Assay Detail
Binding
CHEMBL5365708
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescein-labeled kinase tracer from His-TVMV-TYK2 JH2 (575 to 869 residues) (unknown origin) measured after 90 mins by HTRF assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 9.69 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5427107 | — | — | 1 | 11.00 |
| CHEMBL5437122 | — | — | 1 | 10.30 |
| CHEMBL5440225 | — | — | 1 | 10.30 |
| CHEMBL5412034 | — | — | 1 | 10.22 |
| CHEMBL5418485 | — | — | 1 | 10.15 |
| CHEMBL5413544 | — | — | 1 | 10.10 |
| CHEMBL5439728 | — | — | 1 | 10.05 |
| CHEMBL5416323 | — | — | 1 | 10.00 |
| CHEMBL5437552 | — | — | 1 | 10.00 |
| CHEMBL5411149 | — | — | 1 | 10.00 |
| CHEMBL5396654 | — | — | 1 | 10.00 |
| CHEMBL5411146 | — | — | 1 | 10.00 |
| CHEMBL5403477 | — | — | 1 | 9.70 |
| CHEMBL5405178 | — | — | 1 | 9.70 |
| CHEMBL5403115 | — | — | 1 | 9.70 |
| CHEMBL5403572 | — | — | 1 | 9.70 |
| CHEMBL5438688 | — | — | 1 | 9.52 |
| CHEMBL5408060 | — | — | 1 | 9.52 |
| CHEMBL5409590 | — | — | 1 | 9.40 |
| CHEMBL5399546 | — | — | 1 | 9.30 |
| CHEMBL5401385 | — | — | 1 | 9.22 |
| CHEMBL5420187 | — | — | 1 | 9.22 |
| CHEMBL5430970 | — | — | 1 | 9.10 |
| CHEMBL5415132 | — | — | 1 | 9.05 |
| CHEMBL5409445 | — | — | 1 | 9.00 |
| CHEMBL5406364 | — | — | 1 | 8.96 |
| CHEMBL5433636 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5427107 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5437122 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5440225 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5412034 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL5418485 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5413544 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5439728 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5416323 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5437552 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5411149 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5396654 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5411146 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5403477 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5405178 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5403115 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5403572 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5438688 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5408060 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5409590 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5399546 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5401385 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5420187 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5430970 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5415132 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5409445 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5406364 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5433636 | — | IC50 | = | 4.2 | nM | 8.38 |