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Assay Detail

CHEMBL5228433

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

Binding
Binding affinity to his tagged EED (1 to 441 residues) (unknown origin) incubated for 20 mins in presence of biotinylated H3K27me3 peptide (19 to 33 residues) by alphascreen competitive binding assay
7
Total Activities
7
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

Polycomb protein EED (CHEMBL2189117)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Polycomb Repressive Complex 2 Modulation through the Development of EZH2-EED Interaction Inhibitors and EED Binders.
Tomassi S, Romanelli A, Zwergel C, Valente S, Mai A.
J Med Chem (2021) 64 : 11774 -11797
PubMed 34351144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.42 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5268403 1 8.35
CHEMBL4755618 1 8.23
CHEMBL5283723 1 6.50
CHEMBL4097892 1 6.05
CHEMBL4074159 1 5.80
CHEMBL5282599 1 5.06
CHEMBL5269781 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5268403 IC50 = 4.5 nM 8.35
CHEMBL4755618 IC50 = 5.9 nM 8.23
CHEMBL5283723 IC50 = 320.0 nM 6.50
CHEMBL4097892 IC50 = 890.0 nM 6.05
CHEMBL4074159 IC50 = 1570.0 nM 5.80
CHEMBL5282599 IC50 = 8760.0 nM 5.06
CHEMBL5269781 IC50 = 11580.0 nM 4.94