Assay Detail
Binding
CHEMBL896553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDK1 mediated cAKT2 phosphorylation by AKT2 activation assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.58 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232176 | — | — | 1 | 8.52 |
| CHEMBL228654 | — | — | 1 | 8.30 |
| CHEMBL391101 | — | — | 1 | 8.05 |
| CHEMBL232177 | — | — | 1 | 8.00 |
| CHEMBL234811 | — | — | 1 | 7.85 |
| CHEMBL442229 | — | — | 1 | 7.75 |
| CHEMBL267837 | — | — | 1 | 7.54 |
| CHEMBL400837 | — | — | 1 | 7.47 |
| CHEMBL393902 | — | — | 1 | 7.26 |
| CHEMBL234601 | — | — | 1 | 7.17 |
| CHEMBL231717 | — | — | 1 | 7.10 |
| CHEMBL395163 | — | — | 1 | 6.92 |
| CHEMBL232143 | — | — | 1 | 6.70 |
| CHEMBL107225 | — | — | 1 | 6.58 |
| CHEMBL232135 | — | — | 1 | 6.55 |
| CHEMBL232134 | — | — | 1 | 6.55 |
| CHEMBL441911 | — | — | 1 | 6.54 |
| CHEMBL393636 | — | — | 1 | 6.47 |
| CHEMBL85403 | — | — | 1 | 6.29 |
| CHEMBL232360 | — | — | 1 | 6.28 |
| CHEMBL232144 | — | — | 1 | 6.24 |
| CHEMBL232349 | — | — | 1 | 6.24 |
| CHEMBL231947 | — | — | 1 | 6.17 |
| CHEMBL232136 | — | — | 1 | 6.17 |
| CHEMBL231716 | — | — | 1 | 6.05 |
| CHEMBL393841 | — | — | 1 | 6.00 |
| CHEMBL393840 | — | — | 1 | 6.00 |
| CHEMBL231715 | — | — | 1 | 6.00 |
| CHEMBL426078 | — | — | 1 | 5.96 |
| CHEMBL86755 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232176 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL228654 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL391101 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL232177 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL234811 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL442229 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL267837 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL400837 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL393902 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL234601 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL231717 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL395163 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL232143 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL107225 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL232134 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL232135 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL441911 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL393636 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL85403 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL232360 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL232349 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL232144 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL231947 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL232136 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL231716 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL393841 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL393840 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL231715 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL426078 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL86755 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL394300 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL233373 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL400838 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL232365 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL231979 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL401043 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL393838 | — | IC50 | > | 26000.0 | nM | - |
| CHEMBL393635 | — | IC50 | > | 26000.0 | nM | - |