Assay Detail
Binding
CHEMBL986586
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Inhibition of PARP1
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.56 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481084 | — | — | 1 | 8.52 |
| CHEMBL481081 | — | — | 1 | 8.40 |
| CHEMBL479779 | — | — | 1 | 8.15 |
| CHEMBL517843 | — | — | 1 | 8.15 |
| CHEMBL481082 | — | — | 1 | 8.05 |
| CHEMBL479780 | — | — | 1 | 8.05 |
| CHEMBL479778 | — | — | 1 | 8.00 |
| CHEMBL480895 | — | — | 1 | 7.92 |
| CHEMBL479937 | — | — | 1 | 7.82 |
| CHEMBL520922 | — | — | 1 | 7.77 |
| CHEMBL520745 | — | — | 1 | 7.75 |
| CHEMBL481083 | — | — | 1 | 7.72 |
| CHEMBL481097 | — | — | 1 | 7.72 |
| CHEMBL480896 | — | — | 1 | 7.62 |
| CHEMBL448924 | — | — | 1 | 7.60 |
| CHEMBL508903 | — | — | 1 | 7.60 |
| CHEMBL481477 | — | — | 1 | 7.50 |
| CHEMBL517373 | — | — | 1 | 7.48 |
| CHEMBL479384 | — | — | 1 | 7.46 |
| CHEMBL482055 | — | — | 1 | 7.43 |
| CHEMBL480198 | — | — | 1 | 7.39 |
| CHEMBL481478 | — | — | 1 | 7.35 |
| CHEMBL480322 | — | — | 1 | 7.30 |
| CHEMBL481285 | — | — | 1 | 7.30 |
| CHEMBL445050 | — | — | 1 | 7.28 |
| CHEMBL479777 | — | — | 1 | 7.24 |
| CHEMBL444957 | — | — | 1 | 7.21 |
| CHEMBL121765 | — | — | 1 | 7.00 |
| CHEMBL481096 | — | — | 1 | 6.85 |
| CHEMBL133694 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481084 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL481081 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL479779 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL517843 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL481082 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL479780 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL479778 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL480895 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL479937 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL520922 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL520745 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL481083 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL481097 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL480896 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL448924 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL508903 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL481477 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL517373 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL479384 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL482055 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL480198 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL481478 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL480322 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL481285 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL445050 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL479777 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL444957 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL121765 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL481096 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL133694 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL445012 | — | Ki | = | 870.0 | nM | 6.06 |