Assay Detail
Binding
CHEMBL3119744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.25 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3112858 | — | — | 1 | 6.00 |
| CHEMBL3112849 | — | — | 1 | 5.95 |
| CHEMBL3112855 | — | — | 1 | 5.82 |
| CHEMBL3112847 | — | — | 1 | 5.80 |
| CHEMBL3112851 | — | — | 1 | 5.75 |
| CHEMBL3112857 | — | — | 1 | 5.61 |
| CHEMBL3112867 | — | — | 1 | 5.48 |
| CHEMBL3112850 | — | — | 1 | 5.40 |
| CHEMBL3112848 | — | — | 1 | 5.21 |
| CHEMBL3112854 | — | — | 1 | 5.13 |
| CHEMBL3112853 | — | — | 1 | 5.08 |
| CHEMBL3112856 | — | — | 1 | 5.05 |
| CHEMBL3112862 | — | — | 1 | 5.04 |
| CHEMBL3112592 | — | — | 1 | 5.00 |
| CHEMBL3112690 | — | — | 1 | 5.00 |
| CHEMBL2064330 | — | — | 1 | 5.00 |
| CHEMBL1972466 | — | — | 1 | 5.00 |
| CHEMBL3112852 | — | — | 1 | 5.00 |
| CHEMBL3112859 | — | — | 1 | 5.00 |
| CHEMBL3112860 | — | — | 1 | 5.00 |
| CHEMBL3112861 | — | — | 1 | 5.00 |
| CHEMBL3112863 | — | — | 1 | 5.00 |
| CHEMBL3112864 | — | — | 1 | 5.00 |
| CHEMBL3112865 | — | — | 1 | 5.00 |
| CHEMBL3112866 | SAR-260301 | 1.0 | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3112858 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3112849 | — | IC50 | = | 1131.0 | nM | 5.95 |
| CHEMBL3112855 | — | IC50 | = | 1532.0 | nM | 5.82 |
| CHEMBL3112847 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL3112851 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL3112857 | — | IC50 | = | 2461.0 | nM | 5.61 |
| CHEMBL3112867 | — | IC50 | = | 3315.0 | nM | 5.48 |
| CHEMBL3112850 | — | IC50 | = | 3975.0 | nM | 5.40 |
| CHEMBL3112848 | — | IC50 | = | 6215.0 | nM | 5.21 |
| CHEMBL3112854 | — | IC50 | = | 7418.0 | nM | 5.13 |
| CHEMBL3112853 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3112856 | — | IC50 | = | 8966.0 | nM | 5.05 |
| CHEMBL3112862 | — | IC50 | = | 9149.0 | nM | 5.04 |
| CHEMBL3112592 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112690 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2064330 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1972466 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112852 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112859 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112860 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112861 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112863 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112864 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112865 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3112866 | SAR-260301 | IC50 | = | 10000.0 | nM | 5.00 |