Assay Detail
Binding
CHEMBL3705102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: The secondary assay was a time resolved-FRET LanthaScreen Kinase Binding Assay. (Invitrogen Corporation, Carlsbad, Calif.). This assay evaluates the ability of the test compound to compete with a fluorescently-labeled tracer molecule to bind in the ATP pocket of a kinase.
19
Total Activities
19
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
Substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs as inhibitors of the PDK1 kinase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.84 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3659990 | — | — | 1 | 7.10 |
| CHEMBL3659991 | — | — | 1 | 7.03 |
| CHEMBL3659971 | — | — | 1 | 6.64 |
| CHEMBL3659972 | — | — | 1 | 6.58 |
| CHEMBL3659976 | — | — | 1 | 6.55 |
| CHEMBL3659978 | — | — | 1 | 6.42 |
| CHEMBL3659974 | — | — | 1 | 6.39 |
| CHEMBL3659980 | — | — | 1 | 6.04 |
| CHEMBL3659975 | — | — | 1 | 5.91 |
| CHEMBL3659977 | — | — | 1 | 5.91 |
| CHEMBL3659984 | — | — | 1 | 5.29 |
| CHEMBL3659981 | — | — | 1 | 5.06 |
| CHEMBL3659986 | — | — | 1 | 4.91 |
| CHEMBL3659982 | — | — | 1 | 4.82 |
| CHEMBL3659983 | — | — | 1 | 4.52 |
| CHEMBL3659987 | — | — | 1 | 4.27 |
| CHEMBL3659985 | — | — | 1 | - |
| CHEMBL3659988 | — | — | 1 | - |
| CHEMBL3659989 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3659990 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3659991 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3659971 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL3659972 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL3659976 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3659978 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL3659974 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3659980 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3659975 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL3659977 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL3659984 | — | IC50 | = | 5170.0 | nM | 5.29 |
| CHEMBL3659981 | — | IC50 | = | 8790.0 | nM | 5.06 |
| CHEMBL3659986 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL3659982 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL3659983 | — | IC50 | = | 30300.0 | nM | 4.52 |
| CHEMBL3659987 | — | IC50 | = | 53900.0 | nM | 4.27 |
| CHEMBL3659985 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3659988 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3659989 | — | IC50 | > | 100000.0 | nM | - |