Assay Detail
Binding
CHEMBL3743828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Poly [ADP-ribose] polymerase tankyrase-1 (CHEMBL6164) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.42 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3740104 | — | — | 1 | 8.05 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 5.72 |
| CHEMBL3740897 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3740104 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3740897 | — | IC50 | = | 3200.0 | nM | 5.50 |