Assay Detail
Binding
CHEMBL5389545
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Inhibition of AKT phosphorylation in human T47D cells harboring PI3Kalpha H1047R mutant incubated for 24 hrs by AlphaLISA assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T47D |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase AKT (CHEMBL2111353) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.82 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426352 | — | — | 1 | 9.52 |
| CHEMBL5414256 | — | — | 1 | 9.05 |
| CHEMBL5402470 | — | — | 1 | 9.00 |
| CHEMBL5406950 | — | — | 1 | 9.00 |
| CHEMBL5437679 | — | — | 1 | 8.70 |
| CHEMBL5419204 | — | — | 1 | 8.52 |
| CHEMBL5423227 | — | — | 1 | 8.52 |
| CHEMBL5408522 | — | — | 1 | 8.52 |
| CHEMBL5424195 | — | — | 1 | 8.52 |
| CHEMBL5411976 | — | — | 1 | 8.52 |
| CHEMBL5406570 | — | — | 1 | 8.05 |
| CHEMBL5430524 | — | — | 1 | 7.85 |
| CHEMBL5422741 | — | — | 1 | 7.82 |
| CHEMBL5424291 | — | — | 1 | 7.75 |
| CHEMBL5424735 | — | — | 1 | 7.55 |
| CHEMBL5436038 | — | — | 1 | 7.11 |
| CHEMBL5409207 | — | — | 1 | 6.84 |
| CHEMBL5440814 | — | — | 1 | 6.75 |
| CHEMBL5404456 | — | — | 1 | 6.48 |
| CHEMBL5431134 | — | — | 1 | 6.43 |
| CHEMBL5413908 | — | — | 1 | 5.86 |
| CHEMBL5401780 | — | — | 1 | 5.59 |
| CHEMBL5394975 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426352 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5414256 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5402470 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5406950 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5437679 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5419204 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5423227 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5408522 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5424195 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5411976 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5406570 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5430524 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5422741 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5424291 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5424735 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5436038 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5409207 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL5440814 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL5404456 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5431134 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL5413908 | — | IC50 | = | 1367.0 | nM | 5.86 |
| CHEMBL5401780 | — | IC50 | = | 2544.0 | nM | 5.59 |
| CHEMBL5394975 | — | IC50 | > | 10000.0 | nM | - |