Assay Detail
Binding
CHEMBL5099288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) by mobility shift assay
30
Total Activities
30
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.85 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.89 |
| CHEMBL5173125 | — | — | 1 | 7.60 |
| CHEMBL5187051 | — | — | 1 | 6.90 |
| CHEMBL5183646 | — | — | 1 | 6.80 |
| CHEMBL5179687 | — | — | 1 | 6.71 |
| CHEMBL5185319 | — | — | 1 | 6.56 |
| CHEMBL5202725 | — | — | 1 | 6.47 |
| CHEMBL5180796 | — | — | 1 | 6.43 |
| CHEMBL5170590 | — | — | 1 | 6.33 |
| CHEMBL5175778 | — | — | 1 | - |
| CHEMBL5202781 | — | — | 1 | - |
| CHEMBL5174437 | — | — | 1 | - |
| CHEMBL5191006 | — | — | 1 | - |
| CHEMBL5172866 | — | — | 1 | - |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL5188434 | — | — | 1 | - |
| CHEMBL5191376 | — | — | 1 | - |
| CHEMBL5172884 | — | — | 1 | - |
| CHEMBL5192044 | — | — | 1 | - |
| CHEMBL5204426 | — | — | 1 | - |
| CHEMBL5194733 | — | — | 1 | - |
| CHEMBL5206969 | — | — | 1 | - |
| CHEMBL5182660 | — | — | 1 | - |
| CHEMBL5184950 | — | — | 1 | - |
| CHEMBL5190763 | — | — | 1 | - |
| CHEMBL5186022 | — | — | 1 | - |
| CHEMBL5180870 | — | — | 1 | - |
| CHEMBL5201448 | — | — | 1 | - |
| CHEMBL5192159 | — | — | 1 | - |
| CHEMBL5171575 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5173125 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5187051 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5183646 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5179687 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL5185319 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL5202725 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL5180796 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL5170590 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL5175778 | — | IC50 | - | — | - | |
| CHEMBL5202781 | — | IC50 | - | — | - | |
| CHEMBL5174437 | — | IC50 | - | — | - | |
| CHEMBL5191006 | — | IC50 | - | — | - | |
| CHEMBL5172866 | — | IC50 | - | — | - | |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - | |
| CHEMBL5188434 | — | IC50 | - | — | - | |
| CHEMBL5191376 | — | IC50 | - | — | - | |
| CHEMBL5172884 | — | IC50 | - | — | - | |
| CHEMBL5192044 | — | IC50 | - | — | - | |
| CHEMBL5204426 | — | IC50 | - | — | - | |
| CHEMBL5194733 | — | IC50 | - | — | - | |
| CHEMBL5206969 | — | IC50 | - | — | - | |
| CHEMBL5182660 | — | IC50 | - | — | - | |
| CHEMBL5184950 | — | IC50 | - | — | - | |
| CHEMBL5190763 | — | IC50 | - | — | - | |
| CHEMBL5186022 | — | IC50 | - | — | - | |
| CHEMBL5180870 | — | IC50 | - | — | - | |
| CHEMBL5201448 | — | IC50 | - | — | - | |
| CHEMBL5192159 | — | IC50 | - | — | - | |
| CHEMBL5171575 | — | IC50 | - | — | - |