Assay Detail
Binding
CHEMBL5348803
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Inhibition of CDK8 (unknown origin) in presence of ATP by ADP-Glo assay
23
Total Activities
23
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 |
Publication
Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.90 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4091294 | — | — | 1 | 7.45 |
| CHEMBL4225966 | SEL-120 FREE BASE | 1.0 | 1 | 7.43 |
| CHEMBL5421134 | — | — | 1 | 7.29 |
| CHEMBL3102859 | — | — | 1 | 7.22 |
| CHEMBL5441138 | — | — | 1 | 7.22 |
| CHEMBL5406308 | — | — | 1 | 7.21 |
| CHEMBL5434520 | — | — | 1 | 7.07 |
| CHEMBL5440418 | — | — | 1 | 7.01 |
| CHEMBL5399338 | — | — | 1 | 6.97 |
| CHEMBL5415489 | — | — | 1 | 6.93 |
| CHEMBL5431726 | — | — | 1 | 6.87 |
| CHEMBL5403765 | — | — | 1 | 6.85 |
| CHEMBL5409187 | — | — | 1 | 6.82 |
| CHEMBL5399686 | — | — | 1 | 6.79 |
| CHEMBL5409281 | — | — | 1 | 6.67 |
| CHEMBL2000568 | — | — | 1 | 6.67 |
| CHEMBL5412040 | — | — | 1 | 6.66 |
| CHEMBL5426252 | — | — | 1 | 6.65 |
| CHEMBL5412342 | — | — | 1 | 6.64 |
| CHEMBL5397227 | — | — | 1 | 6.58 |
| CHEMBL5083764 | — | — | 1 | 6.56 |
| CHEMBL5075969 | — | — | 1 | 6.34 |
| CHEMBL5076124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4091294 | — | IC50 | = | 35.2 | nM | 7.45 |
| CHEMBL4225966 | SEL-120 FREE BASE | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL5421134 | — | IC50 | = | 51.9 | nM | 7.29 |
| CHEMBL3102859 | — | IC50 | = | 60.3 | nM | 7.22 |
| CHEMBL5441138 | — | IC50 | = | 59.7 | nM | 7.22 |
| CHEMBL5406308 | — | IC50 | = | 62.4 | nM | 7.21 |
| CHEMBL5434520 | — | IC50 | = | 85.1 | nM | 7.07 |
| CHEMBL5440418 | — | IC50 | = | 98.4 | nM | 7.01 |
| CHEMBL5399338 | — | IC50 | = | 106.6 | nM | 6.97 |
| CHEMBL5415489 | — | IC50 | = | 116.2 | nM | 6.93 |
| CHEMBL5431726 | — | IC50 | = | 136.3 | nM | 6.87 |
| CHEMBL5403765 | — | IC50 | = | 142.5 | nM | 6.85 |
| CHEMBL5409187 | — | IC50 | = | 151.9 | nM | 6.82 |
| CHEMBL5399686 | — | IC50 | = | 162.1 | nM | 6.79 |
| CHEMBL5409281 | — | IC50 | = | 212.8 | nM | 6.67 |
| CHEMBL2000568 | — | IC50 | = | 215.6 | nM | 6.67 |
| CHEMBL5412040 | — | IC50 | = | 220.6 | nM | 6.66 |
| CHEMBL5426252 | — | IC50 | = | 224.8 | nM | 6.65 |
| CHEMBL5412342 | — | IC50 | = | 230.4 | nM | 6.64 |
| CHEMBL5397227 | — | IC50 | = | 264.8 | nM | 6.58 |
| CHEMBL5083764 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL5075969 | — | IC50 | = | 455.7 | nM | 6.34 |
| CHEMBL5076124 | — | IC50 | > | 500.0 | nM | - |