Assay Detail
Binding
CHEMBL4410949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system using GFP-4E-BP1 peptide as substrate incubated for 1 hr by LanthaScreen assay
19
Total Activities
19
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
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.23 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | 2.0 | 1 | 9.00 |
| CHEMBL4529672 | — | — | 1 | 8.40 |
| CHEMBL4564479 | — | — | 1 | 8.22 |
| CHEMBL4549761 | — | — | 1 | 8.00 |
| CHEMBL4572049 | — | — | 1 | 7.96 |
| CHEMBL4538004 | — | — | 1 | 7.89 |
| CHEMBL4441763 | — | — | 1 | 7.70 |
| CHEMBL4588610 | — | — | 1 | 7.68 |
| CHEMBL4585005 | — | — | 1 | 7.55 |
| CHEMBL4538629 | — | — | 1 | 7.48 |
| CHEMBL4517253 | — | — | 1 | 7.40 |
| CHEMBL4461815 | — | — | 1 | 7.30 |
| CHEMBL4475845 | — | — | 1 | 7.21 |
| CHEMBL4456417 | — | — | 1 | 6.72 |
| CHEMBL4525459 | — | — | 1 | 6.43 |
| CHEMBL4451788 | — | — | 1 | 5.77 |
| CHEMBL4440554 | — | — | 1 | 5.66 |
| CHEMBL4475002 | — | — | 1 | 5.64 |
| CHEMBL4522109 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4529672 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4564479 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4549761 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4572049 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4538004 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4441763 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4588610 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4585005 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4538629 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4517253 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4461815 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4475845 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4456417 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL4525459 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL4451788 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL4440554 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4475002 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL4522109 | — | Ki | = | 4000.0 | nM | 5.40 |