Assay Detail
Binding
CHEMBL2383018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP
33
Total Activities
32
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 beta isoform (CHEMBL3145) ↗| 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 | 32 | 8.04 | 9.05 |
| Ki | 1 | 7.82 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2381265 | — | — | 1 | 9.05 |
| CHEMBL2381382 | — | — | 1 | 8.74 |
| CHEMBL2381375 | — | — | 1 | 8.74 |
| CHEMBL2381376 | — | — | 1 | 8.62 |
| CHEMBL2381266 | — | — | 1 | 8.41 |
| CHEMBL2381381 | — | — | 1 | 8.41 |
| CHEMBL2381275 | — | — | 1 | 8.40 |
| CHEMBL2381274 | — | — | 1 | 8.34 |
| CHEMBL2381267 | — | — | 1 | 8.27 |
| CHEMBL2381253 | — | — | 1 | 8.26 |
| CHEMBL2381378 | — | — | 1 | 8.15 |
| CHEMBL2381377 | — | — | 1 | 8.13 |
| CHEMBL2381277 | — | — | 1 | 8.12 |
| CHEMBL2381269 | — | — | 1 | 8.10 |
| CHEMBL2381268 | — | — | 1 | 8.08 |
| CHEMBL2381373 | — | — | 2 | 8.07 |
| CHEMBL2381276 | — | — | 1 | 8.07 |
| CHEMBL2381380 | — | — | 1 | 8.04 |
| CHEMBL2381271 | — | — | 1 | 8.03 |
| CHEMBL2381273 | — | — | 1 | 7.89 |
| CHEMBL2381278 | — | — | 1 | 7.89 |
| CHEMBL2381279 | — | — | 1 | 7.85 |
| CHEMBL2381374 | — | — | 1 | 7.85 |
| CHEMBL2381379 | — | — | 1 | 7.82 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 7.77 |
| CHEMBL2381264 | — | — | 1 | 7.76 |
| CHEMBL2381261 | — | — | 1 | 7.69 |
| CHEMBL2322764 | — | — | 1 | 7.54 |
| CHEMBL2381270 | — | — | 1 | 7.49 |
| CHEMBL2381262 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2381265 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2381382 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2381375 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2381376 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2381266 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL2381381 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL2381275 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2381274 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2381267 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2381253 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2381378 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2381377 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2381277 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL2381269 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2381268 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2381276 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL2381373 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2381380 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL2381271 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL2381278 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2381273 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2381279 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2381374 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2381373 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2381379 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2381264 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL2381261 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL2322764 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2381270 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL2381262 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL2381263 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2381272 | — | IC50 | = | 77.0 | nM | 7.11 |