Assay Detail
Binding
CHEMBL3366869
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PI3Kgamma assessed as depletion of ATP substrate by Ultra Glo luciferase assay
6
Total Activities
6
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 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.54 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3319490 | — | — | 1 | 6.29 |
| CHEMBL3319485 | — | — | 1 | 6.17 |
| CHEMBL3319489 | — | — | 1 | 5.52 |
| CHEMBL3318711 | — | — | 1 | 5.22 |
| CHEMBL3318715 | — | — | 1 | 5.16 |
| CHEMBL3319486 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3319490 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3319485 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3319489 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3318711 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3318715 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3319486 | — | IC50 | = | 13500.0 | nM | 4.87 |