled UFLC analysis
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

Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
Martin MC,Zeng G,Yu J,Schiltz GE
J Med Chem (2020) 63 : 15344 -15370
PubMed 33283516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.89 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414574 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414574 IC50 = 13.0 nM 7.89