Assay Detail
Binding
CHEMBL2343996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse PI3Kalpha
13
Total Activities
13
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-04979064 through Structure-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.06 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331668 | — | — | 1 | 9.72 |
| CHEMBL2331664 | — | — | 1 | 9.52 |
| CHEMBL2331669 | — | — | 1 | 9.40 |
| CHEMBL2331663 | — | — | 1 | 9.27 |
| CHEMBL2331661 | — | — | 1 | 9.27 |
| CHEMBL2331667 | — | — | 1 | 9.23 |
| CHEMBL2331666 | — | — | 1 | 9.04 |
| CHEMBL2331657 | — | — | 1 | 8.85 |
| CHEMBL2331662 | — | — | 1 | 8.71 |
| CHEMBL2331665 | — | — | 1 | 8.41 |
| CHEMBL2331660 | — | — | 1 | 8.24 |
| CHEMBL2331659 | — | — | 1 | - |
| CHEMBL2331658 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331668 | — | Ki | = | 0.191 | nM | 9.72 |
| CHEMBL2331664 | — | Ki | = | 0.299 | nM | 9.52 |
| CHEMBL2331669 | — | Ki | = | 0.395 | nM | 9.40 |
| CHEMBL2331663 | — | Ki | = | 0.532 | nM | 9.27 |
| CHEMBL2331661 | — | Ki | = | 0.542 | nM | 9.27 |
| CHEMBL2331667 | — | Ki | = | 0.584 | nM | 9.23 |
| CHEMBL2331666 | — | Ki | = | 0.922 | nM | 9.04 |
| CHEMBL2331657 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL2331662 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL2331665 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL2331660 | — | Ki | = | 5.69 | nM | 8.24 |
| CHEMBL2331659 | — | Ki | < | 0.5 | nM | - |
| CHEMBL2331658 | — | Ki | < | 0.5 | nM | - |