Assay Detail
Binding
CHEMBL5141277
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Inhibition of human TYK2 by FRET assay
15
Total Activities
15
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
Discovery of Hexahydrofuro[3,2-<i>b</i>]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.70 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189603 | — | — | 1 | 7.03 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.95 |
| CHEMBL5205480 | — | — | 1 | 6.83 |
| CHEMBL5185440 | — | — | 1 | 6.82 |
| CHEMBL5184019 | — | — | 1 | 6.78 |
| CHEMBL5182374 | — | — | 1 | 6.77 |
| CHEMBL5184187 | — | — | 1 | 6.73 |
| CHEMBL5190599 | — | — | 1 | 6.73 |
| CHEMBL5207354 | — | — | 1 | 6.63 |
| CHEMBL5185016 | — | — | 1 | 6.62 |
| CHEMBL5182065 | — | — | 1 | 6.47 |
| CHEMBL5191734 | — | — | 1 | 6.43 |
| CHEMBL5174210 | — | — | 1 | 6.37 |
| CHEMBL5203904 | — | — | 1 | - |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189603 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5205480 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL5185440 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5184019 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5182374 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5184187 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL5190599 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL5207354 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL5185016 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL5182065 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL5191734 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL5174210 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL5203904 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4085457 | RITLECITINIB | IC50 | > | 10000.0 | nM | - |