Assay Detail
Binding
CHEMBL3779189
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Inhibition of CDK8 (unknown origin) expressed in 7dF3 clone of human HEK293 cells preincubated for 2 hrs followed by addition of beta-estradiol by luciferase assay
32
Total Activities
32
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 |
Publication
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.02 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775935 | — | — | 1 | 8.30 |
| CHEMBL3774402 | — | — | 1 | 8.05 |
| CHEMBL3774885 | — | — | 1 | 7.96 |
| CHEMBL3775384 | — | — | 1 | 7.89 |
| CHEMBL3774959 | — | — | 1 | 7.75 |
| CHEMBL3775134 | — | — | 1 | 7.60 |
| CHEMBL3775773 | — | — | 1 | 7.57 |
| CHEMBL3775317 | — | — | 1 | 7.38 |
| CHEMBL3775024 | — | — | 1 | 7.37 |
| CHEMBL3775321 | — | — | 1 | 7.28 |
| CHEMBL3775535 | — | — | 1 | 7.26 |
| CHEMBL3775076 | — | — | 1 | 7.25 |
| CHEMBL3775576 | — | — | 1 | 7.19 |
| CHEMBL3775775 | — | — | 1 | 7.12 |
| CHEMBL3775547 | — | — | 1 | 7.09 |
| CHEMBL3775423 | — | — | 1 | 7.03 |
| CHEMBL3775680 | — | — | 1 | 7.00 |
| CHEMBL3775496 | — | — | 1 | 6.96 |
| CHEMBL3775562 | — | — | 1 | 6.85 |
| CHEMBL3775123 | — | — | 1 | 6.80 |
| CHEMBL3775519 | — | — | 1 | 6.70 |
| CHEMBL3775614 | — | — | 1 | 6.57 |
| CHEMBL3774509 | — | — | 1 | 6.50 |
| CHEMBL3774400 | — | — | 1 | 6.15 |
| CHEMBL3775895 | — | — | 1 | 5.82 |
| CHEMBL3775910 | — | — | 1 | 5.72 |
| CHEMBL3774757 | — | — | 1 | 5.72 |
| CHEMBL3774945 | — | — | 1 | 5.70 |
| CHEMBL3775049 | — | — | 1 | - |
| CHEMBL3774874 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775935 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3774402 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3774885 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3775384 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3774959 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3775134 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3775773 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3775317 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3775024 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3775321 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3775535 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3775076 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3775576 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3775775 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3775547 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3775423 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3775680 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3775496 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3775562 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3775123 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3775519 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3775614 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3774509 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL3774400 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3775895 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3775910 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3774757 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3774945 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3775049 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774874 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775578 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774744 | — | IC50 | > | 30000.0 | nM | - |