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Assay Detail

CHEMBL4828452

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

Binding
Displacement of Bak derived peptide from Bcl-2 (unknown origin) measured after 15 mins by microplate reader assay
20
Total Activities
20
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 potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton.
Wang B, Feng W, Wang J, Dong Y, Liu Y, Yao Y, Zhang J, Shi W, Liu L, Zhang H, He X, Chang X, Wang X, Xu H, Liu F, Feng J.
Bioorg Med Chem (2021) 47 : 116350 -116350
PubMed 34536651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.76 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852442 1 9.52
CHEMBL4851332 1 9.30
CHEMBL4851700 1 9.12
CHEMBL4867128 1 9.10
CHEMBL4863897 1 9.07
CHEMBL4860213 1 9.05
CHEMBL3137309 VENETOCLAX 4.0 1 9.00
CHEMBL4878326 1 9.00
CHEMBL4868427 1 8.82
CHEMBL4858527 1 8.78
CHEMBL4861424 1 8.77
CHEMBL4860155 1 8.72
CHEMBL4847514 1 8.62
CHEMBL4858569 1 8.62
CHEMBL4855736 1 8.52
CHEMBL4873467 1 8.42
CHEMBL4855086 1 8.36
CHEMBL4862150 1 8.33
CHEMBL4878411 1 8.08
CHEMBL4866646 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852442 IC50 = 0.3 nM 9.52
CHEMBL4851332 IC50 = 0.5 nM 9.30
CHEMBL4851700 IC50 = 0.75 nM 9.12
CHEMBL4867128 IC50 = 0.8 nM 9.10
CHEMBL4863897 IC50 = 0.86 nM 9.07
CHEMBL4860213 IC50 = 0.89 nM 9.05
CHEMBL3137309 VENETOCLAX IC50 = 1.0 nM 9.00
CHEMBL4878326 IC50 = 1.0 nM 9.00
CHEMBL4868427 IC50 = 1.5 nM 8.82
CHEMBL4858527 IC50 = 1.65 nM 8.78
CHEMBL4861424 IC50 = 1.7 nM 8.77
CHEMBL4860155 IC50 = 1.9 nM 8.72
CHEMBL4847514 IC50 = 2.4 nM 8.62
CHEMBL4858569 IC50 = 2.4 nM 8.62
CHEMBL4855736 IC50 = 3.0 nM 8.52
CHEMBL4873467 IC50 = 3.8 nM 8.42
CHEMBL4855086 IC50 = 4.4 nM 8.36
CHEMBL4862150 IC50 = 4.7 nM 8.33
CHEMBL4878411 IC50 = 8.4 nM 8.08
CHEMBL4866646 IC50 = 9.2 nM 8.04