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Assay Detail

CHEMBL1031850

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

Binding
Displacement of F-BakBH3 from Bcl-xL by fluorescence polarization assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Bcl-2-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Wei J, Kitada S, Rega MF, Stebbins JL, Zhai D, Cellitti J, Yuan H, Emdadi A, Dahl R, Zhang Z, Yang L, Reed JC, Pellecchia M.
J Med Chem (2009) 52 : 4511 -4523
PubMed 19555126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.90 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539481 1 6.57
CHEMBL538616 1 6.12
CHEMBL552287 1 6.10
CHEMBL554545 1 6.10
CHEMBL541427 1 6.07
CHEMBL541496 1 6.03
CHEMBL541004 1 5.96
CHEMBL552735 1 5.46
CHEMBL551288 APOGOSSYPOL 1 5.43
CHEMBL553474 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539481 IC50 = 270.0 nM 6.57
CHEMBL538616 IC50 = 760.0 nM 6.12
CHEMBL552287 IC50 = 800.0 nM 6.10
CHEMBL554545 IC50 = 800.0 nM 6.10
CHEMBL541427 IC50 = 850.0 nM 6.07
CHEMBL541496 IC50 = 930.0 nM 6.03
CHEMBL541004 IC50 = 1100.0 nM 5.96
CHEMBL552735 IC50 = 3500.0 nM 5.46
CHEMBL551288 APOGOSSYPOL IC50 = 3700.0 nM 5.43
CHEMBL553474 IC50 = 6300.0 nM 5.20