Assay Detail
Binding
CHEMBL5318512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged full-length recombinant beta-catenin (1 to 781 residues) (unknown origin) expressed in Escherichia coli BL21 DE3/N-terminal FAM tagged BCL9 HD2(350 to 375 residues) (unknown origin) protein-protein interaction assessed as inhibition constant incubated for 3 hrs by competitive fluorescence polarization assay
39
Total Activities
39
Compounds Tested
1
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 Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.55 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5398967 | — | — | 1 | 6.19 |
| CHEMBL5416539 | — | — | 1 | 6.14 |
| CHEMBL5404409 | — | — | 1 | 6.05 |
| CHEMBL5413417 | — | — | 1 | 6.04 |
| CHEMBL5422967 | — | — | 1 | 6.00 |
| CHEMBL5399058 | — | — | 1 | 5.96 |
| CHEMBL5400908 | — | — | 1 | 5.93 |
| CHEMBL5440529 | — | — | 1 | 5.93 |
| CHEMBL5398170 | — | — | 1 | 5.90 |
| CHEMBL5406240 | — | — | 1 | 5.80 |
| CHEMBL5420343 | — | — | 1 | 5.73 |
| CHEMBL5397851 | — | — | 1 | 5.61 |
| CHEMBL5418296 | — | — | 1 | 5.50 |
| CHEMBL5422085 | — | — | 1 | 5.49 |
| CHEMBL5412754 | — | — | 1 | 5.42 |
| CHEMBL5424713 | — | — | 1 | 5.41 |
| CHEMBL5398771 | — | — | 1 | 5.40 |
| CHEMBL5394479 | — | — | 1 | 5.38 |
| CHEMBL5440087 | — | — | 1 | 5.37 |
| CHEMBL5428569 | — | — | 1 | 5.37 |
| CHEMBL5399118 | — | — | 1 | 5.35 |
| CHEMBL5435959 | — | — | 1 | 5.33 |
| CHEMBL5411500 | — | — | 1 | 5.31 |
| CHEMBL5396445 | — | — | 1 | 5.29 |
| CHEMBL5436700 | — | — | 1 | 5.28 |
| CHEMBL5396996 | — | — | 1 | 5.28 |
| CHEMBL5433123 | — | — | 1 | 5.27 |
| CHEMBL5440988 | — | — | 1 | 5.27 |
| CHEMBL5395861 | — | — | 1 | 5.17 |
| CHEMBL5409422 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5398967 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5416539 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5404409 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5413417 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5422967 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5399058 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5400908 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL5440529 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL5398170 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL5406240 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL5420343 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5397851 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL5418296 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL5422085 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL5412754 | — | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL5424713 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5398771 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5394479 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5428569 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL5440087 | — | IC50 | = | 4320.0 | nM | 5.37 |
| CHEMBL5399118 | — | IC50 | = | 4470.0 | nM | 5.35 |
| CHEMBL5435959 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL5411500 | — | IC50 | = | 4860.0 | nM | 5.31 |
| CHEMBL5396445 | — | IC50 | = | 5190.0 | nM | 5.29 |
| CHEMBL5436700 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL5396996 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL5433123 | — | IC50 | = | 5390.0 | nM | 5.27 |
| CHEMBL5440988 | — | IC50 | = | 5390.0 | nM | 5.27 |
| CHEMBL5409422 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5395861 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL5431783 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5395984 | — | IC50 | = | 8620.0 | nM | 5.06 |
| CHEMBL5433291 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5416247 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5436831 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5438849 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5440543 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5405503 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406679 | — | IC50 | > | 10000.0 | nM | - |