Assay Detail
Binding
CHEMBL4742449
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Inhibition of CDK8 in human SW-620 cells assessed as reduction in STAT1 S727 phosphorylation pre-incubated for 1 hr before IFNgamma stimulation for 3 hrs by Western blot analysis
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SW-620 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Condensed tricyclic compounds as protein kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| INH | 13 | - | - |
| IC50 | 1 | 8.82 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4791276 | — | — | 1 | 8.82 |
| CHEMBL4785713 | — | — | 1 | - |
| CHEMBL4779550 | — | — | 1 | - |
| CHEMBL4790936 | — | — | 1 | - |
| CHEMBL4777501 | — | — | 1 | - |
| CHEMBL4789603 | — | — | 1 | - |
| CHEMBL4782696 | — | — | 1 | - |
| CHEMBL4777356 | — | — | 1 | - |
| CHEMBL4781993 | — | — | 1 | - |
| CHEMBL4776812 | — | — | 1 | - |
| CHEMBL4792305 | — | — | 1 | - |
| CHEMBL4793477 | — | — | 1 | - |
| CHEMBL4782203 | — | — | 1 | - |
| CHEMBL4778840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4791276 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4785713 | — | INH | < | 500.0 | nM | - |
| CHEMBL4779550 | — | INH | < | 500.0 | nM | - |
| CHEMBL4790936 | — | INH | < | 500.0 | nM | - |
| CHEMBL4777501 | — | INH | < | 500.0 | nM | - |
| CHEMBL4789603 | — | INH | < | 500.0 | nM | - |
| CHEMBL4782696 | — | INH | < | 500.0 | nM | - |
| CHEMBL4777356 | — | INH | < | 500.0 | nM | - |
| CHEMBL4781993 | — | INH | < | 500.0 | nM | - |
| CHEMBL4776812 | — | INH | < | 500.0 | nM | - |
| CHEMBL4792305 | — | INH | < | 500.0 | nM | - |
| CHEMBL4793477 | — | INH | < | 500.0 | nM | - |
| CHEMBL4782203 | — | INH | < | 500.0 | nM | - |
| CHEMBL4778840 | — | INH | < | 500.0 | nM | - |