Assay Detail
Binding
CHEMBL1103719
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Inhibition of human GST-tagged-PDK1 expressed in HEK293 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.04 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094320 | — | — | 1 | 8.52 |
| CHEMBL1095621 | — | — | 1 | 8.52 |
| CHEMBL1097955 | — | — | 1 | 8.52 |
| CHEMBL1095278 | — | — | 1 | 8.30 |
| CHEMBL1095279 | — | — | 1 | 8.22 |
| CHEMBL1097956 | — | — | 1 | 8.22 |
| CHEMBL1097972 | — | — | 1 | 8.22 |
| CHEMBL1095612 | — | — | 1 | 8.22 |
| CHEMBL1095931 | — | — | 1 | 8.10 |
| CHEMBL1096271 | — | — | 1 | 8.10 |
| CHEMBL1097602 | — | — | 1 | 8.10 |
| CHEMBL1097973 | — | — | 1 | 8.05 |
| CHEMBL1098302 | — | — | 1 | 7.89 |
| CHEMBL1094321 | — | — | 1 | 7.85 |
| CHEMBL1095622 | — | — | 1 | 7.82 |
| CHEMBL1097604 | — | — | 1 | 7.82 |
| CHEMBL1095294 | — | — | 1 | 7.77 |
| CHEMBL1094637 | — | — | 1 | 7.75 |
| CHEMBL1095285 | — | — | 1 | 7.68 |
| CHEMBL235157 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094320 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1095621 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1097955 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1095278 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1095279 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1097956 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1097972 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1095612 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1095931 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1096271 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1097602 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1097973 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1098302 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1094321 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1095622 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1097604 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1095294 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1094637 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1095285 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL235157 | — | IC50 | = | 60.0 | nM | 7.22 |