Assay Detail
Binding
CHEMBL5318513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of beta-catenin/BCL9 protein-protein interaction in Wnt-dependent human HCT-116 cells assessed as reduction in Axin2 expression level by qRT-PCR assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| 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 | 40 | 5.73 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5398967 | — | — | 1 | 6.16 |
| CHEMBL5416539 | — | — | 1 | 6.09 |
| CHEMBL5413417 | — | — | 1 | 6.03 |
| CHEMBL5440529 | — | — | 1 | 5.96 |
| CHEMBL5398170 | — | — | 1 | 5.95 |
| CHEMBL5422967 | — | — | 1 | 5.92 |
| CHEMBL5418296 | — | — | 1 | 5.88 |
| CHEMBL5397851 | — | — | 1 | 5.88 |
| CHEMBL5400908 | — | — | 1 | 5.87 |
| CHEMBL5399058 | — | — | 1 | 5.86 |
| CHEMBL5420343 | — | — | 1 | 5.83 |
| CHEMBL5406240 | — | — | 1 | 5.65 |
| CHEMBL2312139 | — | — | 1 | 5.57 |
| CHEMBL5404409 | — | — | 1 | 5.53 |
| CHEMBL5422085 | — | — | 1 | 5.45 |
| CHEMBL5412754 | — | — | 1 | 5.00 |
| CHEMBL5433123 | — | — | 1 | 4.84 |
| CHEMBL5399118 | — | — | 1 | - |
| CHEMBL5416247 | — | — | 1 | - |
| CHEMBL5431783 | — | — | 1 | - |
| CHEMBL5440543 | — | — | 1 | - |
| CHEMBL5398771 | — | — | 1 | - |
| CHEMBL5424713 | — | — | 1 | - |
| CHEMBL5436700 | — | — | 1 | - |
| CHEMBL5405503 | — | — | 1 | - |
| CHEMBL5409422 | — | — | 1 | - |
| CHEMBL5394479 | — | — | 1 | - |
| CHEMBL5396996 | — | — | 1 | - |
| CHEMBL5395861 | — | — | 1 | - |
| CHEMBL5440087 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5398967 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5416539 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5413417 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5440529 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5398170 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL5422967 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5418296 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL5397851 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL5400908 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5399058 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5420343 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL5406240 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL2312139 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL5404409 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL5422085 | — | IC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL5412754 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5433123 | — | IC50 | = | 14560.0 | nM | 4.84 |
| CHEMBL5435959 | — | IC50 | - | — | - | |
| CHEMBL5428569 | — | IC50 | - | — | - | |
| CHEMBL5433291 | — | IC50 | - | — | - | |
| CHEMBL5440988 | — | IC50 | - | — | - | |
| CHEMBL5395984 | — | IC50 | - | — | - | |
| CHEMBL5411500 | — | IC50 | - | — | - | |
| CHEMBL5436831 | — | IC50 | - | — | - | |
| CHEMBL5438849 | — | IC50 | - | — | - | |
| CHEMBL5406679 | — | IC50 | - | — | - | |
| CHEMBL5396445 | — | IC50 | - | — | - | |
| CHEMBL5440087 | — | IC50 | - | — | - | |
| CHEMBL5395861 | — | IC50 | - | — | - | |
| CHEMBL5396996 | — | IC50 | - | — | - | |
| CHEMBL5394479 | — | IC50 | - | — | - | |
| CHEMBL5409422 | — | IC50 | - | — | - | |
| CHEMBL5405503 | — | IC50 | - | — | - | |
| CHEMBL5436700 | — | IC50 | - | — | - | |
| CHEMBL5424713 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5398771 | — | IC50 | - | — | - | |
| CHEMBL5440543 | — | IC50 | - | — | - | |
| CHEMBL5431783 | — | IC50 | - | — | - | |
| CHEMBL5416247 | — | IC50 | - | — | - | |
| CHEMBL5399118 | — | IC50 | - | — | - |