Assay Detail
Binding
CHEMBL5520550
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Inhibition of DNA polymerase theta (unknown origin) ATPase activity incubated for 60 mins in presence of ATP by ADP-glo kinase assay
17
Total Activities
17
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 and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.92 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566472 | — | — | 1 | 8.62 |
| CHEMBL5558410 | — | — | 1 | 7.34 |
| CHEMBL5555891 | — | — | 1 | 7.22 |
| CHEMBL5556723 | — | — | 1 | 7.14 |
| CHEMBL5564238 | — | — | 1 | 7.10 |
| CHEMBL5558738 | — | — | 1 | 6.93 |
| CHEMBL5556040 | — | — | 1 | 6.78 |
| CHEMBL5555002 | — | — | 1 | 6.57 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | 4.61 |
| CHEMBL5562278 | — | — | 1 | - |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | - |
| CHEMBL5558038 | — | — | 1 | - |
| CHEMBL5564092 | — | — | 1 | - |
| CHEMBL5556293 | — | — | 1 | - |
| CHEMBL5559805 | — | — | 1 | - |
| CHEMBL5567364 | — | — | 1 | - |
| CHEMBL5558560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566472 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5558410 | — | IC50 | = | 45.6 | nM | 7.34 |
| CHEMBL5555891 | — | IC50 | = | 59.8 | nM | 7.22 |
| CHEMBL5556723 | — | IC50 | = | 71.9 | nM | 7.14 |
| CHEMBL5564238 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL5558738 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5556040 | — | IC50 | = | 166.2 | nM | 6.78 |
| CHEMBL5555002 | — | IC50 | = | 268.2 | nM | 6.57 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL5562278 | — | IC50 | - | — | - | |
| CHEMBL521686 | OLAPARIB | IC50 | - | — | - | |
| CHEMBL5558038 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5564092 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5556293 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5559805 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5567364 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5558560 | — | IC50 | > | 1000.0 | nM | - |