Assay Detail
Binding
CHEMBL5732094
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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. The IC50s were calculated based on residual enzyme activity in presence of increasing concentrations of compounds.
63
Total Activities
21
Compounds Tested
3
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 | 4.54 | 4.54 |
| kon | 21 | - | - |
| k_off | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3925115 | — | — | 3 | 4.54 |
| CHEMBL3984980 | — | — | 3 | - |
| CHEMBL3969742 | — | — | 3 | - |
| CHEMBL3915929 | — | — | 3 | - |
| CHEMBL3947278 | — | — | 3 | - |
| CHEMBL3892363 | — | — | 3 | - |
| CHEMBL3907218 | — | — | 3 | - |
| CHEMBL3929705 | — | — | 3 | - |
| CHEMBL3911687 | — | — | 3 | - |
| CHEMBL3972156 | — | — | 3 | - |
| CHEMBL3891329 | — | — | 3 | - |
| CHEMBL3947623 | — | — | 3 | - |
| CHEMBL3926240 | — | — | 3 | - |
| CHEMBL3898162 | — | — | 3 | - |
| CHEMBL3969049 | — | — | 3 | - |
| CHEMBL3929889 | — | — | 3 | - |
| CHEMBL3907535 | — | — | 3 | - |
| CHEMBL3970252 | — | — | 3 | - |
| CHEMBL4107982 | — | — | 3 | - |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 3 | - |
| CHEMBL3975917 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3925115 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL3969742 | — | k_off | = | - | s-1 | - |
| CHEMBL4107982 | — | IC50 | = | 1220000.0 | nM | - |
| CHEMBL4107982 | — | kon | = | - | — | - |
| CHEMBL4107982 | — | k_off | = | - | s-1 | - |
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 766000.0 | nM | - |
| CHEMBL4112930 | PAMIPARIB | kon | = | - | — | - |
| CHEMBL4112930 | PAMIPARIB | k_off | = | - | s-1 | - |
| CHEMBL3907218 | — | kon | = | - | — | - |
| CHEMBL3891329 | — | kon | = | - | — | - |
| CHEMBL3891329 | — | k_off | = | - | s-1 | - |
| CHEMBL3969742 | — | IC50 | = | 154000.0 | nM | - |
| CHEMBL3969742 | — | kon | = | - | — | - |
| CHEMBL3970252 | — | k_off | = | - | s-1 | - |
| CHEMBL3915929 | — | IC50 | = | 143000.0 | nM | - |
| CHEMBL3915929 | — | kon | = | - | — | - |
| CHEMBL3915929 | — | k_off | = | - | s-1 | - |
| CHEMBL3947278 | — | IC50 | = | 1050000.0 | nM | - |
| CHEMBL3947278 | — | kon | = | - | — | - |
| CHEMBL3947278 | — | k_off | = | - | s-1 | - |
| CHEMBL3892363 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL3892363 | — | kon | = | - | — | - |
| CHEMBL3892363 | — | k_off | = | - | s-1 | - |
| CHEMBL3907218 | — | IC50 | = | 80000.0 | nM | - |
| CHEMBL3975917 | — | k_off | = | - | s-1 | - |
| CHEMBL3907218 | — | k_off | = | - | s-1 | - |
| CHEMBL3898162 | — | kon | = | - | — | - |
| CHEMBL3969049 | — | k_off | = | - | s-1 | - |
| CHEMBL3947623 | — | IC50 | = | 1500000.0 | nM | - |
| CHEMBL3947623 | — | kon | = | - | — | - |
| CHEMBL3947623 | — | k_off | = | - | s-1 | - |
| CHEMBL3984980 | — | IC50 | = | 700000.0 | nM | - |
| CHEMBL3984980 | — | kon | = | - | — | - |
| CHEMBL3984980 | — | k_off | = | - | s-1 | - |
| CHEMBL3926240 | — | IC50 | = | 2400000.0 | nM | - |
| CHEMBL3926240 | — | kon | = | - | — | - |
| CHEMBL3926240 | — | k_off | = | - | s-1 | - |
| CHEMBL3898162 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL3970252 | — | kon | = | - | — | - |
| CHEMBL3898162 | — | k_off | = | - | s-1 | - |
| CHEMBL3969049 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL3969049 | — | kon | = | - | — | - |
| CHEMBL3975917 | — | kon | = | - | — | - |
| CHEMBL3929889 | — | IC50 | = | 480000.0 | nM | - |
| CHEMBL3929889 | — | kon | = | - | — | - |
| CHEMBL3929889 | — | k_off | = | - | s-1 | - |
| CHEMBL3907535 | — | IC50 | = | 1200000.0 | nM | - |
| CHEMBL3907535 | — | kon | = | - | — | - |
| CHEMBL3907535 | — | k_off | = | - | s-1 | - |
| CHEMBL3970252 | — | IC50 | = | 3800000.0 | nM | - |