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Assay Detail

CHEMBL4840936

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

Binding
Inhibition of C-terminal 6-His-tagged 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
ChEMBL ↗
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

Discovery of an Orally Bioavailable Small-Molecule Inhibitor for the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.
Wang Z, Zhang M, Quereda V, Frydman SM, Ming Q, Luca VC, Duckett DR, Ji H.
J Med Chem (2021) 64 : 12109 -12131
PubMed 34382808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.90 6.06
Ki 22 4.95 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846565 — — 2 6.12
CHEMBL4853982 — — 2 5.72
CHEMBL4863751 — — 2 5.68
CHEMBL4874860 — — 2 5.57
CHEMBL4857780 — — 2 5.40
CHEMBL4851887 — — 2 5.34
CHEMBL4869003 — — 2 5.32
CHEMBL4860362 — — 2 5.30
CHEMBL4852661 — — 2 5.24
CHEMBL4876911 — — 2 5.10
CHEMBL4852707 — — 2 4.96
CHEMBL4869538 — — 2 4.89
CHEMBL4862286 — — 2 4.85
CHEMBL4871689 — — 2 4.50
CHEMBL4847343 — — 2 4.50
CHEMBL4855433 — — 2 4.37
CHEMBL4873635 — — 2 4.34
CHEMBL4869034 — — 2 4.27
CHEMBL4868531 — — 2 4.18
CHEMBL4864467 — — 2 4.17
CHEMBL4858087 — — 2 4.13
CHEMBL4868665 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846565 — Ki = 760.0 nM 6.12
CHEMBL4846565 — IC50 = 870.0 nM 6.06
CHEMBL4853982 — Ki = 1900.0 nM 5.72
CHEMBL4863751 — Ki = 2100.0 nM 5.68
CHEMBL4853982 — IC50 = 2100.0 nM 5.68
CHEMBL4863751 — IC50 = 2300.0 nM 5.64
CHEMBL4874860 — Ki = 2700.0 nM 5.57
CHEMBL4874860 — IC50 = 3000.0 nM 5.52
CHEMBL4857780 — Ki = 4000.0 nM 5.40
CHEMBL4857780 — IC50 = 4500.0 nM 5.35
CHEMBL4851887 — Ki = 4600.0 nM 5.34
CHEMBL4869003 — Ki = 4800.0 nM 5.32
CHEMBL4860362 — Ki = 5000.0 nM 5.30
CHEMBL4851887 — IC50 = 5100.0 nM 5.29
CHEMBL4869003 — IC50 = 5300.0 nM 5.28
CHEMBL4860362 — IC50 = 5500.0 nM 5.26
CHEMBL4852661 — Ki = 5800.0 nM 5.24
CHEMBL4852661 — IC50 = 6400.0 nM 5.19
CHEMBL4876911 — Ki = 8000.0 nM 5.10
CHEMBL4876911 — IC50 = 8900.0 nM 5.05
CHEMBL4852707 — Ki = 11000.0 nM 4.96
CHEMBL4852707 — IC50 = 12000.0 nM 4.92
CHEMBL4869538 — Ki = 13000.0 nM 4.89
CHEMBL4862286 — Ki = 14000.0 nM 4.85
CHEMBL4869538 — IC50 = 14000.0 nM 4.85
CHEMBL4862286 — IC50 = 15000.0 nM 4.82
CHEMBL4847343 — Ki = 32000.0 nM 4.50
CHEMBL4871689 — Ki = 32000.0 nM 4.50
CHEMBL4871689 — IC50 = 35000.0 nM 4.46
CHEMBL4847343 — IC50 = 39000.0 nM 4.41
CHEMBL4855433 — Ki = 43000.0 nM 4.37
CHEMBL4873635 — Ki = 46000.0 nM 4.34
CHEMBL4873635 — IC50 = 51000.0 nM 4.29
CHEMBL4855433 — IC50 = 53000.0 nM 4.28
CHEMBL4869034 — Ki = 54000.0 nM 4.27
CHEMBL4869034 — IC50 = 59000.0 nM 4.23
CHEMBL4868531 — Ki = 66000.0 nM 4.18
CHEMBL4864467 — Ki = 68000.0 nM 4.17
CHEMBL4868531 — IC50 = 73000.0 nM 4.14
CHEMBL4858087 — Ki = 74000.0 nM 4.13
CHEMBL4864467 — IC50 = 76000.0 nM 4.12
CHEMBL4858087 — IC50 = 82000.0 nM 4.09
CHEMBL4868665 — IC50 > 100000.0 nM -
CHEMBL4868665 — Ki > 90000.0 nM -