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Assay Detail

CHEMBL5167427

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

Binding
Inhibition of full length beta-catenin (1 to 781 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3)-N-terminal biotinylated human BCL9 (350 to 375 residues) protein-protein interaction incubated for 1 hr by Alphascreen assay
44
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

beta-catenin-B-cell lymphoma 9 protein complex (CHEMBL3885525)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

New ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein-Protein Interaction.
Wang Z, Zhang M, Thompson HM, Ji H.
ACS Med Chem Lett (2022) 13 : 865 -870
PubMed 35586435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.03 6.06
Ki 22 5.09 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846565 2 6.12
CHEMBL5190873 2 6.07
CHEMBL5208427 2 5.92
CHEMBL5187855 2 5.75
CHEMBL5176904 2 5.70
CHEMBL4863751 2 5.68
CHEMBL5173336 2 5.57
CHEMBL5192048 2 5.17
CHEMBL5190706 2 5.17
CHEMBL5181790 2 5.10
CHEMBL5181564 2 5.01
CHEMBL5209451 2 4.96
CHEMBL5203221 2 4.82
CHEMBL5175072 2 4.82
CHEMBL5200836 2 4.80
CHEMBL5181837 2 4.68
CHEMBL5192661 2 4.62
CHEMBL5205267 2 4.60
CHEMBL5181873 2 4.51
CHEMBL5202892 2 4.43
CHEMBL5209340 2 4.41
CHEMBL5169603 2 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846565 Ki = 760.0 nM 6.12
CHEMBL5190873 Ki = 850.0 nM 6.07
CHEMBL4846565 IC50 = 870.0 nM 6.06
CHEMBL5190873 IC50 = 960.0 nM 6.02
CHEMBL5208427 Ki = 1200.0 nM 5.92
CHEMBL5208427 IC50 = 1400.0 nM 5.85
CHEMBL5187855 Ki = 1800.0 nM 5.75
CHEMBL5176904 Ki = 2000.0 nM 5.70
CHEMBL4863751 Ki = 2100.0 nM 5.68
CHEMBL5187855 IC50 = 2200.0 nM 5.66
CHEMBL4863751 IC50 = 2300.0 nM 5.64
CHEMBL5176904 IC50 = 2500.0 nM 5.60
CHEMBL5173336 Ki = 2700.0 nM 5.57
CHEMBL5173336 IC50 = 3400.0 nM 5.47
CHEMBL5192048 Ki = 6800.0 nM 5.17
CHEMBL5190706 Ki = 6800.0 nM 5.17
CHEMBL5192048 IC50 = 7600.0 nM 5.12
CHEMBL5181790 Ki = 8000.0 nM 5.10
CHEMBL5190706 IC50 = 8300.0 nM 5.08
CHEMBL5181790 IC50 = 8900.0 nM 5.05
CHEMBL5181564 Ki = 9800.0 nM 5.01
CHEMBL5209451 Ki = 11000.0 nM 4.96
CHEMBL5209451 IC50 = 12000.0 nM 4.92
CHEMBL5181564 IC50 = 12000.0 nM 4.92
CHEMBL5175072 Ki = 15000.0 nM 4.82
CHEMBL5203221 Ki = 15000.0 nM 4.82
CHEMBL5200836 Ki = 16000.0 nM 4.80
CHEMBL5203221 IC50 = 18000.0 nM 4.75
CHEMBL5175072 IC50 = 18000.0 nM 4.75
CHEMBL5200836 IC50 = 20000.0 nM 4.70
CHEMBL5181837 Ki = 21000.0 nM 4.68
CHEMBL5181837 IC50 = 23000.0 nM 4.64
CHEMBL5192661 Ki = 24000.0 nM 4.62
CHEMBL5205267 Ki = 25000.0 nM 4.60
CHEMBL5205267 IC50 = 28000.0 nM 4.55
CHEMBL5192661 IC50 = 29000.0 nM 4.54
CHEMBL5181873 Ki = 31000.0 nM 4.51
CHEMBL5202892 Ki = 37000.0 nM 4.43
CHEMBL5181873 IC50 = 38000.0 nM 4.42
CHEMBL5209340 Ki = 39000.0 nM 4.41
CHEMBL5209340 IC50 = 43000.0 nM 4.37
CHEMBL5202892 IC50 = 44000.0 nM 4.36
CHEMBL5169603 Ki = 73000.0 nM 4.14
CHEMBL5169603 IC50 = 81000.0 nM 4.09