Assay Detail
Binding
CHEMBL1768784
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Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.82 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765750 | — | — | 1 | 7.72 |
| CHEMBL1765743 | — | — | 1 | 7.52 |
| CHEMBL1765742 | — | — | 1 | 7.06 |
| CHEMBL1765744 | — | — | 1 | 6.99 |
| CHEMBL1765751 | — | — | 1 | 6.94 |
| CHEMBL1614777 | — | — | 1 | 6.82 |
| CHEMBL1765740 | — | — | 1 | 6.53 |
| CHEMBL1765739 | — | — | 1 | 6.50 |
| CHEMBL1614775 | — | — | 1 | 6.48 |
| CHEMBL1765741 | — | — | 1 | 6.23 |
| CHEMBL1765738 | — | — | 1 | 6.18 |
| CHEMBL1765736 | — | — | 1 | - |
| CHEMBL1765737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765750 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1765743 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1765742 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1765744 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL1765751 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1614777 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL1765740 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL1765739 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL1614775 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL1765741 | — | IC50 | = | 594.0 | nM | 6.23 |
| CHEMBL1765738 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL1765736 | — | IC50 | > | 29300.0 | nM | - |
| CHEMBL1765737 | — | IC50 | - | — | - |