Assay Detail
Binding
CHEMBL1768753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| 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 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 6.17 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765602 | — | — | 1 | 6.70 |
| CHEMBL1765605 | — | — | 1 | 6.60 |
| CHEMBL1765615 | — | — | 1 | 6.60 |
| CHEMBL1765709 | — | — | 1 | 6.60 |
| CHEMBL1765606 | — | — | 1 | 6.30 |
| CHEMBL1765607 | — | — | 1 | 6.30 |
| CHEMBL1765616 | — | — | 1 | 6.30 |
| CHEMBL1765608 | — | — | 1 | 6.12 |
| CHEMBL1765707 | — | — | 1 | 6.12 |
| CHEMBL1765708 | — | — | 1 | 6.12 |
| CHEMBL1765710 | — | — | 1 | 6.12 |
| CHEMBL1765706 | — | — | 1 | 6.00 |
| CHEMBL1765604 | — | — | 1 | 6.00 |
| CHEMBL1765609 | — | — | 1 | 6.00 |
| CHEMBL1765612 | — | — | 1 | 6.00 |
| CHEMBL1765711 | — | — | 1 | 6.00 |
| CHEMBL1765611 | — | — | 1 | 6.00 |
| CHEMBL1765713 | — | — | 1 | 5.90 |
| CHEMBL1765714 | — | — | 1 | 5.90 |
| CHEMBL1256459 | TORIN1 | — | 1 | 5.75 |
| CHEMBL1765601 | — | — | 1 | - |
| CHEMBL1765603 | — | — | 1 | - |
| CHEMBL1765610 | — | — | 1 | - |
| CHEMBL1765613 | — | — | 1 | - |
| CHEMBL1765614 | — | — | 1 | - |
| CHEMBL1765712 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765602 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1765605 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1765615 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1765709 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1765606 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1765607 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1765616 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1765608 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1765707 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1765708 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1765710 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1765706 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765604 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765609 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765612 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765711 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765611 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1765713 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL1765714 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL1256459 | TORIN1 | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1765601 | — | EC50 | > | 1250.0 | nM | - |
| CHEMBL1765603 | — | EC50 | > | 1250.0 | nM | - |
| CHEMBL1765610 | — | EC50 | > | 1250.0 | nM | - |
| CHEMBL1765613 | — | EC50 | > | 1250.0 | nM | - |
| CHEMBL1765614 | — | EC50 | > | 1250.0 | nM | - |
| CHEMBL1765712 | — | EC50 | > | 1250.0 | nM | - |