Assay Detail
Binding
CHEMBL5732092
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
66
Total Activities
21
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 | 22 | 6.09 | 6.70 |
| kon | 22 | - | - |
| k_off | 22 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3984980 | — | — | 3 | 6.70 |
| CHEMBL3922789 | — | — | 3 | 6.52 |
| CHEMBL3926240 | — | — | 3 | 6.52 |
| CHEMBL3933450 | — | — | 3 | 6.52 |
| CHEMBL4107982 | — | — | 3 | 6.40 |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 3 | 6.30 |
| CHEMBL3955609 | — | — | 3 | 6.30 |
| CHEMBL3972156 | — | — | 3 | 6.22 |
| CHEMBL3901034 | — | — | 3 | 6.16 |
| CHEMBL3914932 | — | — | 6 | 6.16 |
| CHEMBL3929705 | — | — | 3 | 6.10 |
| CHEMBL3907535 | — | — | 3 | 6.10 |
| CHEMBL3961684 | — | — | 3 | 6.05 |
| CHEMBL3970252 | — | — | 3 | 6.00 |
| CHEMBL3907218 | — | — | 3 | 5.96 |
| CHEMBL3969742 | — | — | 3 | 5.96 |
| CHEMBL3978989 | — | — | 3 | 5.89 |
| CHEMBL3892363 | — | — | 3 | 5.80 |
| CHEMBL3915929 | — | — | 3 | 5.77 |
| CHEMBL3891329 | — | — | 3 | 5.72 |
| CHEMBL3940569 | — | — | 3 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3984980 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3922789 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3926240 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3933450 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4107982 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3955609 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3972156 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3914932 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3901034 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3914932 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3907535 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3929705 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3961684 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3970252 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3969742 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3907218 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3978989 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3892363 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3915929 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3891329 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3940569 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3907535 | — | kon | = | - | — | - |
| CHEMBL3978989 | — | kon | = | - | — | - |
| CHEMBL3907535 | — | k_off | = | - | s-1 | - |
| CHEMBL3922789 | — | k_off | = | - | s-1 | - |
| CHEMBL3914932 | — | kon | = | - | — | - |
| CHEMBL3891329 | — | kon | = | - | — | - |
| CHEMBL3891329 | — | k_off | = | - | s-1 | - |
| CHEMBL3969742 | — | kon | = | - | — | - |
| CHEMBL3969742 | — | k_off | = | - | s-1 | - |
| CHEMBL3915929 | — | kon | = | - | — | - |
| CHEMBL3915929 | — | k_off | = | - | s-1 | - |
| CHEMBL3892363 | — | kon | = | - | — | - |
| CHEMBL3892363 | — | k_off | = | - | s-1 | - |
| CHEMBL3907218 | — | kon | = | - | — | - |
| CHEMBL3978989 | — | k_off | = | - | s-1 | - |
| CHEMBL3970252 | — | kon | = | - | — | - |
| CHEMBL3940569 | — | k_off | = | - | s-1 | - |
| CHEMBL3940569 | — | kon | = | - | — | - |
| CHEMBL3922789 | — | kon | = | - | — | - |
| CHEMBL3926240 | — | k_off | = | - | s-1 | - |
| CHEMBL4107982 | — | kon | = | - | — | - |
| CHEMBL3926240 | — | kon | = | - | — | - |
| CHEMBL4107982 | — | k_off | = | - | s-1 | - |
| CHEMBL4112930 | PAMIPARIB | kon | = | - | — | - |
| CHEMBL3984980 | — | k_off | = | - | s-1 | - |
| CHEMBL3984980 | — | kon | = | - | — | - |
| CHEMBL4112930 | PAMIPARIB | k_off | = | - | s-1 | - |
| CHEMBL3970252 | — | k_off | = | - | s-1 | - |