Assay Detail
Binding
CHEMBL5125358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged recombinant full length human PI3Kdelta expressed in baculovirus infected Sf21 insect cells incubated for 30 mins by HTRF assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.67 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3039502 | DUVELISIB | 4.0 | 1 | 8.60 |
| CHEMBL5178168 | — | — | 1 | 6.22 |
| CHEMBL5179238 | — | — | 1 | 6.00 |
| CHEMBL5203809 | — | — | 1 | 5.70 |
| CHEMBL5182396 | — | — | 1 | 5.52 |
| CHEMBL5200762 | — | — | 1 | 4.55 |
| CHEMBL5182539 | — | — | 1 | 4.39 |
| CHEMBL5189303 | — | — | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3039502 | DUVELISIB | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5178168 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5179238 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5203809 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5182396 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5200762 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5182539 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL5189303 | — | IC50 | = | 42000.0 | nM | 4.38 |