Assay Detail
Binding
CHEMBL4199839
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system using GFP-4EBP1 as substrate measured after 1 hr by Lathascreen method
5
Total Activities
5
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
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.75 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211915 | — | — | 1 | 6.73 |
| CHEMBL4215969 | — | — | 1 | 5.78 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 5.70 |
| CHEMBL4206442 | — | — | 1 | 5.67 |
| CHEMBL4210320 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211915 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL4215969 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 1981.0 | nM | 5.70 |
| CHEMBL4206442 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4210320 | — | IC50 | = | 13980.0 | nM | 4.85 |