Assay Detail
Binding
CHEMBL5123647
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Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate incubated for 45 mins in the presence of deoxy-oligonucleotide by microplate reader method relative to control
10
Total Activities
10
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, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.99 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5176874 | — | — | 1 | 9.60 |
| CHEMBL5174780 | — | — | 1 | 9.31 |
| CHEMBL5179949 | — | — | 1 | 9.01 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 9.00 |
| CHEMBL5189723 | — | — | 1 | 8.81 |
| CHEMBL5172909 | — | — | 1 | 8.79 |
| CHEMBL5174447 | — | — | 1 | 8.39 |
| CHEMBL5197830 | — | — | 1 | - |
| CHEMBL5185706 | — | — | 1 | - |
| CHEMBL5191145 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5176874 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5174780 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL5179949 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5189723 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL5172909 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL5174447 | — | IC50 | = | 4.08 | nM | 8.39 |
| CHEMBL5197830 | — | IC50 | - | — | - | |
| CHEMBL5185706 | — | IC50 | - | — | - | |
| CHEMBL5191145 | — | IC50 | - | — | - |