Assay Detail
Binding
CHEMBL4716076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3kdelta in anti-IgD-induced human whole blood cells assessed as reduction in Akt phosphorylation at ser 473 residue pretreated with compound for 60 mins followed by anti-IgD stimulation measured after 7 mins by Alexa fluor 488 staining based flow cytometry analysis
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| fIC50 | 5 | - | - |
| IC50 | 5 | 7.55 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763849 | — | — | 2 | 8.57 |
| CHEMBL4754382 | — | — | 2 | 7.72 |
| CHEMBL2216895 | — | — | 2 | 7.50 |
| CHEMBL4790186 | — | — | 2 | 7.08 |
| CHEMBL4784595 | — | — | 2 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763849 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4754382 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL2216895 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4790186 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4784595 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4754382 | — | fIC50 | = | 5.7 | nM | - |
| CHEMBL4763849 | — | fIC50 | = | 1.0 | nM | - |
| CHEMBL4784595 | — | fIC50 | = | 35.4 | nM | - |
| CHEMBL2216895 | — | fIC50 | = | 2.4 | nM | - |
| CHEMBL4790186 | — | fIC50 | = | 10.1 | nM | - |