Assay Detail
Binding
CHEMBL4251840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(R)-N-(1-(3-(8-methyl-5-(methylamino)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridin-2-yl)phenyl)ethyl)-2-(methylsulfonyl)benzamide from N-terminal His-tagged TYK2 JH2 domain (unknown origin) after 30 mins by scintillation proximity assay
24
Total Activities
24
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
Identification of imidazo[1,2-<i>b</i>]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4289426 | — | — | 1 | 8.70 |
| CHEMBL4279883 | — | — | 1 | 8.40 |
| CHEMBL4291611 | — | — | 1 | 8.40 |
| CHEMBL4295039 | — | — | 1 | 8.30 |
| CHEMBL4287761 | — | — | 1 | 8.22 |
| CHEMBL4285841 | — | — | 1 | 8.22 |
| CHEMBL4279157 | — | — | 1 | 8.15 |
| CHEMBL4290130 | — | — | 1 | 8.10 |
| CHEMBL4291200 | — | — | 1 | 8.10 |
| CHEMBL4293907 | — | — | 1 | 8.10 |
| CHEMBL4283351 | — | — | 1 | 7.89 |
| CHEMBL4278757 | — | — | 1 | 7.82 |
| CHEMBL4287081 | — | — | 1 | 7.77 |
| CHEMBL4285755 | — | — | 1 | 7.66 |
| CHEMBL4289875 | — | — | 1 | 7.62 |
| CHEMBL4293510 | — | — | 1 | 7.60 |
| CHEMBL4287153 | — | — | 1 | 7.57 |
| CHEMBL4293619 | — | — | 1 | 7.50 |
| CHEMBL4286006 | — | — | 1 | 7.30 |
| CHEMBL4281304 | — | — | 1 | 7.18 |
| CHEMBL4282627 | — | — | 1 | 6.96 |
| CHEMBL4283724 | — | — | 1 | 6.66 |
| CHEMBL4289149 | — | — | 1 | 6.32 |
| CHEMBL4285530 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4289426 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4279883 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4291611 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4295039 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4287761 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4285841 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4279157 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4290130 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4291200 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4293907 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4283351 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4278757 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4287081 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4285755 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4289875 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4293510 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4287153 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4293619 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4286006 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4281304 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4282627 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4283724 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4289149 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4285530 | — | IC50 | = | 500.0 | nM | 6.30 |