Assay Detail
Binding
CHEMBL5737422
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Kinase Assay: The enzymatic activities against PI3K-α, PI3K-β, PI3K-γ and PI3K-δ were tested in ADAPTA assays. Activity against AURKB and AURKB were tested in Z′-Lyte assays. All assays were performed with ATP concentrations of Km for each kinase. BRD4_1 binding was tested using an AlphaScreen assay. All protocols are available from Life Technologies.
12
Total Activities
4
Compounds Tested
3
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrimido-diazepinone kinase scaffold compounds and methods for treating PI3K-mediated disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.96 | 7.28 |
| kon | 4 | - | - |
| k_off | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979343 | — | — | 3 | 7.28 |
| CHEMBL3959351 | — | — | 3 | 7.26 |
| CHEMBL3942643 | — | — | 3 | 7.16 |
| CHEMBL3898901 | — | — | 3 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979343 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3959351 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3942643 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3898901 | — | IC50 | = | 728.0 | nM | 6.14 |
| CHEMBL3979343 | — | kon | = | - | — | - |
| CHEMBL3979343 | — | k_off | = | - | s-1 | - |
| CHEMBL3898901 | — | kon | = | - | — | - |
| CHEMBL3898901 | — | k_off | = | - | s-1 | - |
| CHEMBL3942643 | — | kon | = | - | — | - |
| CHEMBL3942643 | — | k_off | = | - | s-1 | - |
| CHEMBL3959351 | — | kon | = | - | — | - |
| CHEMBL3959351 | — | k_off | = | - | s-1 | - |