Assay Detail
Binding
CHEMBL4828192
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 cytostim-stimulated IFNgamma production preincubated for 1 hr followed by cytostim stimulation and measured after 20 hrs by electrochemiluminescence assay
34
Total Activities
34
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 of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.46 | 8.90 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4858875 | — | — | 1 | 8.90 |
| CHEMBL4175571 | — | — | 1 | 8.60 |
| CHEMBL4878638 | — | — | 1 | 8.50 |
| CHEMBL4170075 | — | — | 1 | 8.50 |
| CHEMBL4173087 | — | — | 1 | 8.50 |
| CHEMBL4167702 | — | — | 1 | 8.20 |
| CHEMBL4165185 | — | — | 1 | 8.10 |
| CHEMBL4175737 | — | — | 1 | 8.10 |
| CHEMBL4174874 | — | — | 1 | 8.00 |
| CHEMBL4850297 | — | — | 1 | 7.90 |
| CHEMBL4867203 | — | — | 1 | 7.90 |
| CHEMBL4169192 | — | — | 1 | 7.90 |
| CHEMBL4870970 | — | — | 1 | 7.70 |
| CHEMBL4855234 | — | — | 1 | 7.70 |
| CHEMBL4869783 | — | — | 1 | 7.60 |
| CHEMBL4873390 | — | — | 1 | 7.50 |
| CHEMBL4868553 | — | — | 1 | 7.50 |
| CHEMBL4870020 | — | — | 1 | 7.50 |
| CHEMBL4869356 | — | — | 1 | 7.40 |
| CHEMBL4872328 | — | — | 1 | 7.30 |
| CHEMBL4845674 | — | — | 1 | 7.30 |
| CHEMBL4870356 | — | — | 1 | 7.20 |
| CHEMBL4846241 | — | — | 1 | 7.10 |
| CHEMBL4863100 | — | — | 1 | 7.10 |
| CHEMBL4869306 | — | — | 1 | 7.10 |
| CHEMBL4857056 | — | — | 1 | 6.80 |
| CHEMBL4872822 | — | — | 1 | 6.70 |
| CHEMBL4876289 | — | — | 1 | 6.50 |
| CHEMBL4469876 | — | — | 1 | 5.50 |
| CHEMBL4849115 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4858875 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4175571 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4878638 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4170075 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4173087 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4167702 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4165185 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4175737 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4174874 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4850297 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4867203 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4169192 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4870970 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4855234 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4869783 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4868553 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4873390 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4870020 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4869356 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4872328 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4845674 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4870356 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4846241 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4863100 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4869306 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4857056 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4872822 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4876289 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4469876 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4849115 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4859024 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4878870 | — | pIC50 | - | — | - | |
| CHEMBL4852717 | — | pIC50 | - | — | - | |
| CHEMBL4877995 | — | IC50 | = | 62.0 | nM | - |