Assay Detail
Binding
CHEMBL4840759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate in presence of ATP measured after 60 mins 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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.36 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861979 | — | — | 1 | 7.55 |
| CHEMBL4204119 | — | — | 1 | 7.29 |
| CHEMBL4867808 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861979 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4204119 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4867808 | — | IC50 | = | 59.0 | nM | 7.23 |