Assay Detail
Binding
CHEMBL4233142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide substrate measured after 1 hr by Lance Ultra assay
14
Total Activities
14
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
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.50 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4238656 | — | — | 1 | 8.70 |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | 8.10 |
| CHEMBL4250280 | — | — | 1 | 8.00 |
| CHEMBL4246481 | — | — | 1 | 7.54 |
| CHEMBL4246121 | — | — | 1 | 7.52 |
| CHEMBL4239569 | — | — | 1 | 7.50 |
| CHEMBL4239931 | — | — | 1 | 7.32 |
| CHEMBL4251185 | — | — | 1 | 7.28 |
| CHEMBL4239712 | — | — | 1 | 7.14 |
| CHEMBL4248529 | — | — | 1 | 7.06 |
| CHEMBL4240170 | — | — | 1 | 7.02 |
| CHEMBL4244147 | — | — | 1 | 6.84 |
| CHEMBL4246923 | — | — | 1 | - |
| CHEMBL4242668 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4238656 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1801204 | AZD-8055 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4250280 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4246481 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4246121 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4239569 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4239931 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4251185 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4239712 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4248529 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4240170 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4244147 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4246923 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4242668 | — | IC50 | > | 500.0 | nM | - |