Assay Detail
Binding
CHEMBL5510096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of tracer 236 from CDK8/cyclin C (unknown origin) preincubated for 15 mins followed by tracer addition and measured after 60 mins by FRET based lanthascreen assay
17
Total Activities
17
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
Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.67 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5561973 | — | — | 1 | 8.68 |
| CHEMBL5532008 | — | — | 1 | 8.19 |
| CHEMBL5560894 | — | — | 1 | 8.19 |
| CHEMBL5559097 | — | — | 1 | 8.10 |
| CHEMBL5562755 | — | — | 1 | 7.97 |
| CHEMBL5543020 | — | — | 1 | 7.95 |
| CHEMBL4225966 | SEL-120 FREE BASE | 1.0 | 1 | 7.85 |
| CHEMBL5512552 | — | — | 1 | 7.78 |
| CHEMBL5555428 | — | — | 1 | 7.70 |
| CHEMBL5559293 | — | — | 1 | 7.47 |
| CHEMBL5557301 | — | — | 1 | 7.46 |
| CHEMBL5550075 | — | — | 1 | 7.44 |
| CHEMBL5523566 | — | — | 1 | 7.31 |
| CHEMBL5542174 | — | — | 1 | 7.04 |
| CHEMBL5561031 | — | — | 1 | 6.86 |
| CHEMBL5523465 | — | — | 1 | 6.78 |
| CHEMBL5561332 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5561973 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5532008 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5560894 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5559097 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5562755 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5543020 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4225966 | SEL-120 FREE BASE | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5512552 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL5555428 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5559293 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL5557301 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5550075 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL5523566 | — | IC50 | = | 48.6 | nM | 7.31 |
| CHEMBL5542174 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5561031 | — | IC50 | = | 139.3 | nM | 6.86 |
| CHEMBL5523465 | — | IC50 | = | 165.6 | nM | 6.78 |
| CHEMBL5561332 | — | IC50 | > | 1000.0 | nM | - |