Assay Detail
Binding
CHEMBL4414800
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TYK2 JH2 domain in mouse whole blood assessed as inhibition of IFNalpha-induced STAT1 phosphorylation preincubated for 1 hr followed by IFNalpha stimulation and measured after 15 mins by fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL2321619) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.50 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4530719 | — | — | 1 | 7.08 |
| CHEMBL4440718 | — | — | 1 | 6.92 |
| CHEMBL4544320 | — | — | 1 | 6.47 |
| CHEMBL4444178 | — | — | 1 | 6.47 |
| CHEMBL4583185 | — | — | 1 | 6.42 |
| CHEMBL4526283 | — | — | 1 | 6.35 |
| CHEMBL4444169 | — | — | 1 | 6.22 |
| CHEMBL4438202 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4530719 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4440718 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4544320 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4444178 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4583185 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4526283 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4444169 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4438202 | — | IC50 | = | 830.0 | nM | 6.08 |