Assay Detail
Binding
CHEMBL5329523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged human recombinant PARP-1 (1 to 1014 residues) expressed in Sf9 insect cells incubated for 1 hr by 32P-NAD+-based filter binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Hypoxia-activated prodrugs of phenolic olaparib analogues for tumour-selective chemosensitisation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.42 | 9.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5403789 | — | — | 1 | 9.76 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 9.39 |
| CHEMBL5411944 | — | — | 1 | 9.29 |
| CHEMBL5403607 | — | — | 1 | 8.57 |
| CHEMBL5440303 | — | — | 1 | 8.03 |
| CHEMBL5417243 | — | — | 1 | 8.01 |
| CHEMBL5400911 | — | — | 1 | 7.30 |
| CHEMBL5434068 | — | — | 1 | 6.97 |
| CHEMBL66761 | — | — | 1 | 6.86 |
| CHEMBL5405947 | — | — | 1 | 6.71 |
| CHEMBL5428478 | — | — | 1 | 6.02 |
| CHEMBL5431934 | — | — | 1 | 6.01 |
| CHEMBL5408263 | — | — | 1 | 5.68 |
| CHEMBL5430669 | — | — | 1 | 5.26 |
| CHEMBL5429884 | — | — | 1 | - |
| CHEMBL5417872 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5403789 | — | IC50 | = | 0.175 | nM | 9.76 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 0.411 | nM | 9.39 |
| CHEMBL5411944 | — | IC50 | = | 0.511 | nM | 9.29 |
| CHEMBL5403607 | — | IC50 | = | 2.66 | nM | 8.57 |
| CHEMBL5440303 | — | IC50 | = | 9.43 | nM | 8.03 |
| CHEMBL5417243 | — | IC50 | = | 9.76 | nM | 8.01 |
| CHEMBL5400911 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL5434068 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL66761 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5405947 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5428478 | — | IC50 | = | 948.0 | nM | 6.02 |
| CHEMBL5431934 | — | IC50 | = | 972.0 | nM | 6.01 |
| CHEMBL5408263 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5430669 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL5429884 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5417872 | — | IC50 | > | 100000.0 | nM | - |