Assay Detail
Binding
CHEMBL2433124
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TNKS2 (873 to 1161) (unknown origin) expressed in Escherichia coli Rosetta2(DE3) using NAD+ as substrate by fluorescence assay
8
Total Activities
4
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
Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.34 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2431805 | — | — | 2 | 8.70 |
| CHEMBL2431867 | — | — | 2 | 7.14 |
| CHEMBL64780 | — | — | 2 | 6.85 |
| CHEMBL16861 | — | — | 2 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2431805 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2431805 | — | IC50 | = | 2.344 | nM | 8.63 |
| CHEMBL2431867 | — | IC50 | = | 72.44 | nM | 7.14 |
| CHEMBL2431867 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL64780 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL64780 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL16861 | — | IC50 | = | 190.55 | nM | 6.72 |
| CHEMBL16861 | — | IC50 | = | 190.0 | nM | 6.72 |