Assay Detail
Binding
CHEMBL4431950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP1 (unknown origin)
42
Total Activities
41
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 8.04 | 9.24 |
| Ki | 1 | 8.85 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 9.24 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 9.00 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 8.85 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 8.42 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.30 |
| CHEMBL4447698 | — | — | 1 | 8.24 |
| CHEMBL4448508 | — | — | 1 | 7.66 |
| CHEMBL4472182 | — | — | 1 | 7.66 |
| CHEMBL4453414 | — | — | 1 | 7.59 |
| CHEMBL4530032 | — | — | 1 | 7.53 |
| CHEMBL4448791 | — | — | 1 | 7.41 |
| CHEMBL4591736 | — | — | 1 | 7.36 |
| CHEMBL4559177 | — | — | 1 | - |
| CHEMBL4586275 | — | — | 1 | - |
| CHEMBL4465632 | — | — | 1 | - |
| CHEMBL4573183 | — | — | 1 | - |
| CHEMBL4520246 | — | — | 1 | - |
| CHEMBL4559761 | — | — | 1 | - |
| CHEMBL4461020 | — | — | 1 | - |
| CHEMBL4531980 | — | — | 1 | - |
| CHEMBL4452682 | — | — | 1 | - |
| CHEMBL4464793 | — | — | 1 | - |
| CHEMBL4472164 | — | — | 1 | - |
| CHEMBL4520368 | — | — | 1 | - |
| CHEMBL4574816 | — | — | 1 | - |
| CHEMBL4520222 | — | — | 1 | - |
| CHEMBL4446277 | — | — | 1 | - |
| CHEMBL4535327 | — | — | 1 | - |
| CHEMBL4526294 | — | — | 2 | - |
| CHEMBL4458137 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1173055 | RUCAPARIB | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4447698 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4472182 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL4448508 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL4453414 | — | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL4530032 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4448791 | — | IC50 | = | 39.1 | nM | 7.41 |
| CHEMBL4591736 | — | IC50 | = | 43.7 | nM | 7.36 |
| CHEMBL4465632 | — | IC50 | - | — | - | |
| CHEMBL4461020 | — | IC50 | - | — | - | |
| CHEMBL4586275 | — | IC50 | - | — | - | |
| CHEMBL4559177 | — | IC50 | - | — | - | |
| CHEMBL4466469 | — | IC50 | - | — | - | |
| CHEMBL4435751 | — | IC50 | - | — | - | |
| CHEMBL4456584 | — | IC50 | - | — | - | |
| CHEMBL4445318 | — | IC50 | - | — | - | |
| CHEMBL4550219 | — | IC50 | - | — | - | |
| CHEMBL4576743 | — | IC50 | - | — | - | |
| CHEMBL4457127 | — | IC50 | - | — | - | |
| CHEMBL4590169 | — | IC50 | - | — | - | |
| CHEMBL4471965 | — | IC50 | - | — | - | |
| CHEMBL4544675 | — | IC50 | - | — | - | |
| CHEMBL4558915 | — | IC50 | - | — | - | |
| CHEMBL4573183 | — | IC50 | - | — | - | |
| CHEMBL4520246 | — | IC50 | - | — | - | |
| CHEMBL4559761 | — | IC50 | - | — | - | |
| CHEMBL4531980 | — | IC50 | - | — | - | |
| CHEMBL4452682 | — | IC50 | - | — | - | |
| CHEMBL4464793 | — | IC50 | - | — | - | |
| CHEMBL4472164 | — | IC50 | - | — | - | |
| CHEMBL4520368 | — | IC50 | - | — | - | |
| CHEMBL4446277 | — | IC50 | - | — | - | |
| CHEMBL4574816 | — | IC50 | - | — | - | |
| CHEMBL4535327 | — | IC50 | - | — | - | |
| CHEMBL4526294 | — | IC50 | - | — | - | |
| CHEMBL4458137 | — | IC50 | - | — | - | |
| CHEMBL4526294 | — | IC50 | - | — | - | |
| CHEMBL4520222 | — | IC50 | - | — | - |