Assay Detail
Binding
CHEMBL4817099
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Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 40 mins by ADP-glo plus luminescence assay
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 | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.59 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868231 | — | — | 1 | 9.29 |
| CHEMBL4871210 | — | — | 1 | 9.22 |
| CHEMBL4865059 | — | — | 1 | 8.82 |
| CHEMBL4858564 | — | — | 1 | 8.70 |
| CHEMBL4861171 | — | — | 1 | 8.64 |
| CHEMBL4848869 | — | — | 1 | 8.43 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.30 |
| CHEMBL4875356 | — | — | 1 | 8.15 |
| CHEMBL4859306 | — | — | 1 | 7.85 |
| CHEMBL4856241 | — | — | 1 | 6.78 |
| CHEMBL4868711 | — | — | 1 | 6.50 |
| CHEMBL4848908 | — | — | 1 | 5.94 |
| CHEMBL4859625 | — | — | 1 | 5.93 |
| CHEMBL4853655 | — | — | 1 | 5.86 |
| CHEMBL4874038 | — | — | 1 | 5.42 |
| CHEMBL4865897 | — | — | 1 | - |
| CHEMBL4848360 | — | — | 1 | - |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868231 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4871210 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4865059 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4858564 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4861171 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4848869 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4875356 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4859306 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4856241 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4868711 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4848908 | — | IC50 | = | 1142.0 | nM | 5.94 |
| CHEMBL4859625 | — | IC50 | = | 1176.0 | nM | 5.93 |
| CHEMBL4853655 | — | IC50 | = | 1381.0 | nM | 5.86 |
| CHEMBL4874038 | — | IC50 | = | 3806.0 | nM | 5.42 |
| CHEMBL4865897 | — | IC50 | - | — | - | |
| CHEMBL4848360 | — | IC50 | - | — | - | |
| CHEMBL521686 | OLAPARIB | IC50 | - | — | - |