Assay Detail
Binding
CHEMBL4413157
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Binding affinity to wild-type partial length human CDK8 (M1 to T360 residues) expressed in bacterial expression system by Kinomescan assay
3
Total Activities
3
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
CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 6.50 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4080906 | — | — | 1 | 7.77 |
| CHEMBL4226806 | — | — | 1 | 6.08 |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4080906 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL4226806 | — | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL483321 | CP-724714 | Kd | = | 2300.0 | nM | 5.64 |