Assay Detail
Binding
CHEMBL4478191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PI3Kalpha using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based luminescence assay
8
Total Activities
8
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 Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.59 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4565988 | — | — | 1 | 8.10 |
| CHEMBL4527822 | — | — | 1 | 7.44 |
| CHEMBL4593348 | — | — | 1 | 6.61 |
| CHEMBL4166405 | — | — | 1 | 6.35 |
| CHEMBL222102 | KU-55933 | — | 1 | 6.34 |
| CHEMBL2140173 | — | — | 1 | 6.34 |
| CHEMBL2143829 | — | — | 1 | 5.83 |
| CHEMBL4218734 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4565988 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4527822 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4593348 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4166405 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL222102 | KU-55933 | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL2140173 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL2143829 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4218734 | — | IC50 | = | 2110.0 | nM | 5.68 |