Assay Detail
Binding
CHEMBL3996850
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in human whole blood assessed as suppression of CD69 expression incubated for 60 mins
10
Total Activities
10
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 delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.99 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071580 | — | — | 1 | 8.40 |
| CHEMBL4061855 | — | — | 1 | 7.89 |
| CHEMBL4064155 | — | — | 1 | 7.41 |
| CHEMBL4099634 | — | — | 1 | 7.09 |
| CHEMBL4101075 | — | — | 1 | 6.84 |
| CHEMBL4072750 | — | — | 1 | 6.71 |
| CHEMBL4087086 | — | — | 1 | 6.62 |
| CHEMBL4091906 | — | — | 1 | 6.54 |
| CHEMBL4065659 | — | — | 1 | 6.50 |
| CHEMBL4072625 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071580 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4061855 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4064155 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4099634 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4101075 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4072750 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4087086 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL4091906 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4065659 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL4072625 | — | IC50 | = | 1208.0 | nM | 5.92 |