Assay Detail
Binding
CHEMBL4019299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mTOR in human A2058 cells assessed as reduction in phosphorylation of S6 at ser235/236 residues after 1 hr by in-cell Western method
15
Total Activities
15
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
Serine/threonine-protein kinase mTOR (CHEMBL2842) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.10 | 6.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 6.69 |
| CHEMBL4102855 | — | — | 1 | 6.51 |
| CHEMBL4097282 | — | — | 1 | 6.38 |
| CHEMBL4068426 | — | — | 1 | 6.38 |
| CHEMBL4081904 | — | — | 1 | 6.14 |
| CHEMBL4079258 | — | — | 1 | 6.09 |
| CHEMBL4092165 | — | — | 1 | 6.08 |
| CHEMBL4071150 | — | — | 1 | 6.03 |
| CHEMBL4098203 | — | — | 1 | 5.96 |
| CHEMBL4089567 | — | — | 1 | 5.89 |
| CHEMBL4071370 | — | — | 1 | 5.79 |
| CHEMBL4074098 | — | — | 1 | 5.25 |
| CHEMBL4062723 | — | — | 1 | - |
| CHEMBL4100862 | — | — | 1 | - |
| CHEMBL4099904 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084907 | BIMIRALISIB | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4102855 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL4097282 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL4068426 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL4081904 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL4079258 | — | IC50 | = | 817.0 | nM | 6.09 |
| CHEMBL4092165 | — | IC50 | = | 831.0 | nM | 6.08 |
| CHEMBL4071150 | — | IC50 | = | 939.0 | nM | 6.03 |
| CHEMBL4098203 | — | IC50 | = | 1105.0 | nM | 5.96 |
| CHEMBL4089567 | — | IC50 | = | 1282.0 | nM | 5.89 |
| CHEMBL4071370 | — | IC50 | = | 1638.0 | nM | 5.79 |
| CHEMBL4074098 | — | IC50 | = | 5588.0 | nM | 5.25 |
| CHEMBL4062723 | — | IC50 | - | — | - | |
| CHEMBL4100862 | — | IC50 | = | 1100000.0 | nM | - |
| CHEMBL4099904 | — | IC50 | = | 1.7 | 10'7nM | - |