Assay Detail
Functional
CHEMBL5520555
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Antiproliferative activity against BRCA2-deficient human HCT-116 cells assessed as inhibition of cell proliferation incubated for 5 days by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| 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 | 8 | 4.91 | 5.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5555891 | — | — | 1 | 5.21 |
| CHEMBL5564238 | — | — | 1 | 5.14 |
| CHEMBL5556723 | — | — | 1 | 5.08 |
| CHEMBL5558410 | — | — | 1 | 5.05 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 4.82 |
| CHEMBL5558738 | — | — | 1 | 4.75 |
| CHEMBL5566472 | — | — | 1 | 4.33 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5555891 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5564238 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5556723 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL5558410 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL5558738 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL5566472 | — | IC50 | = | 46300.0 | nM | 4.33 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | > | 80000.0 | nM | - |