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Assay Detail

CHEMBL5611693

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Binding
Inhibition of Bfl-1 in human SU-DHL-1 cells assessed as caspase-3/7 activation measured after 6 hrs by UPLC-MRM MS analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SU-DHL-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bcl-2-related protein A1 (CHEMBL6044)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
Lucas SCC, Blackwell JH, Börjesson U, Hargreaves D, Milbradt AG, Bostock MJ, Ahmed S, Beaumont K, Cheung T, Demanze S, Gohlke A, Guerot C, Haider A, Kantae V, Kauffman GW, Kinzel O, Kupcova L, Lainchbury MD, Lamb ML, Leon L, Palisse A, Sacchetto C, Storer RI, Su N, Thomson C, Vales J, Chen Y, Hu X.
J Med Chem (2024) 67 : 16455 -16479
PubMed 39291659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.53 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5613766 1 6.43
CHEMBL5613621 1 5.80
CHEMBL5613029 1 5.75
CHEMBL5614064 1 5.58
CHEMBL5612634 1 5.43
CHEMBL5613885 1 5.16
CHEMBL5612066 1 5.13
CHEMBL5613717 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5613766 EC50 = 370.0 nM 6.43
CHEMBL5613621 EC50 = 1600.0 nM 5.80
CHEMBL5613029 EC50 = 1800.0 nM 5.75
CHEMBL5614064 EC50 = 2600.0 nM 5.58
CHEMBL5612634 EC50 = 3700.0 nM 5.43
CHEMBL5613885 EC50 = 6900.0 nM 5.16
CHEMBL5612066 EC50 = 7400.0 nM 5.13
CHEMBL5613717 EC50 = 11000.0 nM 4.96