Assay Detail
Binding
CHEMBL3854940
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of COT in LPS-stimulated human whole blood assessed as reduction in TNFalpha release incubated for 30 mins followed by stimulation with LPS for 3 hrs by HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 7 | 6.23 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3912476 | — | — | 1 | 7.10 |
| CHEMBL3939592 | — | — | 1 | 6.70 |
| CHEMBL3890505 | — | — | 1 | 6.22 |
| CHEMBL3927501 | — | — | 1 | 6.00 |
| CHEMBL3910848 | — | — | 1 | 5.75 |
| CHEMBL3899461 | — | — | 1 | 5.60 |
| CHEMBL3918552 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3912476 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3939592 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3890505 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3927501 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL3910848 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL3899461 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3918552 | — | IC50 | > | 10000.0 | nM | - |