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Assay Detail

CHEMBL2173039

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

Binding
Inhibition of GST-tagged recombinant Bcl2 interaction with biotinylated Bim peptide by ELISA based competitive binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.
Saugues E, Debaud AL, Anizon F, Bonnefoy N, Moreau P.
Eur J Med Chem (2012) 57 : 112 -125
PubMed 23047228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.60 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408194 OBATOCLAX 3.0 1 6.52
CHEMBL2171509 1 5.85
CHEMBL2171489 1 5.57
CHEMBL2171488 1 5.46
CHEMBL2171506 1 5.18
CHEMBL2171491 1 5.04
CHEMBL555017 GAMBOGIC ACID 1 -
CHEMBL376408 ABT 737 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408194 OBATOCLAX EC50 = 300.0 nM 6.52
CHEMBL2171509 EC50 = 1400.0 nM 5.85
CHEMBL2171489 EC50 = 2700.0 nM 5.57
CHEMBL2171488 EC50 = 3500.0 nM 5.46
CHEMBL2171506 EC50 = 6600.0 nM 5.18
CHEMBL2171491 EC50 = 9200.0 nM 5.04
CHEMBL555017 GAMBOGIC ACID EC50 - -
CHEMBL376408 ABT 737 EC50 < 30.0 nM -