Assay Detail
Binding
CHEMBL5732093
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Enzymatic Assay: PARP-2 and PARP-3 enzymatic assays were conducted using commercial PARP-2/PARP-3 Chemiluminescent Assay Kit (BPS Biosciences) and the protocols with the kits. Briefly, histones were coated in a high binding plate first, and incubated with PARP-2 or PARP-3, and increasing concentrations of compounds for 0.5 h. Then, biotinylated NAD and activated DNA were added to the wells. The biotinylated 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.
30
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.75 | 4.75 |
| kon | 10 | - | - |
| k_off | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3970252 | — | — | 3 | 4.75 |
| CHEMBL3891329 | — | — | 3 | - |
| CHEMBL3911687 | — | — | 3 | - |
| CHEMBL3984980 | — | — | 3 | - |
| CHEMBL3926240 | — | — | 3 | - |
| CHEMBL3940569 | — | — | 3 | - |
| CHEMBL3907535 | — | — | 3 | - |
| CHEMBL3922789 | — | — | 3 | - |
| CHEMBL3978989 | — | — | 3 | - |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3970252 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3891329 | — | IC50 | = | 199000.0 | nM | - |
| CHEMBL3891329 | — | kon | = | - | — | - |
| CHEMBL3891329 | — | k_off | = | - | s-1 | - |
| CHEMBL3911687 | — | IC50 | = | 136000.0 | nM | - |
| CHEMBL3911687 | — | kon | = | - | — | - |
| CHEMBL3911687 | — | k_off | = | - | s-1 | - |
| CHEMBL3984980 | — | IC50 | > | 20000000.0 | nM | - |
| CHEMBL3984980 | — | kon | = | - | — | - |
| CHEMBL3984980 | — | k_off | = | - | s-1 | - |
| CHEMBL3926240 | — | IC50 | = | 11000000.0 | nM | - |
| CHEMBL3926240 | — | kon | = | - | — | - |
| CHEMBL3926240 | — | k_off | = | - | s-1 | - |
| CHEMBL3940569 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL3940569 | — | kon | = | - | — | - |
| CHEMBL3940569 | — | k_off | = | - | s-1 | - |
| CHEMBL3907535 | — | kon | = | - | — | - |
| CHEMBL3907535 | — | k_off | = | - | s-1 | - |
| CHEMBL3922789 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL3922789 | — | kon | = | - | — | - |
| CHEMBL3922789 | — | k_off | = | - | s-1 | - |
| CHEMBL3978989 | — | IC50 | = | 660000.0 | nM | - |
| CHEMBL3978989 | — | kon | = | - | — | - |
| CHEMBL3978989 | — | k_off | = | - | s-1 | - |
| CHEMBL3970252 | — | kon | = | - | — | - |
| CHEMBL3970252 | — | k_off | = | - | s-1 | - |
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 185000.0 | nM | - |
| CHEMBL4112930 | PAMIPARIB | kon | = | - | — | - |
| CHEMBL4112930 | PAMIPARIB | k_off | = | - | s-1 | - |
| CHEMBL3907535 | — | IC50 | = | 760000.0 | nM | - |