Assay Detail
Binding
CHEMBL4723693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo plus luminescence assay
14
Total Activities
14
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 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3Kα inhibitors via docking-based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.31 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.02 |
| CHEMBL4786631 | — | — | 1 | 5.18 |
| CHEMBL4750370 | — | — | 1 | 5.12 |
| CHEMBL4792735 | — | — | 1 | 4.81 |
| CHEMBL4743643 | — | — | 1 | 4.77 |
| CHEMBL4747338 | — | — | 1 | 4.74 |
| CHEMBL4782512 | — | — | 1 | 4.54 |
| CHEMBL4756631 | — | — | 1 | - |
| CHEMBL4797000 | — | — | 1 | - |
| CHEMBL4754150 | — | — | 1 | - |
| CHEMBL4794184 | — | — | 1 | - |
| CHEMBL4762002 | — | — | 1 | - |
| CHEMBL4799648 | — | — | 1 | - |
| CHEMBL4798869 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4786631 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4750370 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4792735 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL4743643 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4747338 | — | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL4782512 | — | IC50 | = | 29200.0 | nM | 4.54 |
| CHEMBL4756631 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4797000 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4754150 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4794184 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4762002 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4799648 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4798869 | — | IC50 | > | 200000.0 | nM | - |