Assay Detail
Binding
CHEMBL3411219
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha mutant human BT474 cells assessed as inhibition of Akt phosphorylation at Tyr-308 after 2 hrs
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BT-474 |
| 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 (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.67 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408270 | — | — | 1 | 6.96 |
| CHEMBL3408252 | — | — | 1 | 6.77 |
| CHEMBL3408262 | — | — | 1 | 6.55 |
| CHEMBL3408263 | — | — | 1 | 6.40 |
| CHEMBL3408250 | — | — | 1 | 6.30 |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | 6.12 |
| CHEMBL3408245 | — | — | 1 | 6.10 |
| CHEMBL3408273 | — | — | 1 | 6.07 |
| CHEMBL3408257 | — | — | 1 | 6.05 |
| CHEMBL3408267 | — | — | 1 | 6.02 |
| CHEMBL3408256 | — | — | 1 | 5.82 |
| CHEMBL3408254 | — | — | 1 | 5.77 |
| CHEMBL3408255 | — | — | 1 | 5.72 |
| CHEMBL3408258 | — | — | 1 | 5.68 |
| CHEMBL3408246 | — | — | 1 | 5.66 |
| CHEMBL3407508 | — | — | 1 | 5.62 |
| CHEMBL3408247 | — | — | 1 | 5.60 |
| CHEMBL3408259 | — | — | 1 | 5.58 |
| CHEMBL3408271 | — | — | 1 | 5.58 |
| CHEMBL3408253 | — | — | 1 | 5.54 |
| CHEMBL3408268 | — | — | 1 | 5.54 |
| CHEMBL3408274 | — | — | 1 | 5.52 |
| CHEMBL3408264 | — | — | 1 | 5.51 |
| CHEMBL3408261 | — | — | 1 | 5.50 |
| CHEMBL3408272 | — | — | 1 | 5.50 |
| CHEMBL3408277 | — | — | 1 | 5.33 |
| CHEMBL3408278 | — | — | 1 | 5.32 |
| CHEMBL3408251 | — | — | 1 | 5.26 |
| CHEMBL3408276 | — | — | 1 | 5.23 |
| CHEMBL3408265 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408270 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3408252 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3408262 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3408263 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3408250 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3408248 | AZD-8186 | IC50 | = | 752.0 | nM | 6.12 |
| CHEMBL3408245 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3408273 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3408257 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3408267 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3408256 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3408254 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3408255 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3408258 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3408246 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3407508 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3408247 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3408271 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3408259 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3408253 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3408268 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3408274 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3408264 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3408261 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3408272 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3408277 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3408278 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3408251 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3408276 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3408265 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3408266 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3408260 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3408249 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3408275 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3408244 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL3408269 | — | IC50 | = | 13000.0 | nM | 4.89 |