Assay Detail
Binding
CHEMBL3887992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tankyrase-2 Enzymatic Assay: Tankyrase-2 enzymatic assay was conducted using commercial Tankyrase-2 Chemiluminescent Assay Kit (BPS Biosciences) and the protocol with the kit. GST-fused tankyrase-2 (recombinant protein expressed and purified from Bacluovirus) were coated on a GSH-precoated plate first, and incubated with increasing concentrations of compounds for 0.5 h. Then, biotinylated NAD was added to the wells. The biotinylated auto-PARylation product was measured by adding streptavidin-HRP and HRP substrates which produce chemiluminescence.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Poly [ADP-ribose] polymerase tankyrase-2 (CHEMBL6154) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.41 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3925115 | — | — | 1 | 7.54 |
| CHEMBL3907218 | — | — | 1 | 7.10 |
| CHEMBL3929705 | — | — | 1 | 6.99 |
| CHEMBL3969049 | — | — | 1 | 6.89 |
| CHEMBL3891329 | — | — | 1 | 6.85 |
| CHEMBL3915929 | — | — | 1 | 6.84 |
| CHEMBL3898162 | — | — | 1 | 6.82 |
| CHEMBL3969742 | — | — | 1 | 6.81 |
| CHEMBL3892363 | — | — | 1 | 6.79 |
| CHEMBL3911687 | — | — | 1 | 6.69 |
| CHEMBL3929889 | — | — | 1 | 6.32 |
| CHEMBL3984980 | — | — | 1 | 6.16 |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 1 | 6.12 |
| CHEMBL3972156 | — | — | 1 | 6.08 |
| CHEMBL3947278 | — | — | 1 | 5.98 |
| CHEMBL3907535 | — | — | 1 | 5.92 |
| CHEMBL4107982 | — | — | 1 | 5.91 |
| CHEMBL3975917 | — | — | 1 | 5.89 |
| CHEMBL3947623 | — | — | 1 | 5.82 |
| CHEMBL3926240 | — | — | 1 | 5.62 |
| CHEMBL3970252 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3925115 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3907218 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3929705 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3969049 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3891329 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3915929 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL3898162 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3969742 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL3892363 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3911687 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL3929889 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3984980 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL3972156 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL3947278 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3907535 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4107982 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL3975917 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3947623 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3926240 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3970252 | — | IC50 | = | 3800.0 | nM | 5.42 |