Assay Detail
Binding
CHEMBL4402446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TYK2 JH2 domain in human whole blood assessed as decrease in IFNalpha/IL2-induced STAT phosphorylation preincubated for 1 hr followed by IFNalpha/IL2 stimulation and measured after 15 mins by fluorescence assay
22
Total Activities
22
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
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.57 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4442827 | — | — | 1 | 7.20 |
| CHEMBL4532948 | — | — | 1 | 7.09 |
| CHEMBL4439957 | — | — | 1 | 7.07 |
| CHEMBL4460368 | — | — | 1 | 7.05 |
| CHEMBL4571920 | — | — | 1 | 6.87 |
| CHEMBL4561123 | — | — | 1 | 6.63 |
| CHEMBL4443010 | — | — | 1 | 6.61 |
| CHEMBL4453441 | — | — | 1 | 6.57 |
| CHEMBL4543066 | — | — | 1 | 6.54 |
| CHEMBL4435047 | — | — | 1 | 6.50 |
| CHEMBL4454109 | — | — | 1 | 6.47 |
| CHEMBL4585272 | — | — | 1 | 6.46 |
| CHEMBL4579439 | — | — | 1 | 6.43 |
| CHEMBL4474801 | — | — | 1 | 6.42 |
| CHEMBL4466139 | — | — | 1 | 6.42 |
| CHEMBL4438296 | — | — | 1 | 6.42 |
| CHEMBL4437714 | — | — | 1 | 6.33 |
| CHEMBL4438107 | — | — | 1 | 6.12 |
| CHEMBL4434711 | — | — | 1 | 6.09 |
| CHEMBL4547009 | — | — | 1 | 6.09 |
| CHEMBL4293907 | — | — | 1 | - |
| CHEMBL4517542 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4442827 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4532948 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL4439957 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL4460368 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL4571920 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL4561123 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL4443010 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL4453441 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4543066 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL4435047 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL4454109 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4585272 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL4579439 | — | Ki | = | 371.0 | nM | 6.43 |
| CHEMBL4474801 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL4466139 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL4438296 | — | Ki | = | 384.0 | nM | 6.42 |
| CHEMBL4437714 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL4438107 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL4434711 | — | Ki | = | 811.0 | nM | 6.09 |
| CHEMBL4547009 | — | Ki | = | 817.0 | nM | 6.09 |
| CHEMBL4293907 | — | Ki | - | — | - | |
| CHEMBL4517542 | — | Ki | - | — | - |