Assay Detail
Binding
CHEMBL4322255
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST tagged-TEV cleavage site-fused human recombinant TNKS2 (873 to 1166 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARsylation incubated for 90 mins in presence of bio-NAD as co-substrate by TR-FRET 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-2 (CHEMBL6154) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.59 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL336718 | — | — | 1 | 7.28 |
| CHEMBL127066 | — | — | 1 | 6.27 |
| CHEMBL4077094 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL336718 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL127066 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4077094 | — | IC50 | = | 620.0 | nM | 6.21 |