Assay Detail
Binding
CHEMBL3995366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
18
Total Activities
9
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
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.50 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4101890 | — | — | 2 | 9.32 |
| CHEMBL1086580 | — | — | 2 | 8.28 |
| CHEMBL3764816 | — | — | 2 | 6.97 |
| CHEMBL562310 | — | — | 2 | 6.87 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 2 | 6.05 |
| CHEMBL521686 | OLAPARIB | 4.0 | 2 | 5.63 |
| CHEMBL372303 | PJ34 | — | 2 | 5.54 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 2 | 5.29 |
| CHEMBL506871 | VELIPARIB | 3.0 | 2 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4101890 | — | IC50 | = | 0.4786 | nM | 9.32 |
| CHEMBL4101890 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1086580 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL1086580 | — | IC50 | = | 5.248 | nM | 8.28 |
| CHEMBL3764816 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3764816 | — | IC50 | = | 107.15 | nM | 6.97 |
| CHEMBL562310 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL562310 | — | IC50 | = | 134.9 | nM | 6.87 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL372303 | PJ34 | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL372303 | PJ34 | IC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 23988.33 | nM | 4.62 |