Assay Detail
Binding
CHEMBL4019283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human mTOR (L1382 to W2549 residues) expressed in mammalian expression system at 10 uM
6
Total Activities
6
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 |
|---|---|---|---|
| Kd | 6 | 7.95 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | 9.03 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.48 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 7.92 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.72 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 7.32 |
| CHEMBL4102855 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592445 | GEDATOLISIB | Kd | = | 0.94 | nM | 9.03 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL4084907 | BIMIRALISIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL2017974 | BUPARLISIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL521851 | PICTILISIB | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL4102855 | — | Kd | = | 61.0 | nM | 7.21 |