Assay Detail
Binding
CHEMBL5029288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PI3Kalpha assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by substrate addition measured after 60 mins by ADP-glo assay
19
Total Activities
19
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 alpha isoform (CHEMBL4005) ↗| 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 | 19 | 7.42 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080551 | — | — | 1 | 7.80 |
| CHEMBL5086461 | — | — | 1 | 7.70 |
| CHEMBL5091128 | — | — | 1 | 7.70 |
| CHEMBL5076543 | — | — | 1 | 7.70 |
| CHEMBL5094877 | — | — | 1 | 7.50 |
| CHEMBL5082066 | — | — | 1 | 7.50 |
| CHEMBL5084056 | — | — | 1 | 7.50 |
| CHEMBL5072469 | — | — | 1 | 7.40 |
| CHEMBL5081964 | — | — | 1 | 7.40 |
| CHEMBL5091438 | — | — | 1 | 7.40 |
| CHEMBL5088457 | — | — | 1 | 7.40 |
| CHEMBL5071394 | — | — | 1 | 7.40 |
| CHEMBL5078679 | — | — | 1 | 7.40 |
| CHEMBL5094025 | — | — | 1 | 7.40 |
| CHEMBL5088310 | — | — | 1 | 7.30 |
| CHEMBL5090799 | — | — | 1 | 7.30 |
| CHEMBL4558527 | AZD-8154 | 2.0 | 1 | 7.20 |
| CHEMBL5077865 | — | — | 1 | 7.00 |
| CHEMBL5094364 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080551 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5086461 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5091128 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5076543 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5094877 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5082066 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5084056 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5072469 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5081964 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5091438 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5088457 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5071394 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5078679 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5094025 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5088310 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5090799 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4558527 | AZD-8154 | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5077865 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5094364 | — | IC50 | = | 125.89 | nM | 6.90 |