Assay Detail
Binding
CHEMBL1117042
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Inhibition of rat brain mTOR assessed as p70S6K-GST protein phosphorylation after 30 mins by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase mTOR (CHEMBL1075134) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.15 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092653 | — | — | 1 | 9.30 |
| CHEMBL1088973 | — | — | 1 | 9.00 |
| CHEMBL1088970 | — | — | 1 | 8.77 |
| CHEMBL1088974 | — | — | 1 | 8.70 |
| CHEMBL1092642 | — | — | 1 | 8.60 |
| CHEMBL1092909 | — | — | 1 | 8.59 |
| CHEMBL1092908 | — | — | 1 | 8.55 |
| CHEMBL1088972 | — | — | 1 | 7.46 |
| CHEMBL1088919 | — | — | 1 | 7.36 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.35 |
| CHEMBL1089219 | — | — | 1 | 7.22 |
| CHEMBL1088971 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092653 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1088973 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1088970 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1088974 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1092642 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1092909 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1092908 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1088972 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1088919 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1089219 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1088971 | — | IC50 | = | 130.0 | nM | 6.89 |