Assay Detail
Functional
CHEMBL5152032
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
21
Total Activities
21
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
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-<i>N</i>-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.43 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196187 | — | — | 1 | 9.00 |
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 8.70 |
| CHEMBL4874589 | — | — | 1 | 8.70 |
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.70 |
| CHEMBL5197101 | — | — | 1 | 8.52 |
| CHEMBL5181905 | — | — | 1 | 8.52 |
| CHEMBL5188853 | — | — | 1 | 8.40 |
| CHEMBL5200723 | — | — | 1 | 8.15 |
| CHEMBL5197824 | — | — | 1 | 7.82 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 7.57 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 7.38 |
| CHEMBL5209181 | — | — | 1 | 7.28 |
| CHEMBL5176615 | — | — | 1 | 6.92 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 6.83 |
| CHEMBL5193246 | — | — | 1 | 6.75 |
| CHEMBL5202060 | — | — | 1 | 6.53 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 6.12 |
| CHEMBL3606021 | — | — | 1 | 5.70 |
| CHEMBL5183769 | — | — | 1 | 5.60 |
| CHEMBL5195580 | — | — | 1 | 5.36 |
| CHEMBL251030 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196187 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5095220 | SARUPARIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4874589 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5197101 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5181905 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5188853 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5200723 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5197824 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5209181 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5176615 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5193246 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5202060 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3606021 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5183769 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5195580 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL251030 | — | IC50 | > | 23000.0 | nM | - |