Assay Detail
Binding
CHEMBL4131013
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Inhibition of PARP1 (unknown origin) by ELISA
42
Total Activities
42
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
Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 8.22 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169012 | — | — | 1 | 10.70 |
| CHEMBL4170665 | — | — | 1 | 10.00 |
| CHEMBL4159834 | — | — | 1 | 9.70 |
| CHEMBL4171279 | — | — | 1 | 9.40 |
| CHEMBL4169337 | — | — | 1 | 9.40 |
| CHEMBL4161414 | — | — | 1 | 9.30 |
| CHEMBL4167280 | — | — | 1 | 9.22 |
| CHEMBL4175790 | — | — | 1 | 9.10 |
| CHEMBL4162463 | — | — | 1 | 9.10 |
| CHEMBL4175142 | — | — | 1 | 9.05 |
| CHEMBL4160023 | — | — | 1 | 9.05 |
| CHEMBL4174093 | — | — | 1 | 8.89 |
| CHEMBL4161687 | — | — | 1 | 8.85 |
| CHEMBL4172321 | — | — | 1 | 8.68 |
| CHEMBL4167044 | — | — | 1 | 8.64 |
| CHEMBL4174278 | — | — | 1 | 8.62 |
| CHEMBL4165908 | — | — | 1 | 8.59 |
| CHEMBL4177196 | — | — | 1 | 8.54 |
| CHEMBL4173148 | — | — | 1 | 8.46 |
| CHEMBL4167934 | — | — | 1 | 8.38 |
| CHEMBL4163384 | — | — | 1 | 8.29 |
| CHEMBL4160677 | — | — | 1 | 8.27 |
| CHEMBL4163596 | — | — | 1 | 8.21 |
| CHEMBL4170845 | — | — | 1 | 8.15 |
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.14 |
| CHEMBL4176518 | — | — | 1 | 8.01 |
| CHEMBL4160236 | — | — | 1 | 7.95 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 7.72 |
| CHEMBL4159134 | — | — | 1 | 7.54 |
| CHEMBL4170490 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169012 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL4170665 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4159834 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4171279 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4169337 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4161414 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4167280 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4175790 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4162463 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4175142 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4160023 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4174093 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4161687 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4172321 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4167044 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4174278 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4165908 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4177196 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4173148 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4167934 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4163384 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4160677 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4163596 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4170845 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4176518 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4160236 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4159134 | — | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL4170490 | — | IC50 | = | 52.2 | nM | 7.28 |
| CHEMBL4172377 | — | IC50 | = | 55.8 | nM | 7.25 |
| CHEMBL4170242 | — | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL4162862 | — | IC50 | = | 83.4 | nM | 7.08 |
| CHEMBL4164827 | — | IC50 | = | 96.8 | nM | 7.01 |
| CHEMBL4170803 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4160600 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4165586 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL4172731 | — | IC50 | = | 156.7 | nM | 6.80 |
| CHEMBL4169021 | — | IC50 | = | 174.9 | nM | 6.76 |
| CHEMBL4176202 | — | IC50 | = | 296.6 | nM | 6.53 |
| CHEMBL4164499 | — | IC50 | = | 323.7 | nM | 6.49 |
| CHEMBL4161087 | — | IC50 | < | 0.1 | nM | - |