Assay Detail
Functional
CHEMBL5152897
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Antiproliferative activity against human DLD-1 cells harbouring wild type BRCA assessed as inhibition of cell growth
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | DLD-1 |
| Confidence | 1 — Organism |
| 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 | 12 | 4.66 | 5.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5180001 | — | — | 1 | 5.53 |
| CHEMBL5179448 | — | — | 1 | 5.06 |
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 4.92 |
| CHEMBL5191912 | — | — | 1 | 4.82 |
| CHEMBL5176160 | — | — | 1 | 4.80 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 4.63 |
| CHEMBL5193674 | — | — | 1 | 4.55 |
| CHEMBL5206717 | — | — | 1 | 4.48 |
| CHEMBL5179882 | — | — | 1 | 4.36 |
| CHEMBL5195834 | — | — | 1 | 4.11 |
| CHEMBL5173989 | — | — | 1 | 4.05 |
| CHEMBL5178741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5180001 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL5179448 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL5095220 | SARUPARIB | IC50 | = | 12060.0 | nM | 4.92 |
| CHEMBL5191912 | — | IC50 | = | 15210.0 | nM | 4.82 |
| CHEMBL5176160 | — | IC50 | = | 15650.0 | nM | 4.80 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 23326.0 | nM | 4.63 |
| CHEMBL5193674 | — | IC50 | = | 28060.0 | nM | 4.55 |
| CHEMBL5206717 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5179882 | — | IC50 | = | 43750.0 | nM | 4.36 |
| CHEMBL5195834 | — | IC50 | = | 77130.0 | nM | 4.11 |
| CHEMBL5173989 | — | IC50 | = | 89190.0 | nM | 4.05 |
| CHEMBL5178741 | — | IC50 | = | 102500.0 | nM | - |