Assay Detail
Binding
CHEMBL4366243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal DYKDDDDK-tagged PI3Kgamma (1 to 1102 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.28 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4528675 | — | — | 1 | 7.66 |
| CHEMBL573339 | PI-103 | — | 1 | 7.19 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4528675 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL573339 | PI-103 | IC50 | = | 64.03 | nM | 7.19 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 104.2 | nM | 6.98 |