Assay Detail
Binding
CHEMBL2013353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TBK1-mediated NFkappaB activation expressed in ds-RNA activated HEK293 cells coexpressing TLR3 after 4.5 hrs by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase TBK1 (CHEMBL5408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.51 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2011940 | — | — | 1 | 8.40 |
| CHEMBL2011933 | — | — | 1 | 8.22 |
| CHEMBL2011934 | — | — | 1 | 8.22 |
| CHEMBL2011936 | — | — | 1 | 8.10 |
| CHEMBL2011930 | — | — | 1 | 7.96 |
| CHEMBL2011941 | — | — | 1 | 7.92 |
| CHEMBL2011929 | — | — | 1 | 7.85 |
| CHEMBL2011945 | — | — | 1 | 7.77 |
| CHEMBL2011932 | — | — | 1 | 7.70 |
| CHEMBL2011931 | — | — | 1 | 7.60 |
| CHEMBL2011939 | — | — | 1 | 7.58 |
| CHEMBL2010815 | — | — | 1 | 7.47 |
| CHEMBL2011944 | — | — | 1 | 7.46 |
| CHEMBL2011935 | — | — | 1 | 7.40 |
| CHEMBL2011928 | — | — | 1 | 7.14 |
| CHEMBL2011927 | — | — | 1 | 7.12 |
| CHEMBL2011937 | — | — | 1 | 7.08 |
| CHEMBL2011938 | — | — | 1 | 7.06 |
| CHEMBL2011926 | — | — | 1 | 6.96 |
| CHEMBL2011943 | — | — | 1 | 6.86 |
| CHEMBL2011942 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2011940 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2011933 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2011934 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2011936 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2011930 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2011941 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2011929 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2011945 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2011932 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2011931 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2011939 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2010815 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2011944 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2011935 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2011928 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2011927 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2011937 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2011938 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2011926 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL2011943 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL2011942 | — | EC50 | = | 1460.0 | nM | 5.84 |