Assay Detail
Binding
CHEMBL5731587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
p110alpha (Alpha) PI3K Binding Assay: PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is performed in the presence of PIP2:3PS lipid substrate (Promega #V1792) and ATP. Following the termination if the kinase reaction, turnover of ATP to ADP by the phosphorylation of the lipid substrate is detected using the Promega ADP-Glo (Promega #V1792) assay. ReactionFinal Kinase ATP PIP2:3PS TimeKinase Source Concentration (uM) (uM) (min.)PI3K alpha Millipore 0.2 nM 40 50 120#14-602-K PI3K beta Promega 0.6 nM 40 50 120#V1751 PI3K delta Millipore 0.25 nM 40 50 120#14-604-K PI3K gamma Millipore 0.4 nM 25 50 120#14-558-KAfter 120 minutes of reaction time, the kinase reaction is terminated. Any ATP remaining after the reaction is depleted, leaving only ADP. Then the Kinase Detection Reagent is added to convert ADP to ATP, which is used in a coupled luciferin/luciferase reaction. The luminescent output is measured and is correlated with kinase activity.
27
Total Activities
9
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 3-kinase regulatory subunit beta (CHEMBL4437) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Benzoxazepin oxazolidinone compounds and methods of use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.78 | 7.28 |
| kon | 9 | - | - |
| k_off | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2387080 | TASELISIB | 3.0 | 3 | 7.28 |
| CHEMBL521851 | PICTILISIB | 2.0 | 3 | 7.15 |
| CHEMBL4650215 | INAVOLISIB | 4.0 | 3 | 7.00 |
| CHEMBL5916599 | — | — | 3 | 6.91 |
| CHEMBL5789652 | — | — | 3 | 6.88 |
| CHEMBL5196718 | — | — | 3 | 6.47 |
| CHEMBL5186155 | — | — | 3 | 6.47 |
| CHEMBL5967979 | — | — | 3 | 6.09 |
| CHEMBL5748747 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2387080 | TASELISIB | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL521851 | PICTILISIB | Ki | = | 70.2 | nM | 7.15 |
| CHEMBL4650215 | INAVOLISIB | Ki | = | 99.7 | nM | 7.00 |
| CHEMBL5916599 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL5789652 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL5186155 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL5196718 | — | Ki | = | 335.0 | nM | 6.47 |
| CHEMBL5967979 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL2387080 | TASELISIB | kon | = | - | — | - |
| CHEMBL2387080 | TASELISIB | k_off | = | - | s-1 | - |
| CHEMBL521851 | PICTILISIB | kon | = | - | — | - |
| CHEMBL521851 | PICTILISIB | k_off | = | - | s-1 | - |
| CHEMBL4650215 | INAVOLISIB | kon | = | - | — | - |
| CHEMBL4650215 | INAVOLISIB | k_off | = | - | s-1 | - |
| CHEMBL5748747 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5748747 | — | kon | = | - | — | - |
| CHEMBL5748747 | — | k_off | = | - | s-1 | - |
| CHEMBL5196718 | — | k_off | = | - | s-1 | - |
| CHEMBL5967979 | — | kon | = | - | — | - |
| CHEMBL5967979 | — | k_off | = | - | s-1 | - |
| CHEMBL5186155 | — | kon | = | - | — | - |
| CHEMBL5186155 | — | k_off | = | - | s-1 | - |
| CHEMBL5916599 | — | kon | = | - | — | - |
| CHEMBL5916599 | — | k_off | = | - | s-1 | - |
| CHEMBL5789652 | — | kon | = | - | — | - |
| CHEMBL5789652 | — | k_off | = | - | s-1 | - |
| CHEMBL5196718 | — | kon | = | - | — | - |