Assay Detail
Binding
CHEMBL2328239
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Inhibition of PI3Kalpha (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.38 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 8.22 |
| CHEMBL1910989 | — | — | 1 | 6.54 |
| CHEMBL2323114 | — | — | 1 | 6.43 |
| CHEMBL2323117 | — | — | 1 | 6.37 |
| CHEMBL2323116 | — | — | 1 | 6.08 |
| CHEMBL2323119 | — | — | 1 | 5.98 |
| CHEMBL2323115 | — | — | 1 | 5.04 |
| CHEMBL2323113 | — | — | 1 | - |
| CHEMBL2323118 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL586702 | ZSTK-474 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1910989 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2323114 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL2323117 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL2323116 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL2323119 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2323115 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2323113 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2323118 | — | IC50 | > | 10000.0 | nM | - |