Assay Detail
Binding
CHEMBL952237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP1 in human HeLa cells by fluid scintillation counting using [adenylated-32P]NAD as substrate
23
Total Activities
23
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
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.99 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455590 | — | — | 1 | 8.66 |
| CHEMBL148173 | — | — | 1 | 8.30 |
| CHEMBL497571 | — | — | 1 | 8.16 |
| CHEMBL525167 | — | — | 1 | 8.14 |
| CHEMBL372303 | PJ34 | — | 1 | 7.70 |
| CHEMBL508796 | — | — | 1 | 7.53 |
| CHEMBL131820 | — | — | 1 | 7.22 |
| CHEMBL446861 | — | — | 1 | 7.03 |
| CHEMBL496937 | — | — | 1 | 6.97 |
| CHEMBL497591 | — | — | 1 | 6.96 |
| CHEMBL506109 | — | — | 1 | 6.83 |
| CHEMBL125200 | — | — | 1 | 6.80 |
| CHEMBL497592 | — | — | 1 | 6.37 |
| CHEMBL522056 | — | — | 1 | 6.29 |
| CHEMBL505159 | — | — | 1 | 5.74 |
| CHEMBL525534 | — | — | 1 | 5.16 |
| CHEMBL497774 | — | — | 1 | 5.01 |
| CHEMBL497775 | — | — | 1 | - |
| CHEMBL498585 | — | — | 1 | - |
| CHEMBL496112 | — | — | 1 | - |
| CHEMBL522908 | — | — | 1 | - |
| CHEMBL497382 | — | — | 1 | - |
| CHEMBL447363 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455590 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL148173 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL497571 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL525167 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL372303 | PJ34 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL508796 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL131820 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL446861 | — | IC50 | = | 92.7 | nM | 7.03 |
| CHEMBL496937 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL497591 | — | IC50 | = | 110.3 | nM | 6.96 |
| CHEMBL506109 | — | IC50 | = | 148.6 | nM | 6.83 |
| CHEMBL125200 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL497592 | — | IC50 | = | 428.1 | nM | 6.37 |
| CHEMBL522056 | — | IC50 | = | 519.2 | nM | 6.29 |
| CHEMBL505159 | — | IC50 | = | 1841.5 | nM | 5.74 |
| CHEMBL525534 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL497774 | — | IC50 | = | 9720.0 | nM | 5.01 |
| CHEMBL497775 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL498585 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL496112 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL522908 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL497382 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL447363 | — | IC50 | > | 10000.0 | nM | - |