Assay Detail
Binding
CHEMBL5389546
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Inhibition of AKT phosphorylation in human SK-BR-3 cells harboring wildtype PI3Kalpha incubated for 24 hrs by AlphaLISA assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| 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 | 18 | 5.90 | 6.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5404456 | — | — | 1 | 6.94 |
| CHEMBL5406950 | — | — | 1 | 6.25 |
| CHEMBL5408522 | — | — | 1 | 6.17 |
| CHEMBL5437679 | — | — | 1 | 6.11 |
| CHEMBL5423227 | — | — | 1 | 5.83 |
| CHEMBL5424195 | — | — | 1 | 5.74 |
| CHEMBL5419204 | — | — | 1 | 5.50 |
| CHEMBL5414256 | — | — | 1 | 5.32 |
| CHEMBL5436038 | — | — | 1 | 5.23 |
| CHEMBL5440814 | — | — | 1 | - |
| CHEMBL5401780 | — | — | 1 | - |
| CHEMBL5426352 | — | — | 1 | - |
| CHEMBL5424735 | — | — | 1 | - |
| CHEMBL5394975 | — | — | 1 | - |
| CHEMBL5411976 | — | — | 1 | - |
| CHEMBL5402470 | — | — | 1 | - |
| CHEMBL5413908 | — | — | 1 | - |
| CHEMBL5431134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5404456 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5406950 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL5408522 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL5437679 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL5423227 | — | IC50 | = | 1465.0 | nM | 5.83 |
| CHEMBL5424195 | — | IC50 | = | 1803.0 | nM | 5.74 |
| CHEMBL5419204 | — | IC50 | = | 3185.0 | nM | 5.50 |
| CHEMBL5414256 | — | IC50 | = | 4739.0 | nM | 5.32 |
| CHEMBL5436038 | — | IC50 | = | 5894.0 | nM | 5.23 |
| CHEMBL5440814 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5401780 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426352 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5424735 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5394975 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5411976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5402470 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413908 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5431134 | — | IC50 | > | 10000.0 | nM | - |