Assay Detail
Binding
CHEMBL1110690
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Inhibition of PARP2 by top count scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.29 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090136 | — | — | 1 | 9.00 |
| CHEMBL577549 | — | — | 1 | 9.00 |
| CHEMBL1090467 | — | — | 1 | 8.82 |
| CHEMBL1093844 | — | — | 1 | 8.70 |
| CHEMBL576423 | — | — | 1 | 8.70 |
| CHEMBL1093309 | — | — | 1 | 8.52 |
| CHEMBL1092691 | — | — | 1 | 8.52 |
| CHEMBL1093900 | — | — | 1 | 8.52 |
| CHEMBL1089125 | — | — | 1 | 8.40 |
| CHEMBL571285 | — | — | 1 | 8.10 |
| CHEMBL1090483 | — | — | 1 | 8.00 |
| CHEMBL1090582 | — | — | 1 | 7.96 |
| CHEMBL1093012 | — | — | 1 | 7.92 |
| CHEMBL1090482 | — | — | 1 | 7.75 |
| CHEMBL1092737 | — | — | 1 | 7.75 |
| CHEMBL1092223 | — | — | 1 | 7.64 |
| CHEMBL1089474 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090136 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL577549 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1090467 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1093844 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL576423 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1093309 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1092691 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1093900 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1089125 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL571285 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1090483 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1090582 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1093012 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1090482 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1092737 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1092223 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1089474 | — | Ki | = | 26.0 | nM | 7.58 |