Assay Detail
Binding
CHEMBL5521717
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Inhibition of PARP1 (unknown origin) using histone as substrate incubated for 45 mins by absorbance based analysis
16
Total Activities
16
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
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.37 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5562332 | — | — | 1 | 9.92 |
| CHEMBL5566491 | — | — | 1 | 9.05 |
| CHEMBL5550003 | — | — | 1 | 8.96 |
| CHEMBL5567666 | — | — | 1 | 8.96 |
| CHEMBL5542393 | — | — | 1 | 8.68 |
| CHEMBL5567210 | — | — | 1 | 8.48 |
| CHEMBL5561784 | — | — | 1 | 8.43 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.37 |
| CHEMBL5560815 | — | — | 1 | 8.33 |
| CHEMBL5560235 | — | — | 1 | 8.24 |
| CHEMBL5555264 | — | — | 1 | 8.15 |
| CHEMBL5566081 | — | — | 1 | 8.14 |
| CHEMBL5556439 | — | — | 1 | 7.49 |
| CHEMBL5559117 | — | — | 1 | 7.38 |
| CHEMBL5568564 | — | — | 1 | 7.04 |
| CHEMBL5560130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5562332 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5566491 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5550003 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5567666 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5542393 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5567210 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5561784 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5560815 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5560235 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5555264 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5566081 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5556439 | — | IC50 | = | 32.2 | nM | 7.49 |
| CHEMBL5559117 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5568564 | — | IC50 | = | 91.7 | nM | 7.04 |
| CHEMBL5560130 | — | IC50 | > | 1000.0 | nM | - |