Assay Detail
Binding
CHEMBL3411217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PI3Kgamma using PIP2 by Kinase-Glo Plus assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 (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 | 5.88 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408270 | — | — | 1 | 6.85 |
| CHEMBL3408252 | — | — | 1 | 6.68 |
| CHEMBL3408267 | — | — | 1 | 6.60 |
| CHEMBL3408250 | — | — | 1 | 6.50 |
| CHEMBL3408262 | — | — | 1 | 6.46 |
| CHEMBL3408260 | — | — | 1 | 6.28 |
| CHEMBL3408269 | — | — | 1 | 6.28 |
| CHEMBL3408255 | — | — | 1 | 6.20 |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | 6.17 |
| CHEMBL3408263 | — | — | 1 | 6.16 |
| CHEMBL3408245 | — | — | 1 | 6.16 |
| CHEMBL3408268 | — | — | 1 | 6.15 |
| CHEMBL3408266 | — | — | 1 | 6.08 |
| CHEMBL3408258 | — | — | 1 | 6.03 |
| CHEMBL3408264 | — | — | 1 | 6.00 |
| CHEMBL3408261 | — | — | 1 | 5.92 |
| CHEMBL3408277 | — | — | 1 | 5.92 |
| CHEMBL3408273 | — | — | 1 | 5.85 |
| CHEMBL3408256 | — | — | 1 | 5.85 |
| CHEMBL3408257 | — | — | 1 | 5.82 |
| CHEMBL3408278 | — | — | 1 | 5.80 |
| CHEMBL3408254 | — | — | 1 | 5.80 |
| CHEMBL3408251 | — | — | 1 | 5.75 |
| CHEMBL3408253 | — | — | 1 | 5.66 |
| CHEMBL3408265 | — | — | 1 | 5.62 |
| CHEMBL3408247 | — | — | 1 | 5.60 |
| CHEMBL3408259 | — | — | 1 | 5.58 |
| CHEMBL3407508 | — | — | 1 | 5.58 |
| CHEMBL3408271 | — | — | 1 | 5.54 |
| CHEMBL3408272 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408270 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3408252 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3408267 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3408250 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3408262 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3408260 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3408269 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3408255 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3408248 | AZD-8186 | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL3408263 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3408245 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3408268 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3408266 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3408258 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3408264 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3408261 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3408277 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3408256 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3408273 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3408257 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3408278 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3408254 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3408251 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3408253 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3408265 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3408247 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3407508 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3408259 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3408271 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3408272 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3408274 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3408276 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3408246 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3408249 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3408275 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3408244 | — | IC50 | = | 13000.0 | nM | 4.89 |