Assay Detail
Binding
CHEMBL5519907
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured for 1 hr in presence of ATP by ADP-Glo assay
6
Total Activities
6
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 gamma isoform (CHEMBL3267) ↗| 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 | 6 | 7.71 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.30 |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | 7.79 |
| CHEMBL4297181 | SAMOTOLISIB | 2.0 | 1 | 7.62 |
| CHEMBL5170300 | — | — | 1 | 7.60 |
| CHEMBL3393066 | VS-5584 | 1.0 | 1 | 7.53 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3218576 | COPANLISIB | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL4297181 | SAMOTOLISIB | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL5170300 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3393066 | VS-5584 | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL3218578 | BGT-226 FREE BASE | IC50 | = | 38.0 | nM | 7.42 |