Assay Detail
Binding
CHEMBL5519905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured for 1 hr by HTRF assay
4
Total Activities
4
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 | 4 | 8.18 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | 8.85 |
| CHEMBL5170300 | — | — | 1 | 8.53 |
| CHEMBL3393066 | VS-5584 | 1.0 | 1 | 7.80 |
| CHEMBL4749655 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3218576 | COPANLISIB | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL5170300 | — | IC50 | = | 2.98 | nM | 8.53 |
| CHEMBL3393066 | VS-5584 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4749655 | — | IC50 | = | 28.0 | nM | 7.55 |