Assay Detail
Binding
CHEMBL5622308
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 60 mins in presence of ATP by ADP-Glo assay
4
Total Activities
4
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.28 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5624603 | — | — | 1 | 9.19 |
| CHEMBL4212775 | — | — | 1 | 8.93 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 7.71 |
| CHEMBL4204119 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5624603 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4212775 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 19.32 | nM | 7.71 |
| CHEMBL4204119 | — | IC50 | = | 51.0 | nM | 7.29 |