Assay Detail
Binding
CHEMBL3606198
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P110alpha (unknown origin) by Kinase-Glo assay
3
Total Activities
3
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 a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.11 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.30 |
| CHEMBL3605177 | — | — | 1 | 8.30 |
| CHEMBL3605178 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3605177 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3605178 | — | IC50 | = | 19.0 | nM | 7.72 |