Assay Detail
Binding
CHEMBL5152028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal 6His-6Lys-TEV tagged PARP1 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay
25
Total Activities
25
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 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 | 25 | 7.87 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874589 | — | — | 1 | 8.52 |
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 8.52 |
| CHEMBL5202060 | — | — | 1 | 8.40 |
| CHEMBL5188853 | — | — | 1 | 8.30 |
| CHEMBL5197101 | — | — | 1 | 8.30 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 8.15 |
| CHEMBL5190481 | — | — | 1 | 8.15 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.15 |
| CHEMBL5196187 | — | — | 1 | 8.10 |
| CHEMBL5183769 | — | — | 1 | 8.10 |
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.05 |
| CHEMBL5193246 | — | — | 1 | 8.05 |
| CHEMBL5191396 | — | — | 1 | 8.05 |
| CHEMBL5177596 | — | — | 1 | 8.05 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 7.89 |
| CHEMBL5200723 | — | — | 1 | 7.75 |
| CHEMBL5181905 | — | — | 1 | 7.54 |
| CHEMBL5195580 | — | — | 1 | 7.54 |
| CHEMBL5197824 | — | — | 1 | 7.52 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 7.46 |
| CHEMBL5178594 | — | — | 1 | 7.42 |
| CHEMBL5209181 | — | — | 1 | 7.29 |
| CHEMBL251030 | — | — | 1 | 7.19 |
| CHEMBL3606021 | — | — | 1 | 7.10 |
| CHEMBL5176615 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874589 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5095220 | SARUPARIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5202060 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5188853 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5197101 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5190481 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5196187 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5183769 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5193246 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5191396 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5177596 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5200723 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5181905 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5195580 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5197824 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5178594 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5209181 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL251030 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3606021 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5176615 | — | IC50 | = | 82.0 | nM | 7.09 |