Assay Detail
Binding
CHEMBL3854930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by caliper microfluidic mobility shift assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 | 25 | 7.03 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3912476 | — | — | 1 | 8.40 |
| CHEMBL3939592 | — | — | 1 | 8.22 |
| CHEMBL3890505 | — | — | 1 | 8.05 |
| CHEMBL3927501 | — | — | 1 | 8.05 |
| CHEMBL3899461 | — | — | 1 | 7.80 |
| CHEMBL3910848 | — | — | 1 | 7.70 |
| CHEMBL3918552 | — | — | 1 | 7.66 |
| CHEMBL3944315 | — | — | 1 | 7.42 |
| CHEMBL3980906 | — | — | 1 | 7.40 |
| CHEMBL3937721 | — | — | 1 | 7.30 |
| CHEMBL3936462 | — | — | 1 | 7.10 |
| CHEMBL3919207 | — | — | 1 | 7.05 |
| CHEMBL3908516 | — | — | 1 | 7.02 |
| CHEMBL3966844 | — | — | 1 | 7.00 |
| CHEMBL3928098 | — | — | 1 | 6.82 |
| CHEMBL3955726 | — | — | 1 | 6.80 |
| CHEMBL3910291 | — | — | 1 | 6.70 |
| CHEMBL3937086 | — | — | 1 | 6.17 |
| CHEMBL3909782 | — | — | 1 | 6.10 |
| CHEMBL3911325 | — | — | 1 | 5.89 |
| CHEMBL3987154 | — | — | 1 | 5.89 |
| CHEMBL3928698 | — | — | 1 | 5.58 |
| CHEMBL3981321 | — | — | 1 | 5.46 |
| CHEMBL3902393 | — | — | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3912476 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3939592 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3890505 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3927501 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3899461 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3910848 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3918552 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3944315 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3980906 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3937721 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3936462 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3919207 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3908516 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3966844 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3928098 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3955726 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3910291 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3937086 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3909782 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3911325 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3987154 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3928698 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3981321 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3902393 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | IC50 | > | 25000.0 | nM | - |