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Assay Detail

CHEMBL1693159

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

Binding
Displacement of wild type mBimBH3 from human Bcl-w by solution competition assay
9
Total Activities
9
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

Bcl-2-like protein 2 (CHEMBL4677)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB.
J Med Chem (2011) 54 : 1914 -1926
PubMed 21366295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.64 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376408 ABT 737 1.0 1 7.40
CHEMBL1689141 1 6.61
CHEMBL1689145 1 6.56
CHEMBL1689139 1 6.36
CHEMBL1689143 1 6.27
CHEMBL1689140 1 -
CHEMBL1689142 1 -
CHEMBL1689144 1 -
CHEMBL1689146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376408 ABT 737 IC50 = 40.0 nM 7.40
CHEMBL1689141 IC50 = 245.0 nM 6.61
CHEMBL1689145 IC50 = 275.0 nM 6.56
CHEMBL1689139 IC50 = 440.0 nM 6.36
CHEMBL1689143 IC50 = 540.0 nM 6.27
CHEMBL1689140 IC50 > 1000.0 nM -
CHEMBL1689142 IC50 > 1000.0 nM -
CHEMBL1689144 IC50 > 1000.0 nM -
CHEMBL1689146 IC50 > 1000.0 nM -