Assay Detail
Binding
CHEMBL5384758
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Inhibition of His tagged human recombinant CDK8/Cyclin C expressed in baculovirus expression system incubated for 15 mins by FRET-based LanthaScreen binding competition assay
24
Total Activities
24
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 Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.50 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5435821 | — | — | 1 | 9.43 |
| CHEMBL5434183 | — | — | 1 | 9.40 |
| CHEMBL5409410 | — | — | 1 | 9.40 |
| CHEMBL5405004 | — | — | 1 | 9.32 |
| CHEMBL5414359 | — | — | 1 | 9.31 |
| CHEMBL5416117 | — | — | 1 | 9.20 |
| CHEMBL5396725 | — | — | 1 | 9.15 |
| CHEMBL5402477 | — | — | 1 | 9.15 |
| CHEMBL5411825 | — | — | 1 | 9.08 |
| CHEMBL5440319 | — | — | 1 | 9.06 |
| CHEMBL5416758 | — | — | 1 | 9.05 |
| CHEMBL5425043 | — | — | 1 | 8.82 |
| CHEMBL5423457 | — | — | 1 | 8.48 |
| CHEMBL5429467 | — | — | 1 | 8.32 |
| CHEMBL5417604 | — | — | 1 | 8.27 |
| CHEMBL5432423 | — | — | 1 | 8.21 |
| CHEMBL5427899 | — | — | 1 | 8.13 |
| CHEMBL4225966 | SEL-120 FREE BASE | 1.0 | 1 | 7.85 |
| CHEMBL5416134 | — | — | 1 | 7.77 |
| CHEMBL5412471 | — | — | 1 | 7.45 |
| CHEMBL5397969 | — | — | 1 | 7.10 |
| CHEMBL5436530 | — | — | 1 | 7.08 |
| CHEMBL5402190 | — | — | 1 | 6.56 |
| CHEMBL5406025 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5435821 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL5434183 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5409410 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5405004 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL5414359 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL5416117 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL5396725 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5402477 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL5411825 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL5440319 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL5416758 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5425043 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5423457 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL5429467 | — | IC50 | = | 4.82 | nM | 8.32 |
| CHEMBL5417604 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5432423 | — | IC50 | = | 6.14 | nM | 8.21 |
| CHEMBL5427899 | — | IC50 | = | 7.32 | nM | 8.13 |
| CHEMBL4225966 | SEL-120 FREE BASE | IC50 | = | 14.11 | nM | 7.85 |
| CHEMBL5416134 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL5412471 | — | IC50 | = | 35.7 | nM | 7.45 |
| CHEMBL5397969 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5436530 | — | IC50 | = | 82.9 | nM | 7.08 |
| CHEMBL5402190 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL5406025 | — | IC50 | > | 1000.0 | nM | - |