Assay Detail
Binding
CHEMBL5138982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human N-terminal GST-tagged mTOR assessed as phosphorylated 4EBP1 by TR-FRET assay
8
Total Activities
8
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 NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.15 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.07 |
| CHEMBL2017976 | — | — | 1 | 6.36 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 5.65 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 5.47 |
| CHEMBL2017977 | — | — | 1 | 5.20 |
| CHEMBL5192813 | — | — | 1 | - |
| CHEMBL5173332 | — | — | 1 | - |
| CHEMBL5173182 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2017976 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 2259.0 | nM | 5.65 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 3351.0 | nM | 5.47 |
| CHEMBL2017977 | — | IC50 | = | 6309.0 | nM | 5.20 |
| CHEMBL5192813 | — | IC50 | > | 9100.0 | nM | - |
| CHEMBL5173332 | — | IC50 | > | 9100.0 | nM | - |
| CHEMBL5173182 | — | IC50 | > | 9100.0 | nM | - |