Assay Detail
Binding
CHEMBL4024908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) after 60 mins using fluorescein-labeled kinase tracer by HTRF assay
14
Total Activities
14
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
Identification of highly potent and selective PI3Kδ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.18 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4092654 | — | — | 1 | 7.27 |
| CHEMBL4063245 | — | — | 1 | 6.75 |
| CHEMBL4093593 | — | — | 1 | 6.60 |
| CHEMBL3805348 | — | — | 1 | 6.57 |
| CHEMBL4084897 | — | — | 1 | 6.57 |
| CHEMBL4067592 | — | — | 1 | 6.21 |
| CHEMBL4089756 | — | — | 1 | 6.20 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 6.10 |
| CHEMBL4080945 | — | — | 1 | 6.03 |
| CHEMBL4071877 | — | — | 1 | 5.96 |
| CHEMBL4061641 | — | — | 1 | 5.92 |
| CHEMBL4105190 | — | — | 1 | 5.77 |
| CHEMBL4086343 | — | — | 1 | 5.48 |
| CHEMBL4088828 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4092654 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4063245 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4093593 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3805348 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4084897 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4067592 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4089756 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4080945 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4071877 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4061641 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4105190 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4086343 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4088828 | — | IC50 | = | 8300.0 | nM | 5.08 |