Assay Detail
Binding
CHEMBL3382735
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Inhibition of JAK1 in human whole blood assessed as inhibition of IL-6-induced pSTAT1
8
Total Activities
8
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 |
Publication
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.70 | 7.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.13 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 6.20 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.98 |
| CHEMBL3360356 | — | — | 1 | 5.56 |
| CHEMBL3360355 | — | — | 1 | 5.35 |
| CHEMBL3360353 | — | — | 1 | 5.25 |
| CHEMBL3360357 | — | — | 1 | 5.21 |
| CHEMBL3360840 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 629.0 | nM | 6.20 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 1053.0 | nM | 5.98 |
| CHEMBL3360356 | — | IC50 | = | 2749.0 | nM | 5.56 |
| CHEMBL3360355 | — | IC50 | = | 4467.0 | nM | 5.35 |
| CHEMBL3360353 | — | IC50 | = | 5590.0 | nM | 5.25 |
| CHEMBL3360357 | — | IC50 | = | 6152.0 | nM | 5.21 |
| CHEMBL3360840 | — | IC50 | = | 11900.0 | nM | 4.92 |