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Assay Detail

CHEMBL888453

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

Binding
Displacement of FAM-Bim peptide from human Bcl2 by fluorescence polarization assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
Tang G, Ding K, Ding K, Nikolovska-Coleska Z, Yang CY, Qiu S, Shangary S, Wang R, Guo J, Gao W, Meagher J, Stuckey J, Krajewski K, Jiang S, Roller PP, Wang S.
J Med Chem (2007) 50 : 3163 -3166
PubMed 17552510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.79 7.77
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226578 1 7.77
CHEMBL51483 GOSSYPOL 3.0 1 6.77
CHEMBL389660 1 6.47
CHEMBL226678 1 6.14
CHEMBL226679 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226578 Ki = 17.0 nM 7.77
CHEMBL51483 GOSSYPOL Ki = 170.0 nM 6.77
CHEMBL389660 Ki = 340.0 nM 6.47
CHEMBL226678 Ki = 730.0 nM 6.14
CHEMBL226679 Activity - -