Assay Detail
Binding
CHEMBL2388269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay
14
Total Activities
14
Compounds Tested
2
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 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 9.34 | 9.96 |
| IC50 | 2 | 8.52 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386970 | — | — | 1 | 9.96 |
| CHEMBL2387079 | — | — | 1 | 9.85 |
| CHEMBL2387086 | — | — | 1 | 9.77 |
| CHEMBL2387080 | TASELISIB | 3.0 | 1 | 9.54 |
| CHEMBL2387082 | — | — | 1 | 9.54 |
| CHEMBL2386972 | — | — | 1 | 9.52 |
| CHEMBL2387081 | — | — | 1 | 9.51 |
| CHEMBL2386971 | — | — | 1 | 9.47 |
| CHEMBL2387083 | — | — | 1 | 9.40 |
| CHEMBL2387085 | — | — | 1 | 8.55 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.52 |
| CHEMBL2387084 | — | — | 1 | 7.68 |
| CHEMBL2387087 | — | — | 1 | - |
| CHEMBL2381373 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386970 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL2387079 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL2387086 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL2387080 | TASELISIB | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL2387082 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL2386972 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2387081 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL2386971 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2387083 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2387085 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2387084 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL2387087 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2381373 | — | IC50 | < | 0.5 | nM | - |