Assay Detail
Binding
CHEMBL4029554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human His-tagged CDK8/Cyclin C expressed in baculovirus expression system using Ulight-GS peptide as substrate measured after 30 mins by TR-FRET based LANCE assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 9.08 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4078454 | — | — | 1 | 9.70 |
| CHEMBL4096487 | — | — | 1 | 9.40 |
| CHEMBL4072496 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4078454 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4096487 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4072496 | — | IC50 | = | 7.0 | nM | 8.15 |