Assay Detail
Binding
CHEMBL3132510
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Inhibition of TBK1 in HEK293 cells after 4.5 hrs by ISRE-luciferase reporter gene assay in presence of poly I:C
21
Total Activities
21
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
Serine/threonine-protein kinase TBK1 (CHEMBL5408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.01 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2011933 | — | — | 1 | 8.22 |
| CHEMBL3125721 | — | — | 1 | 8.15 |
| CHEMBL2011936 | — | — | 1 | 8.10 |
| CHEMBL3125726 | — | — | 1 | 7.52 |
| CHEMBL3125727 | — | — | 1 | 7.43 |
| CHEMBL373751 | GSK-319347A | — | 1 | 7.14 |
| CHEMBL3125728 | — | — | 1 | 7.11 |
| CHEMBL3125729 | — | — | 1 | 7.05 |
| CHEMBL3125720 | — | — | 1 | 6.89 |
| CHEMBL3125730 | — | — | 1 | 6.87 |
| CHEMBL3125723 | — | — | 1 | 6.78 |
| CHEMBL3125731 | — | — | 1 | 6.77 |
| CHEMBL3125732 | — | — | 1 | 6.57 |
| CHEMBL3125733 | — | — | 1 | 6.07 |
| CHEMBL3125734 | — | — | 1 | 5.75 |
| CHEMBL3125722 | — | — | 1 | 5.66 |
| CHEMBL3125724 | — | — | 1 | - |
| CHEMBL3125738 | — | — | 1 | - |
| CHEMBL3125739 | — | — | 1 | - |
| CHEMBL3125740 | — | — | 1 | - |
| CHEMBL3125741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2011933 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3125721 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2011936 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3125726 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3125727 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL373751 | GSK-319347A | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3125728 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3125729 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3125720 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL3125730 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL3125723 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3125731 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3125732 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL3125733 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL3125734 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL3125722 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL3125724 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL3125738 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3125739 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3125740 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3125741 | — | IC50 | > | 30000.0 | nM | - |