Assay Detail
Binding
CHEMBL4832706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma in human U937 cells assessed as reduction in AKT phosphorylation preincubated for 30 mins followed by MIP1alpha stimulation for 3 mins by fluorescence analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| 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 Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.99 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4866794 | — | — | 1 | 8.15 |
| CHEMBL4864109 | — | — | 1 | 8.05 |
| CHEMBL4859017 | — | — | 1 | 7.82 |
| CHEMBL4855904 | — | — | 1 | 7.62 |
| CHEMBL4857826 | — | — | 1 | 7.55 |
| CHEMBL4850655 | — | — | 1 | 7.26 |
| CHEMBL4878811 | — | — | 1 | 7.21 |
| CHEMBL4867254 | — | — | 1 | 7.19 |
| CHEMBL4846278 | — | — | 1 | 6.96 |
| CHEMBL4878615 | — | — | 1 | 6.92 |
| CHEMBL4848126 | — | — | 1 | 6.85 |
| CHEMBL4849042 | — | — | 1 | 6.82 |
| CHEMBL4859466 | — | — | 1 | 6.82 |
| CHEMBL4861144 | — | — | 1 | 6.70 |
| CHEMBL4878721 | — | — | 1 | 6.62 |
| CHEMBL4857607 | — | — | 1 | 6.62 |
| CHEMBL4868011 | — | — | 1 | 6.46 |
| CHEMBL4857001 | — | — | 1 | 6.45 |
| CHEMBL4854845 | — | — | 1 | 6.40 |
| CHEMBL4873556 | — | — | 1 | 6.33 |
| CHEMBL2071342 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4866794 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4864109 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4859017 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4855904 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4857826 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4850655 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4878811 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4867254 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4846278 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4878615 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4848126 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4849042 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4859466 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4861144 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4878721 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4857607 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4868011 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4857001 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL4854845 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4873556 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2071342 | — | IC50 | = | 810.0 | nM | 6.09 |