Assay Detail
Binding
CHEMBL3854933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of COT in LPS-stimulated human PBMC assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by LPS stimulation for 12 mins by flow cytometric analysis
8
Total Activities
8
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 |
Target
Mitogen-activated protein kinase kinase kinase 8 (CHEMBL4899) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.79 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3912476 | — | — | 1 | 7.52 |
| CHEMBL3939592 | — | — | 1 | 7.22 |
| CHEMBL3890505 | — | — | 1 | 7.10 |
| CHEMBL3927501 | — | — | 1 | 6.92 |
| CHEMBL3899461 | — | — | 1 | 6.55 |
| CHEMBL3918552 | — | — | 1 | 6.55 |
| CHEMBL3910848 | — | — | 1 | 6.27 |
| CHEMBL3944315 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3912476 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3939592 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3890505 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3927501 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3899461 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3918552 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3910848 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3944315 | — | IC50 | = | 620.0 | nM | 6.21 |