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Assay Detail

CHEMBL5163776

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

Binding
Displacement of fluorescent-labeled BID-BH3 peptide from His-tagged human BFL-1 (1 to 151 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant by fluorescence polarization-based competitive binding assay
3
Total Activities
3
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

Bcl-2-related protein A1 (CHEMBL6044)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Feng X, Yan Z, Zhou F, Lou J, Lyu X, Ren X, Zeng Z, Liu C, Zhang S, Zhu D, Huang H, Yang J, Zhao Y.
Eur J Med Chem (2022) 236 : 114327 -114327
PubMed 35385805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.31 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576854 1 7.00
CHEMBL1271764 1 6.40
CHEMBL5189912 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576854 Ki = 100.0 nM 7.00
CHEMBL1271764 Ki = 400.0 nM 6.40
CHEMBL5189912 Ki = 2900.0 nM 5.54