Assay Detail
Binding
CHEMBL5131233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TYK2 in human Jurkat cells assessed as reduction in IFNalpha induced STAT3 phosphorylation incubated for 24 hrs by HTRF assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel TYK2 Inhibitors with an <i>N</i>-(Methyl-<i>d</i> <sub>3</sub>)pyridazine-3-carboxamide Skeleton for the Treatment of Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.24 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5190418 | — | — | 1 | 9.07 |
| CHEMBL5180664 | — | — | 1 | 9.01 |
| CHEMBL5209315 | — | — | 1 | 9.00 |
| CHEMBL5193226 | — | — | 1 | 8.96 |
| CHEMBL5196735 | — | — | 1 | 8.96 |
| CHEMBL5184093 | — | — | 1 | 8.96 |
| CHEMBL5203217 | — | — | 1 | 8.89 |
| CHEMBL5203256 | — | — | 1 | 8.85 |
| CHEMBL5207953 | — | — | 1 | 8.80 |
| CHEMBL5191508 | — | — | 1 | 8.72 |
| CHEMBL5194842 | — | — | 1 | 8.64 |
| CHEMBL5198448 | — | — | 1 | 8.54 |
| CHEMBL5204955 | — | — | 1 | 8.51 |
| CHEMBL4435170 | DEUCRAVACITINIB | 4.0 | 1 | 8.49 |
| CHEMBL5179468 | — | — | 1 | 8.42 |
| CHEMBL5200056 | — | — | 1 | 8.30 |
| CHEMBL5177410 | — | — | 1 | 8.23 |
| CHEMBL5189220 | — | — | 1 | 8.02 |
| CHEMBL5173760 | — | — | 1 | 7.85 |
| CHEMBL5188967 | — | — | 1 | 7.82 |
| CHEMBL5171417 | — | — | 1 | 7.80 |
| CHEMBL5189913 | — | — | 1 | 7.75 |
| CHEMBL5204171 | — | — | 1 | 7.75 |
| CHEMBL5175777 | — | — | 1 | 7.54 |
| CHEMBL5182426 | — | — | 1 | 7.50 |
| CHEMBL5205855 | — | — | 1 | 7.41 |
| CHEMBL5179489 | — | — | 1 | 7.24 |
| CHEMBL5184123 | — | — | 1 | 7.17 |
| CHEMBL5181780 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5190418 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL5180664 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5209315 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5193226 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5196735 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5184093 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5203217 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5203256 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5207953 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5191508 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5194842 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5198448 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5204955 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4435170 | DEUCRAVACITINIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5179468 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5200056 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5177410 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5189220 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5173760 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5188967 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5171417 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5189913 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5204171 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5175777 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5182426 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5205855 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5179489 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5184123 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5181780 | — | IC50 | = | 129.0 | nM | 6.89 |