Assay Detail
Binding
CHEMBL3816166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant PI3Kalpha (unknown origin) using dioctanoylglycerol-PIP2 as substrate incubated for 30 mins in presence of TAMRA-PIP3 by fluorescence polarization assay
11
Total Activities
11
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 Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.51 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178606 | — | — | 1 | 9.00 |
| CHEMBL3813842 | PAXALISIB | 2.0 | 1 | 8.70 |
| CHEMBL3814414 | — | — | 1 | 8.70 |
| CHEMBL2178608 | — | — | 1 | 8.70 |
| CHEMBL3814925 | — | — | 1 | 8.52 |
| CHEMBL3814544 | — | — | 1 | 8.52 |
| CHEMBL3813906 | — | — | 1 | 8.52 |
| CHEMBL3815084 | — | — | 1 | 8.30 |
| CHEMBL3814365 | — | — | 1 | 8.30 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.30 |
| CHEMBL3814933 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178606 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3813842 | PAXALISIB | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3814414 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2178608 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3814925 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3814544 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3813906 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3815084 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3814365 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1922094 | APITOLISIB | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3814933 | — | Ki | = | 10.0 | nM | 8.00 |