Assay Detail
Binding
CHEMBL1925471
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K subunit p110gamma assessed as formation of phosphatidylinositide-3-phosphate product formation after 30 mins by fluorescence polarization assay
7
Total Activities
7
Compounds Tested
1
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 gamma isoform (CHEMBL3267) ↗| 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 | 7 | 7.69 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1922093 | — | — | 1 | 8.00 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 7.85 |
| CHEMBL1922090 | — | — | 1 | 7.77 |
| CHEMBL1922092 | — | — | 1 | 7.70 |
| CHEMBL1922095 | — | — | 1 | 7.60 |
| CHEMBL1921986 | — | — | 1 | 7.48 |
| CHEMBL1922091 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1922093 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1922090 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1922092 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1922095 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1921986 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1922091 | — | IC50 | = | 37.0 | nM | 7.43 |