Assay Detail
Binding
CHEMBL1107899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.98 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090382 | — | — | 1 | 7.72 |
| CHEMBL1093754 | — | — | 1 | 7.60 |
| CHEMBL1094015 | — | — | 1 | 7.54 |
| CHEMBL1091491 | — | — | 1 | 7.52 |
| CHEMBL1092815 | — | — | 1 | 7.44 |
| CHEMBL1092486 | — | — | 1 | 7.41 |
| CHEMBL1094017 | — | — | 1 | 7.37 |
| CHEMBL1091492 | — | — | 1 | 7.31 |
| CHEMBL1090388 | — | — | 1 | 7.28 |
| CHEMBL1092768 | — | — | 1 | 7.28 |
| CHEMBL1092120 | — | — | 1 | 7.24 |
| CHEMBL1092119 | — | — | 1 | 7.20 |
| CHEMBL1091456 | — | — | 1 | 7.20 |
| CHEMBL1092485 | — | — | 1 | 7.16 |
| CHEMBL1091455 | — | — | 1 | 7.11 |
| CHEMBL1090043 | — | — | 1 | 7.05 |
| CHEMBL1092781 | — | — | 1 | 7.00 |
| CHEMBL1090381 | — | — | 1 | 6.98 |
| CHEMBL1092474 | — | — | 1 | 6.92 |
| CHEMBL1094016 | — | — | 1 | 6.81 |
| CHEMBL1090383 | — | — | 1 | 6.76 |
| CHEMBL1092814 | — | — | 1 | 6.66 |
| CHEMBL1088746 | — | — | 1 | 6.43 |
| CHEMBL1088745 | — | — | 1 | 6.34 |
| CHEMBL1091070 | — | — | 1 | 5.96 |
| CHEMBL1091071 | — | — | 1 | 5.83 |
| CHEMBL1092818 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090382 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1093754 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1094015 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1091491 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1092815 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1092486 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1094017 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1091492 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1090388 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1092768 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1092120 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1092119 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1091456 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1092485 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1091455 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1090043 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1092781 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1090381 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1092474 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL1094016 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1090383 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL1092814 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL1088746 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL1088745 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL1091070 | — | IC50 | = | 1106.0 | nM | 5.96 |
| CHEMBL1091071 | — | IC50 | = | 1478.0 | nM | 5.83 |
| CHEMBL1092818 | — | IC50 | = | 5895.0 | nM | 5.23 |