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Assay Detail

CHEMBL3877071

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

Binding
Inhibition of FITC-betaA-DIIRNIARHLAQVGDSMRSI-NH2 binding to recombinant human Bcl2A1 (1 to 152 residues) BH3 binding site expressed in Escherichia coli measured after 2 hrs by fluorescence polarization assay
4
Total Activities
2
Compounds Tested
2
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

Electrophilic Helical Peptides That Bond Covalently, Irreversibly, and Selectively in a Protein-Protein Interaction Site.
de Araujo AD, Lim J, Good AC, Skerlj RT, Fairlie DP.
ACS Med Chem Lett (2017) 8 : 22 -26
PubMed 28105269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.50 7.50
IC50 2 7.52 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3883565 2 8.07
CHEMBL3884841 2 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3883565 IC50 = 8.5 nM 8.07
CHEMBL3884841 Ki = 32.0 nM 7.50
CHEMBL3884841 IC50 = 110.0 nM 6.96
CHEMBL3883565 Ki < 0.1 nM -