Assay Detail
Binding
CHEMBL5138978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Alexa Fluor labelled Tracer-314 from human N-terminal GST-tagged mTOR incubated for 1 hr by TR-FRET assay
24
Total Activities
23
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 | 24 | 5.67 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.72 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.15 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 6.01 |
| CHEMBL5197306 | — | — | 1 | 5.87 |
| CHEMBL5174001 | — | — | 1 | 5.76 |
| CHEMBL5175657 | — | — | 1 | 5.70 |
| CHEMBL2017977 | — | — | 1 | 5.68 |
| CHEMBL5181180 | — | — | 1 | 5.66 |
| CHEMBL5203121 | — | — | 1 | 5.61 |
| CHEMBL5185902 | — | — | 1 | 5.59 |
| CHEMBL5177354 | — | — | 1 | 5.54 |
| CHEMBL5187418 | — | — | 1 | 5.44 |
| CHEMBL5181013 | — | — | 1 | 5.41 |
| CHEMBL5207057 | — | — | 1 | 5.41 |
| CHEMBL5187488 | — | — | 1 | 5.30 |
| CHEMBL5208098 | — | — | 1 | 5.30 |
| CHEMBL5188146 | — | — | 1 | 5.29 |
| CHEMBL5188186 | — | — | 1 | 5.23 |
| CHEMBL5192317 | — | — | 1 | 5.21 |
| CHEMBL5185811 | — | — | 1 | 5.17 |
| CHEMBL5173182 | — | — | 2 | 5.04 |
| CHEMBL5202872 | — | — | 1 | - |
| CHEMBL5177612 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 712.0 | nM | 6.15 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 973.0 | nM | 6.01 |
| CHEMBL5197306 | — | IC50 | = | 1337.0 | nM | 5.87 |
| CHEMBL5174001 | — | IC50 | = | 1716.0 | nM | 5.76 |
| CHEMBL5175657 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2017977 | — | IC50 | = | 2065.0 | nM | 5.68 |
| CHEMBL5181180 | — | IC50 | = | 2176.0 | nM | 5.66 |
| CHEMBL5203121 | — | IC50 | = | 2474.0 | nM | 5.61 |
| CHEMBL5185902 | — | IC50 | = | 2577.0 | nM | 5.59 |
| CHEMBL5177354 | — | IC50 | = | 2878.0 | nM | 5.54 |
| CHEMBL5187418 | — | IC50 | = | 3613.0 | nM | 5.44 |
| CHEMBL5207057 | — | IC50 | = | 3935.0 | nM | 5.41 |
| CHEMBL5181013 | — | IC50 | = | 3876.0 | nM | 5.41 |
| CHEMBL5208098 | — | IC50 | = | 5057.0 | nM | 5.30 |
| CHEMBL5187488 | — | IC50 | = | 4971.0 | nM | 5.30 |
| CHEMBL5188146 | — | IC50 | = | 5114.0 | nM | 5.29 |
| CHEMBL5188186 | — | IC50 | = | 5937.0 | nM | 5.23 |
| CHEMBL5192317 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5185811 | — | IC50 | = | 6797.0 | nM | 5.17 |
| CHEMBL5173182 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL5202872 | — | IC50 | > | 9100.0 | nM | - |
| CHEMBL5177612 | — | IC50 | > | 9100.0 | nM | - |
| CHEMBL5173182 | — | IC50 | > | 9100.0 | nM | - |