Assay Detail
Binding
CHEMBL4001606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta-mediated AKT phosphorylation at ser473 residue in human JeKo1 cells preincubated for 60 mins followed by anti-IgM stimulation measured after 10 mins by TR-FRET assay
5
Total Activities
5
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 triazole aminopyrazines as a highly potent and selective series of PI3Kδ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.19 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4089227 | — | — | 1 | 7.70 |
| CHEMBL4091680 | — | — | 1 | 7.30 |
| CHEMBL4072500 | — | — | 1 | 7.05 |
| CHEMBL4091640 | — | — | 1 | 6.96 |
| CHEMBL4101902 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4089227 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4091680 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4072500 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4091640 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4101902 | — | IC50 | = | 120.0 | nM | 6.92 |