Assay Detail
Binding
CHEMBL4003526
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tankyrase (unknown origin) expressed in TCF/LEF-HEK293 cells assessed as inhibition of Wnt/beta-catenin signaling pathway in Wnt3a conditioned medium measured after 20 hrs by luciferase reporter gene assay
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.21 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098188 | — | — | 2 | 7.54 |
| CHEMBL4069447 | — | — | 2 | 7.43 |
| CHEMBL4059827 | — | — | 2 | 6.66 |
| CHEMBL4080163 | — | — | 1 | - |
| CHEMBL1892587 | — | — | 1 | - |
| CHEMBL4063631 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098188 | — | IC50 | = | 28.84 | nM | 7.54 |
| CHEMBL4098188 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4069447 | — | IC50 | = | 37.15 | nM | 7.43 |
| CHEMBL4069447 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4059827 | — | IC50 | = | 218.78 | nM | 6.66 |
| CHEMBL4059827 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4080163 | — | IC50 | - | — | - | |
| CHEMBL1892587 | — | IC50 | - | — | - | |
| CHEMBL4063631 | — | IC50 | - | — | - |