Assay Detail
Binding
CHEMBL4366254
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal GST-tagged PI3Kalpha (1 to 1068 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 1 hr by ADP-Glo assay
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
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 | 7.70 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4584781 | — | — | 1 | 9.37 |
| CHEMBL4528675 | — | — | 1 | 9.20 |
| CHEMBL4519698 | — | — | 1 | 8.70 |
| CHEMBL4475948 | — | — | 1 | 8.39 |
| CHEMBL4544815 | — | — | 1 | 8.29 |
| CHEMBL573339 | PI-103 | — | 1 | 8.02 |
| CHEMBL4513405 | — | — | 1 | 7.92 |
| CHEMBL4452675 | — | — | 1 | 7.81 |
| CHEMBL4473266 | — | — | 1 | 7.72 |
| CHEMBL4451044 | — | — | 1 | 7.68 |
| CHEMBL4444508 | — | — | 1 | 7.66 |
| CHEMBL4529195 | — | — | 1 | 7.34 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 7.09 |
| CHEMBL4461794 | — | — | 1 | 7.07 |
| CHEMBL4529790 | — | — | 1 | 6.99 |
| CHEMBL4455115 | — | — | 1 | 6.95 |
| CHEMBL4571692 | — | — | 1 | 6.94 |
| CHEMBL4450906 | — | — | 1 | 6.88 |
| CHEMBL4460772 | — | — | 1 | 6.30 |
| CHEMBL4468420 | — | — | 1 | - |
| CHEMBL4577338 | — | — | 1 | - |
| CHEMBL4467799 | — | — | 1 | - |
| CHEMBL4444052 | — | — | 1 | - |
| CHEMBL4443157 | — | — | 1 | - |
| CHEMBL4466274 | — | — | 1 | - |
| CHEMBL4550849 | — | — | 1 | - |
| CHEMBL4558087 | — | — | 1 | - |
| CHEMBL4439623 | — | — | 1 | - |
| CHEMBL4551072 | — | — | 1 | - |
| CHEMBL4470593 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4584781 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4528675 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4519698 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4475948 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4544815 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL573339 | PI-103 | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4513405 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4452675 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL4473266 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4451044 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4444508 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4529195 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 80.5 | nM | 7.09 |
| CHEMBL4461794 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4529790 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4455115 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4571692 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4450906 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4460772 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4464019 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4540680 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4445202 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4546021 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4563627 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4520869 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4587305 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4468153 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4549852 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4438161 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4578498 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444876 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4571676 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4564155 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4454653 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4451792 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4462575 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4462789 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4452258 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4578589 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4470593 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4551072 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4439623 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4558087 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4550849 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4466274 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4443157 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444052 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4467799 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4577338 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4468420 | — | IC50 | > | 1000.0 | nM | - |