Assay Detail
Binding
CHEMBL5152893
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Inhibition of PARP-2 (unknown origin)
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 | 7.32 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 10.00 |
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 8.40 |
| CHEMBL5190645 | — | — | 1 | 8.28 |
| CHEMBL5193674 | — | — | 1 | 8.05 |
| CHEMBL5180001 | — | — | 1 | 7.75 |
| CHEMBL5198072 | — | — | 1 | 7.70 |
| CHEMBL5205419 | — | — | 1 | 7.68 |
| CHEMBL5185522 | — | — | 1 | 7.64 |
| CHEMBL5201927 | — | — | 1 | 7.42 |
| CHEMBL5202261 | — | — | 1 | 7.40 |
| CHEMBL5206717 | — | — | 1 | 7.38 |
| CHEMBL5185548 | — | — | 1 | 7.22 |
| CHEMBL5178741 | — | — | 1 | 7.17 |
| CHEMBL5196723 | — | — | 1 | 7.06 |
| CHEMBL5179882 | — | — | 1 | 6.88 |
| CHEMBL5195834 | — | — | 1 | 6.86 |
| CHEMBL5187899 | — | — | 1 | 6.82 |
| CHEMBL5191912 | — | — | 1 | 6.81 |
| CHEMBL5173989 | — | — | 1 | 6.72 |
| CHEMBL5179279 | — | — | 1 | 6.47 |
| CHEMBL5180063 | — | — | 1 | 6.35 |
| CHEMBL5176626 | — | — | 1 | 6.31 |
| CHEMBL5179448 | — | — | 1 | 6.01 |
| CHEMBL5185063 | — | — | 1 | - |
| CHEMBL5191816 | — | — | 1 | - |
| CHEMBL5176160 | — | — | 1 | - |
| CHEMBL5205409 | — | — | 1 | - |
| CHEMBL5208807 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5095220 | SARUPARIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5190645 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5193674 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5180001 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5198072 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5205419 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5185522 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5201927 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5202261 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5206717 | — | IC50 | = | 41.53 | nM | 7.38 |
| CHEMBL5185548 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5178741 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5196723 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5179882 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL5195834 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5187899 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5191912 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5173989 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5179279 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5180063 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5176626 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL5179448 | — | IC50 | = | 982.0 | nM | 6.01 |
| CHEMBL5185063 | — | IC50 | - | — | - | |
| CHEMBL5191816 | — | IC50 | - | — | - | |
| CHEMBL5176160 | — | IC50 | - | — | - | |
| CHEMBL5205409 | — | IC50 | - | — | - | |
| CHEMBL5208807 | — | IC50 | - | — | - |