Assay Detail
Binding
CHEMBL4019301
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal GST-tagged mTOR (1360 to 2549 residues) expressed in baculovirus expression system using after 1 hr AlexaFluor647-labeled kinase tracer 314 by TR-FRET assay
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 |
|---|---|---|---|
| Ki | 15 | 6.54 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 7.21 |
| CHEMBL4097282 | — | — | 1 | 6.97 |
| CHEMBL4068426 | — | — | 1 | 6.96 |
| CHEMBL4079258 | — | — | 1 | 6.73 |
| CHEMBL4102855 | — | — | 1 | 6.69 |
| CHEMBL4092165 | — | — | 1 | 6.65 |
| CHEMBL4098203 | — | — | 1 | 6.62 |
| CHEMBL4071370 | — | — | 1 | 6.55 |
| CHEMBL4089567 | — | — | 1 | 6.40 |
| CHEMBL4071150 | — | — | 1 | 6.21 |
| CHEMBL4081904 | — | — | 1 | 5.92 |
| CHEMBL4074098 | — | — | 1 | 5.59 |
| CHEMBL4062723 | — | — | 1 | - |
| CHEMBL4100862 | — | — | 1 | - |
| CHEMBL4099904 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084907 | BIMIRALISIB | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4097282 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL4068426 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4079258 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL4102855 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL4092165 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL4098203 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL4071370 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL4089567 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL4071150 | — | Ki | = | 609.0 | nM | 6.21 |
| CHEMBL4081904 | — | Ki | = | 1213.0 | nM | 5.92 |
| CHEMBL4074098 | — | Ki | = | 2539.0 | nM | 5.59 |
| CHEMBL4062723 | — | Ki | = | 660000.0 | nM | - |
| CHEMBL4100862 | — | Ki | = | 110000.0 | nM | - |
| CHEMBL4099904 | — | Ki | - | — | - |