Assay Detail
Binding
CHEMBL3110587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay
10
Total Activities
5
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
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.47 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45245 | — | — | 2 | 7.86 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 2 | 7.85 |
| CHEMBL3108871 | — | — | 2 | 7.62 |
| CHEMBL435073 | — | — | 2 | 7.35 |
| CHEMBL372303 | PJ34 | — | 2 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45245 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL45245 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3108871 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL3108871 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL435073 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL435073 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL372303 | PJ34 | IC50 | = | 218.78 | nM | 6.66 |
| CHEMBL372303 | PJ34 | IC50 | = | 219.0 | nM | 6.66 |