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Assay Detail

CHEMBL5586931

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

Binding
Binding affinity to Bcl-2 (unknown origin) pre-incubated for 30 mins followed by addition FAM-peptide further incubated for 20 mins by fluorescence polarization-based binding assay
7
Total Activities
7
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

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

Publication

Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1<i>H</i>-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.
Deng H, Zhang J, Liu L, Zhang H, Han Y, Wu L, Jing Y, Huang M, Zhao L.
J Med Chem (2024) 67 : 13925 -13958
PubMed 39121336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.80 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555017 GAMBOGIC ACID 1 6.80
CHEMBL5598253 1 -
CHEMBL5598470 1 -
CHEMBL5597184 1 -
CHEMBL5596340 1 -
CHEMBL3417704 1 -
CHEMBL3137309 VENETOCLAX 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555017 GAMBOGIC ACID IC50 = 160.0 nM 6.80
CHEMBL5598253 IC50 > 100000.0 nM -
CHEMBL5598470 IC50 > 100000.0 nM -
CHEMBL5597184 IC50 > 100000.0 nM -
CHEMBL5596340 IC50 > 100000.0 nM -
CHEMBL3417704 IC50 > 100000.0 nM -
CHEMBL3137309 VENETOCLAX IC50 > 100000.0 nM -