Assay Detail
Binding
CHEMBL4003521
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected sf9 cells using TACS-Sapphire as substrate measured after 30 mins by colorimetric assay
11
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Poly [ADP-ribose] polymerase tankyrase-1 (CHEMBL6164) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 11 | 7.57 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069447 | — | — | 2 | 8.29 |
| CHEMBL4098188 | — | — | 2 | 8.04 |
| CHEMBL4059827 | — | — | 2 | 7.47 |
| CHEMBL1956162 | — | — | 2 | 6.46 |
| CHEMBL4080163 | — | — | 1 | - |
| CHEMBL1892587 | — | — | 1 | - |
| CHEMBL4063631 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069447 | — | IC50 | = | 5.129 | nM | 8.29 |
| CHEMBL4069447 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4098188 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL4098188 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4059827 | — | IC50 | = | 33.88 | nM | 7.47 |
| CHEMBL4059827 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1956162 | — | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL1956162 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4080163 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1892587 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4063631 | — | IC50 | > | 100000.0 | nM | - |