Assay Detail
Binding
CHEMBL2061273
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse PI3Kalpha
12
Total Activities
12
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
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.93 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2057726 | — | — | 1 | 9.36 |
| CHEMBL2057725 | — | — | 1 | 8.81 |
| CHEMBL2057736 | — | — | 1 | 8.70 |
| CHEMBL2057727 | — | — | 1 | 8.43 |
| CHEMBL2057728 | — | — | 1 | 8.15 |
| CHEMBL2057735 | — | — | 1 | 8.00 |
| CHEMBL2057734 | — | — | 1 | 7.90 |
| CHEMBL2057731 | — | — | 1 | 7.87 |
| CHEMBL2057729 | — | — | 1 | 7.58 |
| CHEMBL2057730 | — | — | 1 | 7.44 |
| CHEMBL2057732 | — | — | 1 | 6.86 |
| CHEMBL2057733 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2057726 | — | Ki | = | 0.436 | nM | 9.36 |
| CHEMBL2057725 | — | Ki | = | 1.56 | nM | 8.81 |
| CHEMBL2057736 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2057727 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL2057728 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2057735 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2057734 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL2057731 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2057729 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2057730 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2057732 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL2057733 | — | Ki | = | 827.0 | nM | 6.08 |