Assay Detail
Binding
CHEMBL1768754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mTOR in p53-deficient MEF assessed as phosphorylation of S6K1 at Thr389 by immunoblotting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase mTOR (CHEMBL1255165) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 8.08 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765602 | — | — | 1 | 9.60 |
| CHEMBL1765605 | — | — | 1 | 9.00 |
| CHEMBL1765606 | — | — | 1 | 9.00 |
| CHEMBL1765608 | — | — | 1 | 9.00 |
| CHEMBL1765707 | — | — | 1 | 9.00 |
| CHEMBL1765708 | — | — | 1 | 9.00 |
| CHEMBL1256459 | TORIN1 | — | 1 | 8.70 |
| CHEMBL1765615 | — | — | 1 | 8.70 |
| CHEMBL1765709 | — | — | 1 | 8.70 |
| CHEMBL1765710 | — | — | 1 | 8.30 |
| CHEMBL1765609 | — | — | 1 | 8.00 |
| CHEMBL1765603 | — | — | 1 | 8.00 |
| CHEMBL1765610 | — | — | 1 | 8.00 |
| CHEMBL1765616 | — | — | 1 | 8.00 |
| CHEMBL1765614 | — | — | 1 | 8.00 |
| CHEMBL1765612 | — | — | 1 | 7.70 |
| CHEMBL1765613 | — | — | 1 | 7.70 |
| CHEMBL1765601 | — | — | 1 | 7.60 |
| CHEMBL1765607 | — | — | 1 | 7.60 |
| CHEMBL1765712 | — | — | 1 | 7.60 |
| CHEMBL1765714 | — | — | 1 | 7.46 |
| CHEMBL1765604 | — | — | 1 | 7.30 |
| CHEMBL1765611 | — | — | 1 | 7.30 |
| CHEMBL1765706 | — | — | 1 | 7.30 |
| CHEMBL1765711 | — | — | 1 | 7.00 |
| CHEMBL1765713 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765602 | — | EC50 | = | 0.25 | nM | 9.60 |
| CHEMBL1765605 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1765606 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1765608 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1765707 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1765708 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1256459 | TORIN1 | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1765615 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1765709 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1765710 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1765609 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1765603 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1765610 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1765616 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1765614 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1765612 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1765613 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1765601 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1765607 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1765712 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1765714 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1765604 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1765611 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1765706 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1765711 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1765713 | — | EC50 | = | 250.0 | nM | 6.60 |