Assay Detail
Binding
CHEMBL1074648
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Inhibition of PARP1 in human HeLa cells assessed as inhibition of hydrogen peroxide-induced poly(ADP-ribosyl)ation
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 44 | 6.12 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595694 | — | — | 1 | 6.89 |
| CHEMBL595928 | — | — | 1 | 6.80 |
| CHEMBL610165 | — | — | 1 | 6.75 |
| CHEMBL594521 | — | — | 1 | 6.70 |
| CHEMBL611621 | — | — | 1 | 6.70 |
| CHEMBL593592 | — | — | 1 | 6.64 |
| CHEMBL596389 | — | — | 1 | 6.64 |
| CHEMBL611049 | — | — | 1 | 6.58 |
| CHEMBL611322 | — | — | 1 | 6.55 |
| CHEMBL592909 | — | — | 1 | 6.51 |
| CHEMBL609002 | — | — | 1 | 6.48 |
| CHEMBL596390 | — | — | 1 | 6.46 |
| CHEMBL595018 | — | — | 1 | 6.44 |
| CHEMBL595679 | — | — | 1 | 6.39 |
| CHEMBL593202 | — | — | 1 | 6.38 |
| CHEMBL611958 | — | — | 1 | 6.36 |
| CHEMBL593837 | — | — | 1 | 6.26 |
| CHEMBL594522 | — | — | 1 | 6.24 |
| CHEMBL594976 | — | — | 1 | 6.19 |
| CHEMBL593364 | — | — | 1 | 6.18 |
| CHEMBL595692 | — | — | 1 | 6.16 |
| CHEMBL596168 | — | — | 1 | 6.08 |
| CHEMBL595927 | — | — | 1 | 6.05 |
| CHEMBL595926 | — | — | 1 | 5.96 |
| CHEMBL596391 | — | — | 1 | 5.96 |
| CHEMBL595236 | — | — | 1 | 5.92 |
| CHEMBL593201 | — | — | 1 | 5.89 |
| CHEMBL595693 | — | — | 1 | 5.85 |
| CHEMBL596354 | — | — | 1 | 5.80 |
| CHEMBL595237 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595694 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL595928 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL610165 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL594521 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL611621 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL593592 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL596389 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL611049 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL611322 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL592909 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL609002 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL596390 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL595018 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL595679 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL593202 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL611958 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL593837 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL594522 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL594976 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL593364 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL595692 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL596168 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL595927 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL596391 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL595926 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL595236 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL593201 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL595693 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL596354 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL595237 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL594599 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL595680 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL593133 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL595019 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL593363 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL595464 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL593593 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL595681 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL593611 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL594975 | — | EC50 | - | — | - | |
| CHEMBL592910 | — | EC50 | - | — | - | |
| CHEMBL603318 | — | EC50 | - | — | - | |
| CHEMBL594999 | — | EC50 | - | — | - | |
| CHEMBL608994 | — | EC50 | - | — | - |