Assay Detail
Binding
CHEMBL4220018
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Inhibition of PDK1 (unknown origin) after 1 hr in presence of Ser/Thr-07 by fluorometric assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.61 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228654 | — | — | 1 | 8.05 |
| CHEMBL3659990 | — | — | 1 | 7.10 |
| CHEMBL3659991 | — | — | 1 | 7.05 |
| CHEMBL3659971 | — | — | 1 | 6.70 |
| CHEMBL3659972 | — | — | 1 | 6.70 |
| CHEMBL3659976 | — | — | 1 | 6.52 |
| CHEMBL3659978 | — | — | 1 | 6.40 |
| CHEMBL3659974 | — | — | 1 | 6.40 |
| CHEMBL3659973 | — | — | 1 | 6.10 |
| CHEMBL3659980 | — | — | 1 | 6.05 |
| CHEMBL3659975 | — | — | 1 | 5.92 |
| CHEMBL3659977 | — | — | 1 | 5.92 |
| CHEMBL4228611 | — | — | 1 | 5.28 |
| CHEMBL3659981 | — | — | 1 | 5.06 |
| CHEMBL3659979 | — | — | 1 | 4.96 |
| CHEMBL3659986 | — | — | 1 | 4.91 |
| CHEMBL3659982 | — | — | 1 | 4.82 |
| CHEMBL4226486 | — | — | 1 | 4.54 |
| CHEMBL3659983 | — | — | 1 | 4.52 |
| CHEMBL3659987 | — | — | 1 | 4.27 |
| CHEMBL501406 | — | — | 1 | 4.08 |
| CHEMBL465091 | — | — | 1 | 3.99 |
| CHEMBL4225389 | — | — | 1 | 3.79 |
| CHEMBL3659988 | — | — | 1 | - |
| CHEMBL3659989 | — | — | 1 | - |
| CHEMBL3659985 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228654 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3659990 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3659991 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3659971 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3659972 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3659976 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3659978 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3659974 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3659973 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3659980 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3659975 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3659977 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4228611 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3659981 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL3659979 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL3659986 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL3659982 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL4226486 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL3659983 | — | IC50 | = | 30300.0 | nM | 4.52 |
| CHEMBL3659987 | — | IC50 | = | 53900.0 | nM | 4.27 |
| CHEMBL501406 | — | IC50 | = | 82400.0 | nM | 4.08 |
| CHEMBL465091 | — | IC50 | = | 101900.0 | nM | 3.99 |
| CHEMBL4225389 | — | IC50 | = | 163600.0 | nM | 3.79 |
| CHEMBL3659988 | — | IC50 | - | — | - | |
| CHEMBL3659989 | — | IC50 | - | — | - | |
| CHEMBL3659985 | — | IC50 | - | — | - |