Assay Detail
Binding
CHEMBL4016546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-CD3/anti-CD28-mediated IFNgamma production preincubated for 1 hr followed by anti-CD3/anti-CD28 activation measured after overnight incubation by AlphaLisa assay
12
Total Activities
12
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
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.03 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4074315 | — | — | 1 | 7.55 |
| CHEMBL4064666 | — | — | 1 | 7.46 |
| CHEMBL4092344 | — | — | 1 | 7.44 |
| CHEMBL4100099 | — | — | 1 | 7.25 |
| CHEMBL4059848 | — | — | 1 | 7.15 |
| CHEMBL4094814 | — | — | 1 | 7.09 |
| CHEMBL4078237 | — | — | 1 | 7.01 |
| CHEMBL4070029 | — | — | 1 | 6.92 |
| CHEMBL4102552 | — | — | 1 | 6.92 |
| CHEMBL4073255 | — | — | 1 | 6.85 |
| CHEMBL4097222 | — | — | 1 | 6.52 |
| CHEMBL4084604 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4074315 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4064666 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4092344 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4100099 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4059848 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4094814 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4078237 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4070029 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4102552 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4073255 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4097222 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4084604 | — | IC50 | = | 560.0 | nM | 6.25 |