Assay Detail
Binding
CHEMBL881278
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In vitro inhibitory concentration against Poly(ADP-ribose) polymerase 1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.78 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195758 | — | — | 1 | 8.05 |
| CHEMBL198355 | — | — | 1 | 7.80 |
| CHEMBL193336 | — | — | 1 | 7.70 |
| CHEMBL194535 | — | — | 1 | 7.64 |
| CHEMBL194482 | — | — | 1 | 7.34 |
| CHEMBL425201 | — | — | 1 | 7.19 |
| CHEMBL372303 | PJ34 | — | 1 | 6.96 |
| CHEMBL194684 | — | — | 1 | 6.92 |
| CHEMBL196504 | — | — | 1 | 6.92 |
| CHEMBL197469 | — | — | 1 | 6.70 |
| CHEMBL370207 | — | — | 1 | 6.60 |
| CHEMBL198230 | — | — | 1 | 6.56 |
| CHEMBL194416 | — | — | 1 | 6.33 |
| CHEMBL193679 | — | — | 1 | 6.30 |
| CHEMBL373210 | — | — | 1 | 6.02 |
| CHEMBL198422 | — | — | 1 | 5.21 |
| CHEMBL370171 | — | — | 1 | 5.07 |
| CHEMBL194404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195758 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL198355 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL193336 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL194535 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL194482 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL425201 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL372303 | PJ34 | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL194684 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL196504 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL197469 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL370207 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL198230 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL194416 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL193679 | — | IC50 | = | 495.0 | nM | 6.30 |
| CHEMBL373210 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL198422 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL370171 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL194404 | — | IC50 | > | 10000.0 | nM | - |