Assay Detail
Binding
CHEMBL4124224
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma in mouse RAW264 cells assessed as reduction in Akt phosphorylation at Ser473 residue preincubated for 15 mins followed by C5a stimulation measured after 3 mins by TR-FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL2189158) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.37 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127396 | — | — | 1 | 8.60 |
| CHEMBL4129600 | — | — | 1 | 8.30 |
| CHEMBL4126601 | — | — | 1 | 8.20 |
| CHEMBL4126445 | — | — | 1 | 8.20 |
| CHEMBL4126010 | — | — | 1 | 8.20 |
| CHEMBL4126156 | — | — | 1 | 8.10 |
| CHEMBL4128537 | — | — | 1 | 7.70 |
| CHEMBL4128230 | — | — | 1 | 7.70 |
| CHEMBL4129877 | — | — | 1 | 7.50 |
| CHEMBL4127833 | — | — | 1 | 7.40 |
| CHEMBL4129457 | — | — | 1 | 6.60 |
| CHEMBL4128652 | — | — | 1 | 6.40 |
| CHEMBL4130021 | — | — | 1 | 6.40 |
| CHEMBL4127414 | — | — | 1 | 6.20 |
| CHEMBL4128809 | — | — | 1 | 5.10 |
| CHEMBL4127150 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127396 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4129600 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4126601 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4126445 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4126010 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4126156 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4128537 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4128230 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4129877 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4127833 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4129457 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4128652 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4130021 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4127414 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4128809 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4127150 | — | IC50 | > | 1000.0 | nM | - |