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Assay Detail

CHEMBL4619130

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

Binding
Inhibition FITC-labeled BCoR peptide binding to wild type human BCL6 BTB domain (5 to 129 residues) expressed in baculovirus infected Sf9 cells after 30 mins by TR-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

B-cell lymphoma 6 protein (CHEMBL4105786)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.
Teng M, Ficarro SB, Yoon H, Che J, Zhou J, Fischer ES, Marto JA, Zhang T, Gray NS.
ACS Med Chem Lett (2020) 11 : 1269 -1273
PubMed 32551010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.36 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4646073 1 6.82
CHEMBL4640734 1 6.60
CHEMBL4644523 1 6.43
CHEMBL4077392 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4646073 IC50 = 152.0 nM 6.82
CHEMBL4640734 IC50 = 251.0 nM 6.60
CHEMBL4644523 IC50 = 368.0 nM 6.43
CHEMBL4077392 IC50 = 2699.0 nM 5.57