Assay Detail
Binding
CHEMBL1042277
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Inhibition of PARP1 in human C41 cells after 30 mins by cell-based assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | C41 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565882 | — | — | 1 | 9.00 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 8.70 |
| CHEMBL565881 | — | — | 1 | 8.66 |
| CHEMBL452800 | — | — | 1 | 8.52 |
| CHEMBL576319 | — | — | 1 | 8.43 |
| CHEMBL569195 | — | — | 1 | 8.43 |
| CHEMBL574147 | — | — | 1 | 8.43 |
| CHEMBL576423 | — | — | 1 | 8.11 |
| CHEMBL571285 | — | — | 1 | 8.05 |
| CHEMBL579023 | — | — | 1 | 8.04 |
| CHEMBL577549 | — | — | 1 | 7.92 |
| CHEMBL583933 | — | — | 1 | 7.75 |
| CHEMBL578397 | — | — | 1 | 7.70 |
| CHEMBL569635 | — | — | 1 | 7.70 |
| CHEMBL578804 | — | — | 1 | 7.70 |
| CHEMBL571928 | — | — | 1 | 7.58 |
| CHEMBL576910 | — | — | 1 | 7.19 |
| CHEMBL578185 | — | — | 1 | 7.15 |
| CHEMBL569636 | — | — | 1 | 6.48 |
| CHEMBL583526 | — | — | 1 | 6.34 |
| CHEMBL568722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565882 | — | EC50 | = | 0.99 | nM | 9.00 |
| CHEMBL506871 | VELIPARIB | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL565881 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL452800 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL576319 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL569195 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL574147 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL576423 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL571285 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL579023 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL577549 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL583933 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL578397 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL569635 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL578804 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL571928 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL576910 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL578185 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL569636 | — | EC50 | = | 328.0 | nM | 6.48 |
| CHEMBL583526 | — | EC50 | = | 461.0 | nM | 6.34 |
| CHEMBL568722 | — | EC50 | > | 1000.0 | nM | - |