Assay Detail
Binding
CHEMBL4003522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-GST-tagged TNKS2 (849 to 1166 residues) expressed in baculovirus infected Sf9 cells using biotinylated NAD+ as substrate measured after 2 hrs
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-2 (CHEMBL6154) ↗| 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 | 8.85 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069447 | — | — | 2 | 10.00 |
| CHEMBL4098188 | — | — | 2 | 9.70 |
| CHEMBL4059827 | — | — | 2 | 8.19 |
| CHEMBL1956162 | — | — | 2 | 7.51 |
| CHEMBL4080163 | — | — | 1 | - |
| CHEMBL1892587 | — | — | 1 | - |
| CHEMBL4063631 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069447 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4069447 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4098188 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4098188 | — | IC50 | = | 0.2042 | nM | 9.69 |
| CHEMBL4059827 | — | IC50 | = | 6.457 | nM | 8.19 |
| CHEMBL4059827 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1956162 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL1956162 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4080163 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1892587 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4063631 | — | IC50 | > | 100000.0 | nM | - |