Assay Detail
Binding
CHEMBL2383013
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Inhibition of PI3Kalpha in human PC3 cells assessed as inhibition of AKT phosphorylation at Ser473 after 2 hrs by ELISA
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| 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
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.14 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2381377 | — | — | 1 | 8.05 |
| CHEMBL2381381 | — | — | 1 | 8.00 |
| CHEMBL2381375 | — | — | 1 | 7.70 |
| CHEMBL2381275 | — | — | 1 | 7.68 |
| CHEMBL2381265 | — | — | 1 | 7.68 |
| CHEMBL2381376 | — | — | 1 | 7.66 |
| CHEMBL2381373 | — | — | 1 | 7.62 |
| CHEMBL2381266 | — | — | 1 | 7.62 |
| CHEMBL2381380 | — | — | 1 | 7.51 |
| CHEMBL2381274 | — | — | 1 | 7.43 |
| CHEMBL2381382 | — | — | 1 | 7.42 |
| CHEMBL2381374 | — | — | 1 | 7.33 |
| CHEMBL2381270 | — | — | 1 | 7.28 |
| CHEMBL2381278 | — | — | 1 | 7.27 |
| CHEMBL2381268 | — | — | 1 | 7.24 |
| CHEMBL2381277 | — | — | 1 | 7.17 |
| CHEMBL2381276 | — | — | 1 | 7.16 |
| CHEMBL2381273 | — | — | 1 | 7.15 |
| CHEMBL2381269 | — | — | 1 | 7.12 |
| CHEMBL2381271 | — | — | 1 | 7.08 |
| CHEMBL2381279 | — | — | 1 | 7.05 |
| CHEMBL2381378 | — | — | 1 | 7.05 |
| CHEMBL2381261 | — | — | 1 | 7.00 |
| CHEMBL2381379 | — | — | 1 | 6.91 |
| CHEMBL2322764 | — | — | 1 | 6.81 |
| CHEMBL2381253 | — | — | 1 | 6.80 |
| CHEMBL2381267 | — | — | 1 | 6.76 |
| CHEMBL2381251 | — | — | 1 | 6.75 |
| CHEMBL2381264 | — | — | 1 | 6.73 |
| CHEMBL2381252 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2381377 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2381381 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2381375 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2381275 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2381265 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2381376 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2381373 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2381266 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2381380 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2381274 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2381382 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2381374 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2381270 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2381278 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2381268 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2381277 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2381276 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2381273 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2381269 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2381271 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2381279 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2381378 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2381261 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2381379 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2322764 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2381253 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL2381267 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL2381251 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2381264 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL2381252 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL2381263 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL2381262 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL2381254 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL2381256 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2381260 | — | IC50 | - | — | - | |
| CHEMBL2381259 | — | IC50 | - | — | - | |
| CHEMBL2381258 | — | IC50 | - | — | - | |
| CHEMBL2381257 | — | IC50 | - | — | - | |
| CHEMBL2381255 | — | IC50 | - | — | - | |
| CHEMBL2381272 | — | IC50 | - | — | - |