Assay Detail
Binding
CHEMBL1109707
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant mTOR assessed as reduction in GFP-4EBP1 phosphorylation after 30 mins by FRET assay
12
Total Activities
12
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
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.67 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091977 | — | — | 1 | 8.40 |
| CHEMBL1093267 | — | — | 1 | 8.40 |
| CHEMBL1090601 | — | — | 1 | 8.30 |
| CHEMBL1090598 | — | — | 1 | 8.00 |
| CHEMBL1090239 | — | — | 1 | 8.00 |
| CHEMBL1091978 | — | — | 1 | 7.68 |
| CHEMBL1083192 | — | — | 1 | 7.54 |
| CHEMBL1091979 | — | — | 1 | 7.52 |
| CHEMBL594844 | — | — | 1 | 7.38 |
| CHEMBL1090599 | — | — | 1 | 7.30 |
| CHEMBL1090600 | — | — | 1 | 7.23 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091977 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1093267 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1090601 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1090598 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1090239 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1091978 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1083192 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1091979 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL594844 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1090599 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1090600 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL521851 | PICTILISIB | Ki | = | 570.0 | nM | 6.24 |