Assay Detail
Binding
CHEMBL5152894
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP-1 (unknown origin) binding to DNA assessed as DNA trapping activity
28
Total Activities
28
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
Synthesis and in vitro biological evaluation of 3-ethyl-1,5-naphthyridin-2(1H)-one derivatives as potent PARP-1 selective inhibitors and PARP-1 DNA trappers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.56 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 9.19 |
| CHEMBL5178741 | — | — | 1 | 8.79 |
| CHEMBL5179882 | — | — | 1 | 8.73 |
| CHEMBL5193674 | — | — | 1 | 8.53 |
| CHEMBL5179448 | — | — | 1 | 8.45 |
| CHEMBL5191912 | — | — | 1 | 8.35 |
| CHEMBL5173989 | — | — | 1 | 8.32 |
| CHEMBL5176160 | — | — | 1 | 8.32 |
| CHEMBL5180001 | — | — | 1 | 8.09 |
| CHEMBL5196723 | — | — | 1 | 7.99 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 7.97 |
| CHEMBL5206717 | — | — | 1 | 7.95 |
| CHEMBL5205419 | — | — | 1 | 7.19 |
| CHEMBL5185063 | — | — | 1 | 6.80 |
| CHEMBL5190645 | — | — | 1 | 6.64 |
| CHEMBL5185548 | — | — | 1 | 6.61 |
| CHEMBL5202261 | — | — | 1 | 6.59 |
| CHEMBL5185522 | — | — | 1 | 6.42 |
| CHEMBL5201927 | — | — | 1 | 6.14 |
| CHEMBL5195834 | — | — | 1 | 5.84 |
| CHEMBL5187899 | — | — | 1 | 5.80 |
| CHEMBL5198072 | — | — | 1 | - |
| CHEMBL5176626 | — | — | 1 | - |
| CHEMBL5205409 | — | — | 1 | - |
| CHEMBL5191816 | — | — | 1 | - |
| CHEMBL5179279 | — | — | 1 | - |
| CHEMBL5208807 | — | — | 1 | - |
| CHEMBL5180063 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5095220 | SARUPARIB | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5178741 | — | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL5179882 | — | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL5193674 | — | IC50 | = | 2.97 | nM | 8.53 |
| CHEMBL5179448 | — | IC50 | = | 3.58 | nM | 8.45 |
| CHEMBL5191912 | — | IC50 | = | 4.51 | nM | 8.35 |
| CHEMBL5173989 | — | IC50 | = | 4.76 | nM | 8.32 |
| CHEMBL5176160 | — | IC50 | = | 4.783 | nM | 8.32 |
| CHEMBL5180001 | — | IC50 | = | 8.14 | nM | 8.09 |
| CHEMBL5196723 | — | IC50 | = | 10.36 | nM | 7.99 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 10.62 | nM | 7.97 |
| CHEMBL5206717 | — | IC50 | = | 11.25 | nM | 7.95 |
| CHEMBL5205419 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5185063 | — | IC50 | = | 158.1 | nM | 6.80 |
| CHEMBL5190645 | — | IC50 | = | 231.2 | nM | 6.64 |
| CHEMBL5185548 | — | IC50 | = | 243.8 | nM | 6.61 |
| CHEMBL5202261 | — | IC50 | = | 258.8 | nM | 6.59 |
| CHEMBL5185522 | — | IC50 | = | 380.1 | nM | 6.42 |
| CHEMBL5201927 | — | IC50 | = | 727.4 | nM | 6.14 |
| CHEMBL5195834 | — | IC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL5187899 | — | IC50 | = | 1575.0 | nM | 5.80 |
| CHEMBL5198072 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5176626 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5205409 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5191816 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5179279 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5208807 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL5180063 | — | IC50 | > | 2500.0 | nM | - |