Assay Detail
Binding
CHEMBL2157248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K p110delta using PIP2 as substrate assessed as PIP3 formation by fluorescence polarization assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.40 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152774 | — | — | 1 | 9.22 |
| CHEMBL2152775 | — | — | 1 | 8.72 |
| CHEMBL2152771 | — | — | 1 | 8.59 |
| CHEMBL2152769 | — | — | 1 | 8.55 |
| CHEMBL2152768 | — | — | 1 | 8.42 |
| CHEMBL2152776 | — | — | 1 | 8.40 |
| CHEMBL2152770 | — | — | 1 | 8.20 |
| CHEMBL2152772 | — | — | 1 | 7.92 |
| CHEMBL2152773 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152774 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2152775 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2152771 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2152769 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2152768 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2152776 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2152770 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2152772 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2152773 | — | IC50 | = | 27.0 | nM | 7.57 |