Assay Detail
Binding
CHEMBL3607349
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Inhibition of PARP1 in human HeLa cells assessed as reduction of H2O2-induced PAR formation preincubated for 30 mins followed by H2O2 addition measured after 15 mins by immunocytochemical analysis
26
Total Activities
26
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 of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.04 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3605985 | — | — | 1 | 7.40 |
| CHEMBL3606021 | — | — | 1 | 7.40 |
| CHEMBL3606024 | — | — | 1 | 7.05 |
| CHEMBL3606016 | — | — | 1 | 7.00 |
| CHEMBL3605998 | — | — | 1 | 6.96 |
| CHEMBL3606018 | — | — | 1 | 6.82 |
| CHEMBL3605978 | — | — | 1 | 6.70 |
| CHEMBL3606008 | — | — | 1 | 6.43 |
| CHEMBL3606023 | — | — | 1 | 6.30 |
| CHEMBL3606017 | — | — | 1 | 6.25 |
| CHEMBL3606010 | — | — | 1 | 6.00 |
| CHEMBL3605996 | — | — | 1 | 5.96 |
| CHEMBL1329044 | — | — | 1 | 5.94 |
| CHEMBL3606014 | — | — | 1 | 5.80 |
| CHEMBL3606022 | — | — | 1 | 5.72 |
| CHEMBL3605986 | — | — | 1 | 5.70 |
| CHEMBL3605976 | — | — | 1 | 5.67 |
| CHEMBL3605983 | — | — | 1 | 5.65 |
| CHEMBL3606003 | — | — | 1 | 5.52 |
| CHEMBL3605967 | — | — | 1 | 5.28 |
| CHEMBL3606006 | — | — | 1 | 5.27 |
| CHEMBL3606001 | — | — | 1 | 5.22 |
| CHEMBL3606005 | — | — | 1 | 5.18 |
| CHEMBL3605997 | — | — | 1 | 5.00 |
| CHEMBL3606007 | — | — | 1 | 4.87 |
| CHEMBL3605999 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3605985 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3606021 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3606024 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3606016 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3605998 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3606018 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3605978 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3606008 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3606023 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3606017 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3606010 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3605996 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1329044 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3606014 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3606022 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3605986 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3605976 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL3605983 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL3606003 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3605967 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3606006 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3606001 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3606005 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3605997 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL3606007 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL3605999 | — | IC50 | > | 10000.0 | nM | - |