Assay Detail
Binding
CHEMBL1767525
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Inhibition of full length human PARP-1 after 10 mins by FlashPlate scintillation proximity assay
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-Benzamidoisoquinolin-1-ones and 5-(ω-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.47 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1767068 | — | — | 1 | 7.89 |
| CHEMBL1767067 | — | — | 1 | 7.52 |
| CHEMBL1767066 | — | — | 1 | 6.26 |
| CHEMBL446240 | — | — | 2 | 6.03 |
| CHEMBL1767065 | — | — | 1 | 5.80 |
| CHEMBL1767056 | — | — | 1 | 5.52 |
| CHEMBL1584950 | — | — | 1 | 5.39 |
| CHEMBL1767057 | — | — | 1 | 5.35 |
| CHEMBL1767063 | — | — | 1 | 5.18 |
| CHEMBL1767053 | — | — | 1 | 5.12 |
| CHEMBL1767064 | — | — | 1 | 5.07 |
| CHEMBL1767048 | — | — | 1 | 4.97 |
| CHEMBL1767051 | — | — | 1 | 4.95 |
| CHEMBL1767049 | — | — | 1 | 4.87 |
| CHEMBL1767054 | — | — | 1 | 4.86 |
| CHEMBL1767061 | — | — | 1 | 4.78 |
| CHEMBL1767050 | — | — | 1 | 4.75 |
| CHEMBL1767058 | — | — | 1 | 4.65 |
| CHEMBL1767055 | — | — | 1 | 4.50 |
| CHEMBL1767062 | — | — | 1 | - |
| CHEMBL1765110 | — | — | 1 | - |
| CHEMBL1767060 | — | — | 1 | - |
| CHEMBL1767059 | — | — | 1 | - |
| CHEMBL1767052 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1767068 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1767067 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1767066 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL446240 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL446240 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1767065 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1767056 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1584950 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL1767057 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1767063 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1767053 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL1767064 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1767048 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1767051 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL1767049 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL1767054 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL1767061 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL1767050 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1767058 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL1767055 | — | IC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL1767062 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL1765110 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1767060 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1767059 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1767052 | — | IC50 | - | — | - |