Assay Detail
Binding
CHEMBL5155268
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma in SDF-1alpha stimulated human whole blood assessed as reduction in phospho-AKT kinase activity preincubated for 1 hr followed by SDF-1alpha stimulation and measured after 2 mins by flow cytometric analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.29 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5172719 | — | — | 1 | 6.68 |
| CHEMBL5196935 | — | — | 1 | 6.62 |
| CHEMBL5171421 | — | — | 1 | 6.58 |
| CHEMBL5209268 | — | — | 1 | 6.52 |
| CHEMBL5206549 | — | — | 1 | 6.38 |
| CHEMBL5203289 | — | — | 1 | 6.29 |
| CHEMBL5176293 | — | — | 1 | 6.22 |
| CHEMBL5201929 | — | — | 1 | 6.22 |
| CHEMBL5205997 | — | — | 1 | 6.12 |
| CHEMBL5186453 | — | — | 1 | 6.10 |
| CHEMBL5189490 | — | — | 1 | 5.89 |
| CHEMBL5177397 | — | — | 1 | 5.89 |
| CHEMBL5171703 | — | — | 1 | - |
| CHEMBL5179088 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5172719 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5196935 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5171421 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5209268 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5206549 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5203289 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5176293 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5201929 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5205997 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5186453 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5189490 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5177397 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5171703 | — | IC50 | - | — | - | |
| CHEMBL5179088 | — | IC50 | - | — | - |