Assay Detail
Binding
CHEMBL1925467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K subunit p110alpha assessed as formation of phosphatidylinositide-3-phosphate product formation after 30 mins by fluorescence polarization assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.62 | 9.15 |
| Ki | 1 | 8.55 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1922090 | — | — | 1 | 9.15 |
| CHEMBL1922092 | — | — | 1 | 9.00 |
| CHEMBL1922095 | — | — | 1 | 8.77 |
| CHEMBL1083192 | — | — | 1 | 8.70 |
| CHEMBL1922091 | — | — | 1 | 8.68 |
| CHEMBL1922093 | — | — | 1 | 8.55 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.52 |
| CHEMBL1091978 | — | — | 1 | 8.40 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.32 |
| CHEMBL1921986 | — | — | 1 | 8.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1922090 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1922092 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1922095 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1083192 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1922091 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1922093 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1091978 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1921986 | — | IC50 | = | 8.7 | nM | 8.06 |