Assay Detail
Binding
CHEMBL5132147
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Inhibition of human PARP2 using NAD+ as substrate incubated for 1 hr by ELISA
9
Total Activities
9
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
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.23 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 9.30 |
| CHEMBL5203682 | — | — | 1 | 8.54 |
| CHEMBL5182785 | — | — | 1 | 8.38 |
| CHEMBL5170407 | — | — | 1 | 8.24 |
| CHEMBL5183006 | — | — | 1 | 8.19 |
| CHEMBL5174694 | — | — | 1 | 8.18 |
| CHEMBL5193574 | — | — | 1 | 8.10 |
| CHEMBL5208255 | — | — | 1 | 7.95 |
| CHEMBL5197357 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5203682 | — | IC50 | = | 2.91 | nM | 8.54 |
| CHEMBL5182785 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL5170407 | — | IC50 | = | 5.71 | nM | 8.24 |
| CHEMBL5183006 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5174694 | — | IC50 | = | 6.68 | nM | 8.18 |
| CHEMBL5193574 | — | IC50 | = | 8.04 | nM | 8.10 |
| CHEMBL5208255 | — | IC50 | = | 11.21 | nM | 7.95 |
| CHEMBL5197357 | — | IC50 | = | 61.9 | nM | 7.21 |