Assay Detail
Binding
CHEMBL4366252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end residues) using Ulight-4E-BP1 as substrate incubated for 30 mins by fluorescence assay
52
Total Activities
52
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 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 7.48 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.85 |
| CHEMBL4529195 | — | — | 1 | 8.44 |
| CHEMBL4452675 | — | — | 1 | 8.37 |
| CHEMBL573339 | PI-103 | — | 1 | 8.28 |
| CHEMBL4444508 | — | — | 1 | 7.90 |
| CHEMBL4513405 | — | — | 1 | 7.86 |
| CHEMBL4528675 | — | — | 1 | 7.86 |
| CHEMBL4519698 | — | — | 1 | 7.85 |
| CHEMBL4473266 | — | — | 1 | 7.82 |
| CHEMBL4544815 | — | — | 1 | 7.75 |
| CHEMBL4475948 | — | — | 1 | 7.71 |
| CHEMBL4584781 | — | — | 1 | 7.70 |
| CHEMBL4451044 | — | — | 1 | 7.46 |
| CHEMBL4529790 | — | — | 1 | 7.31 |
| CHEMBL4450906 | — | — | 1 | 6.60 |
| CHEMBL4461794 | — | — | 1 | 6.57 |
| CHEMBL4455115 | — | — | 1 | 6.54 |
| CHEMBL4571692 | — | — | 1 | 6.48 |
| CHEMBL4460772 | — | — | 1 | 6.20 |
| CHEMBL4558087 | — | — | 1 | 6.06 |
| CHEMBL4444052 | — | — | 1 | - |
| CHEMBL4439623 | — | — | 1 | - |
| CHEMBL4470593 | — | — | 1 | - |
| CHEMBL4550849 | — | — | 1 | - |
| CHEMBL4578589 | — | — | 1 | - |
| CHEMBL4466274 | — | — | 1 | - |
| CHEMBL4452258 | — | — | 1 | - |
| CHEMBL4468420 | — | — | 1 | - |
| CHEMBL4551072 | — | — | 1 | - |
| CHEMBL4443157 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL4529195 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4452675 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL573339 | PI-103 | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4444508 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4513405 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4528675 | — | IC50 | = | 13.85 | nM | 7.86 |
| CHEMBL4519698 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4473266 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL4544815 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL4475948 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4584781 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4451044 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL4529790 | — | IC50 | = | 48.6 | nM | 7.31 |
| CHEMBL4450906 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL4461794 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL4455115 | — | IC50 | = | 290.5 | nM | 6.54 |
| CHEMBL4571692 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4460772 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL4558087 | — | IC50 | = | 873.0 | nM | 6.06 |
| CHEMBL4454653 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4564155 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4571676 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444876 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4578498 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4438161 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4549852 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4563627 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4587305 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4577338 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4468153 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4581724 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4535706 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4464019 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4540680 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4451792 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4462575 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4462789 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4520869 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4467799 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4443157 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4551072 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4468420 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4452258 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4466274 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4578589 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4550849 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4470593 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4439623 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444052 | — | IC50 | > | 1000.0 | nM | - |