Assay Detail
Binding
CHEMBL3227714
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse PI3K alpha expressed in insect cells coexpressing p85 subunit assessed as PI(3,4,5)P3 formation using PI(4,5)P2 as substrate by measuring displacement of TAMRA-labeled PI(3,4,5)P3 from Grip1 PH domain after 35 mins by ligand displacement fluorescence polarization assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL2499) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.78 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | 9.24 |
| CHEMBL3218402 | — | — | 1 | 9.05 |
| CHEMBL3218401 | — | — | 1 | 8.96 |
| CHEMBL3218943 | — | — | 1 | 8.92 |
| CHEMBL1234353 | — | — | 1 | 8.85 |
| CHEMBL2057725 | — | — | 1 | 8.85 |
| CHEMBL3218403 | — | — | 1 | 8.52 |
| CHEMBL3218404 | — | — | 1 | 8.44 |
| CHEMBL3218405 | — | — | 1 | 8.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1234354 | PF-04691502 | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL3218402 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3218401 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3218943 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1234353 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2057725 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3218403 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3218404 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3218405 | — | Ki | = | 6.6 | nM | 8.18 |