Assay Detail
Binding
CHEMBL5365709
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 reduction in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by IFNalpha stimulation and measured after 15 mins by fluorescence assay
27
Total Activities
27
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
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.07 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5413544 | — | — | 1 | 7.96 |
| CHEMBL5439728 | — | — | 1 | 7.82 |
| CHEMBL5437122 | — | — | 1 | 7.80 |
| CHEMBL5411149 | — | — | 1 | 7.66 |
| CHEMBL5412034 | — | — | 1 | 7.55 |
| CHEMBL5403115 | — | — | 1 | 7.48 |
| CHEMBL5408060 | — | — | 1 | 7.42 |
| CHEMBL5427107 | — | — | 1 | 7.39 |
| CHEMBL5437552 | — | — | 1 | 7.39 |
| CHEMBL5409590 | — | — | 1 | 7.28 |
| CHEMBL5420187 | — | — | 1 | 7.28 |
| CHEMBL5433636 | — | — | 1 | 7.22 |
| CHEMBL5415132 | — | — | 1 | 7.13 |
| CHEMBL5403477 | — | — | 1 | 7.12 |
| CHEMBL5396654 | — | — | 1 | 7.03 |
| CHEMBL5440225 | — | — | 1 | 7.01 |
| CHEMBL5438688 | — | — | 1 | 6.97 |
| CHEMBL5430970 | — | — | 1 | 6.91 |
| CHEMBL5418485 | — | — | 1 | 6.88 |
| CHEMBL5405178 | — | — | 1 | 6.88 |
| CHEMBL5399546 | — | — | 1 | 6.76 |
| CHEMBL5401385 | — | — | 1 | 6.54 |
| CHEMBL5406364 | — | — | 1 | 6.53 |
| CHEMBL5411146 | — | — | 1 | 6.51 |
| CHEMBL5403572 | — | — | 1 | 6.47 |
| CHEMBL5409445 | — | — | 1 | 6.31 |
| CHEMBL5416323 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5413544 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5439728 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5437122 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5411149 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5412034 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5403115 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5408060 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5427107 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5437552 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5409590 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5420187 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5433636 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5415132 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5403477 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5396654 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5440225 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5438688 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5430970 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5418485 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5405178 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5399546 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL5401385 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL5406364 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL5411146 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL5403572 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL5409445 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL5416323 | — | IC50 | = | 2610.0 | nM | 5.58 |