Assay Detail
Binding
CHEMBL5029287
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in anti-IgM-stimulated human JeKo-1 cells assessed as inhibition of AKT phosphorylation at Ser473 residue incubated for 60 mins by TR-FRET assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | JeKo-1 |
| 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 AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.20 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081634 | — | — | 1 | 9.00 |
| CHEMBL5082066 | — | — | 1 | 8.90 |
| CHEMBL5087061 | — | — | 1 | 8.80 |
| CHEMBL5091438 | — | — | 1 | 8.70 |
| CHEMBL5086461 | — | — | 1 | 8.60 |
| CHEMBL5094877 | — | — | 1 | 8.50 |
| CHEMBL5081964 | — | — | 1 | 8.50 |
| CHEMBL5090799 | — | — | 1 | 8.50 |
| CHEMBL5091128 | — | — | 1 | 8.40 |
| CHEMBL5077865 | — | — | 1 | 8.40 |
| CHEMBL5071394 | — | — | 1 | 8.40 |
| CHEMBL4558527 | AZD-8154 | 2.0 | 1 | 8.40 |
| CHEMBL5088457 | — | — | 1 | 8.40 |
| CHEMBL5080551 | — | — | 1 | 8.40 |
| CHEMBL5094364 | — | — | 1 | 8.30 |
| CHEMBL5078679 | — | — | 1 | 8.20 |
| CHEMBL5076543 | — | — | 1 | 8.20 |
| CHEMBL5072469 | — | — | 1 | 8.20 |
| CHEMBL5089084 | — | — | 1 | 8.20 |
| CHEMBL5094025 | — | — | 1 | 8.10 |
| CHEMBL5088310 | — | — | 1 | 8.10 |
| CHEMBL5084056 | — | — | 1 | 7.90 |
| CHEMBL5082486 | — | — | 1 | 7.50 |
| CHEMBL5077792 | — | — | 1 | 7.30 |
| CHEMBL5081600 | — | — | 1 | 6.90 |
| CHEMBL4129600 | — | — | 1 | 6.40 |
| CHEMBL4126156 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081634 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5082066 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL5087061 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5091438 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5086461 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL5094877 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5081964 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5090799 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5091128 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5077865 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5071394 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4558527 | AZD-8154 | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5088457 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5080551 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5094364 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5078679 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5076543 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5072469 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5089084 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5094025 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL5088310 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL5084056 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5082486 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5077792 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5081600 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4129600 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4126156 | — | IC50 | > | 794.33 | nM | - |