Assay Detail
Binding
CHEMBL2383016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.26 | 9.22 |
| Ki | 2 | 9.06 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2381373 | — | — | 1 | 9.26 |
| CHEMBL2381271 | — | — | 1 | 9.22 |
| CHEMBL2381269 | — | — | 1 | 9.15 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.85 |
| CHEMBL2381379 | — | — | 1 | 8.85 |
| CHEMBL2381270 | — | — | 1 | 8.82 |
| CHEMBL2322764 | — | — | 1 | 8.66 |
| CHEMBL2381253 | — | — | 1 | 8.52 |
| CHEMBL2381265 | — | — | 1 | 8.46 |
| CHEMBL2381273 | — | — | 1 | 8.43 |
| CHEMBL2381266 | — | — | 1 | 8.37 |
| CHEMBL2381268 | — | — | 1 | 8.08 |
| CHEMBL2381261 | — | — | 1 | 8.08 |
| CHEMBL2381272 | — | — | 1 | 7.96 |
| CHEMBL2381262 | — | — | 1 | 7.72 |
| CHEMBL2381267 | — | — | 1 | 7.44 |
| CHEMBL2381263 | — | — | 1 | 7.26 |
| CHEMBL2381264 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2381373 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL2381271 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2381269 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL521851 | PICTILISIB | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2381379 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2381270 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2322764 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2381253 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2381265 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2381273 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2381266 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2381268 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2381261 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2381272 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2381262 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL2381267 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2381263 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2381264 | — | IC50 | = | 80.0 | nM | 7.10 |