Assay Detail
Binding
CHEMBL3411220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kbeta in PTEN-null human MDA-MB-468 cells assessed as inhibition of Akt phosphorylation 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 | MDA-MB-468 |
| 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 (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 | 7.86 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408270 | — | — | 1 | 9.40 |
| CHEMBL3408252 | — | — | 1 | 9.00 |
| CHEMBL3408262 | — | — | 1 | 8.70 |
| CHEMBL3408263 | — | — | 1 | 8.70 |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | 8.52 |
| CHEMBL3408267 | — | — | 1 | 8.52 |
| CHEMBL3408257 | — | — | 1 | 8.22 |
| CHEMBL3408258 | — | — | 1 | 8.15 |
| CHEMBL3408245 | — | — | 1 | 8.05 |
| CHEMBL3408277 | — | — | 1 | 8.00 |
| CHEMBL3408271 | — | — | 1 | 7.92 |
| CHEMBL3408278 | — | — | 1 | 7.92 |
| CHEMBL3408256 | — | — | 1 | 7.89 |
| CHEMBL3408268 | — | — | 1 | 7.85 |
| CHEMBL3408264 | — | — | 1 | 7.85 |
| CHEMBL3408274 | — | — | 1 | 7.82 |
| CHEMBL3408260 | — | — | 1 | 7.82 |
| CHEMBL3408254 | — | — | 1 | 7.82 |
| CHEMBL3408261 | — | — | 1 | 7.80 |
| CHEMBL3408251 | — | — | 1 | 7.80 |
| CHEMBL3408259 | — | — | 1 | 7.77 |
| CHEMBL3408255 | — | — | 1 | 7.77 |
| CHEMBL3408247 | — | — | 1 | 7.77 |
| CHEMBL3408266 | — | — | 1 | 7.77 |
| CHEMBL3408250 | — | — | 1 | 7.70 |
| CHEMBL3408246 | — | — | 1 | 7.62 |
| CHEMBL3408269 | — | — | 1 | 7.51 |
| CHEMBL3407508 | — | — | 1 | 7.50 |
| CHEMBL3408265 | — | — | 1 | 7.48 |
| CHEMBL3408272 | — | — | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408270 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3408252 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3408263 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3408262 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3408248 | AZD-8186 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3408267 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3408257 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3408258 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3408245 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3408277 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3408271 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3408278 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3408256 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3408268 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3408264 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3408274 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3408254 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3408260 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3408261 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3408251 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3408259 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3408255 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3408247 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3408266 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3408250 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3408246 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3408269 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3407508 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3408265 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3408272 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3408273 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3408253 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3408249 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3408276 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3408244 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL3408275 | — | IC50 | = | 132.0 | nM | 6.88 |