Assay Detail
Binding
CHEMBL4432790
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Inhibition of PARP-1 (unknown origin) after 1 hr in presence of NAD+/biotinylated NAD+/slDNA by ELISA
17
Total Activities
17
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
Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.51 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 8.96 |
| CHEMBL4460350 | — | — | 1 | 7.96 |
| CHEMBL4458889 | — | — | 1 | 7.89 |
| CHEMBL4590570 | — | — | 1 | 7.72 |
| CHEMBL4545981 | — | — | 1 | 7.70 |
| CHEMBL4522170 | — | — | 1 | 7.70 |
| CHEMBL4454541 | — | — | 1 | 7.68 |
| CHEMBL4435879 | — | — | 1 | 7.55 |
| CHEMBL4592544 | — | — | 1 | 7.55 |
| CHEMBL4563153 | — | — | 1 | 7.54 |
| CHEMBL4447860 | — | — | 1 | 7.27 |
| CHEMBL4454690 | — | — | 1 | 7.24 |
| CHEMBL4459573 | — | — | 1 | 7.12 |
| CHEMBL4463611 | — | — | 1 | 7.04 |
| CHEMBL4515565 | — | — | 1 | 6.99 |
| CHEMBL4458372 | — | — | 1 | 6.96 |
| CHEMBL4570886 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL506871 | VELIPARIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4460350 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4458889 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4590570 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4545981 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4522170 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4454541 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4435879 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4592544 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4563153 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4447860 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4454690 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4459573 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4463611 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4515565 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4458372 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4570886 | — | IC50 | = | 139.0 | nM | 6.86 |