Assay Detail
Binding
CHEMBL5683044
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Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis
6
Total Activities
3
Compounds Tested
2
Activity Types
4
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Cell Type | T-cell |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.29 | 8.95 |
| pIC50 | 1 | - | - |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0005140 |
| EFO_ID | EFO_ID | - | — | HP:0001370 |
| EFO_TERM | EFO_TERM | - | — | autoimmune disease |
| EFO_TERM | EFO_TERM | - | — | rheumatoid arthritis |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301607 | FILGOTINIB | 4.0 | 2 | 8.95 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 2 | 7.12 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 1.127 | nM | 8.95 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 75.86 | nM | 7.12 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 1127.2 | nM | 5.95 |
| CHEMBL2105759 | BARICITINIB | pIC50 | - | — | - | |
| CHEMBL2105759 | BARICITINIB | IC50 | - | — | - |