Assay Detail
Binding
CHEMBL5519922
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Inhibition of His-tagged PI3Kalpha (unknown origin) in the presence of ATP by kinase hotspot assay
2
Total Activities
2
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
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.44 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5173125 | — | — | 1 | 7.60 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5173125 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 52.0 | nM | 7.28 |