Assay Detail
Binding
CHEMBL2400732
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P110alpha (unknown origin) using L-a-phosphatidylinositol as substrate by luminescence assay
15
Total Activities
15
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 NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.47 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.30 |
| CHEMBL2397186 | — | — | 1 | 8.12 |
| CHEMBL2397196 | — | — | 1 | 8.02 |
| CHEMBL2397199 | — | — | 1 | 7.92 |
| CHEMBL2397187 | — | — | 1 | 7.85 |
| CHEMBL2397198 | — | — | 1 | 7.80 |
| CHEMBL2397193 | — | — | 1 | 7.80 |
| CHEMBL2397192 | — | — | 1 | 7.72 |
| CHEMBL2397191 | — | — | 1 | 7.72 |
| CHEMBL2397194 | — | — | 1 | 7.70 |
| CHEMBL2397197 | — | — | 1 | 7.41 |
| CHEMBL2397195 | — | — | 1 | 6.50 |
| CHEMBL2397189 | — | — | 1 | 6.21 |
| CHEMBL2397188 | — | — | 1 | 5.57 |
| CHEMBL2397190 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2397186 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2397196 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL2397199 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2397187 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2397198 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2397193 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2397192 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2397191 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2397194 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2397197 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2397195 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2397189 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2397188 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2397190 | — | IC50 | > | 9100.0 | nM | - |