Assay Detail
Binding
CHEMBL4380518
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length human N-terminal His-tagged TBK1 using biotin-labelled Ahx-GDEDFSSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubated for 30 mins in presence of 1 mM of ATP by TR-FRET assay
37
Total Activities
37
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
Serine/threonine-protein kinase TBK1 (CHEMBL5408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.36 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454902 | — | — | 1 | 8.30 |
| CHEMBL4436188 | — | — | 1 | 8.22 |
| CHEMBL4566796 | — | — | 1 | 8.15 |
| CHEMBL4538751 | — | — | 1 | 7.77 |
| CHEMBL4435393 | — | — | 1 | 7.75 |
| CHEMBL4537673 | BAY-985 | — | 1 | 7.52 |
| CHEMBL577784 | BX-795 | — | 1 | 7.35 |
| CHEMBL4543618 | — | — | 1 | 7.30 |
| CHEMBL4468020 | — | — | 1 | 6.86 |
| CHEMBL4594167 | — | — | 1 | 6.81 |
| CHEMBL4453292 | — | — | 1 | 6.78 |
| CHEMBL4553949 | — | — | 1 | 6.43 |
| CHEMBL4515413 | — | — | 1 | 6.41 |
| CHEMBL4451595 | — | — | 1 | 6.41 |
| CHEMBL4552254 | — | — | 1 | 6.36 |
| CHEMBL4453481 | — | — | 1 | 6.28 |
| CHEMBL4459120 | — | — | 1 | 6.21 |
| CHEMBL4455930 | — | — | 1 | 6.08 |
| CHEMBL4450510 | — | — | 1 | 5.90 |
| CHEMBL4456062 | — | — | 1 | 5.86 |
| CHEMBL4483062 | — | — | 1 | 5.72 |
| CHEMBL4587843 | — | — | 1 | 5.69 |
| CHEMBL4436416 | — | — | 1 | 5.68 |
| CHEMBL4549459 | — | — | 1 | 5.64 |
| CHEMBL4577511 | — | — | 1 | 5.60 |
| CHEMBL4573638 | — | — | 1 | 5.58 |
| CHEMBL4438389 | — | — | 1 | 5.43 |
| CHEMBL4462056 | — | — | 1 | 5.29 |
| CHEMBL4521346 | — | — | 1 | 5.29 |
| CHEMBL4566710 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454902 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4436188 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4566796 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4538751 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4435393 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4537673 | BAY-985 | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL577784 | BX-795 | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4543618 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4468020 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4594167 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4453292 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4553949 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4515413 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL4451595 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL4552254 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL4453481 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4459120 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL4455930 | — | IC50 | = | 829.0 | nM | 6.08 |
| CHEMBL4450510 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4456062 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL4483062 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL4587843 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4436416 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4549459 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL4577511 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL4573638 | — | IC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL4438389 | — | IC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL4521346 | — | IC50 | = | 5110.0 | nM | 5.29 |
| CHEMBL4462056 | — | IC50 | = | 5070.0 | nM | 5.29 |
| CHEMBL4566710 | — | IC50 | = | 5290.0 | nM | 5.28 |
| CHEMBL4575832 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4461416 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL4538591 | BAY-440 | IC50 | > | 20000.0 | nM | - |
| CHEMBL4547610 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4466150 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4524534 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4545291 | — | IC50 | > | 20000.0 | nM | - |