Assay Detail
Binding
CHEMBL2175553
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Inhibition of PI3Kalpha by AlphaScreen assay
35
Total Activities
35
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 potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.43 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2172629 | — | — | 1 | 7.33 |
| CHEMBL2172635 | — | — | 1 | 7.27 |
| CHEMBL2172486 | — | — | 1 | 7.17 |
| CHEMBL2172482 | — | — | 1 | 7.14 |
| CHEMBL2172485 | — | — | 1 | 7.07 |
| CHEMBL2172487 | — | — | 1 | 7.02 |
| CHEMBL2172634 | — | — | 1 | 6.98 |
| CHEMBL2172475 | — | — | 1 | 6.95 |
| CHEMBL2172636 | — | — | 1 | 6.92 |
| CHEMBL2172480 | — | — | 1 | 6.92 |
| CHEMBL2172630 | — | — | 1 | 6.91 |
| CHEMBL2172489 | — | — | 1 | 6.84 |
| CHEMBL2172632 | — | — | 1 | 6.76 |
| CHEMBL2172490 | — | — | 1 | 6.75 |
| CHEMBL2172484 | — | — | 1 | 6.62 |
| CHEMBL2172633 | — | — | 1 | 6.59 |
| CHEMBL2172483 | — | — | 1 | 6.57 |
| CHEMBL2172640 | — | — | 1 | 6.51 |
| CHEMBL2172481 | — | — | 1 | 6.41 |
| CHEMBL2172488 | — | — | 1 | 6.33 |
| CHEMBL2172637 | — | — | 1 | 6.23 |
| CHEMBL2172624 | — | — | 1 | 6.20 |
| CHEMBL2172638 | — | — | 1 | 6.19 |
| CHEMBL2172639 | — | — | 1 | 6.18 |
| CHEMBL2172625 | — | — | 1 | 6.12 |
| CHEMBL1615183 | — | — | 1 | 6.10 |
| CHEMBL2172627 | — | — | 1 | 5.94 |
| CHEMBL2172631 | — | — | 1 | 5.94 |
| CHEMBL2172474 | — | — | 1 | 5.78 |
| CHEMBL2172628 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2172629 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2172635 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2172486 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2172482 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2172485 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2172487 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2172634 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL2172475 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2172636 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL2172480 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2172630 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2172489 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL2172632 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL2172490 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL2172484 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL2172633 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL2172483 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL2172640 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL2172481 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL2172488 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL2172637 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2172624 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL2172638 | — | IC50 | = | 648.0 | nM | 6.19 |
| CHEMBL2172639 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL2172625 | — | IC50 | = | 763.0 | nM | 6.12 |
| CHEMBL1615183 | — | IC50 | = | 798.0 | nM | 6.10 |
| CHEMBL2172627 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL2172631 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL2172474 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL2172628 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL2172479 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL2172477 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL2172476 | — | IC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL2172626 | — | IC50 | = | 5840.0 | nM | 5.23 |
| CHEMBL2172478 | — | IC50 | > | 125000.0 | nM | - |