Assay Detail
Binding
CHEMBL4404829
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Inhibition of JAK2/JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation pre-incubated for 30 mins before GM-CSF stimulation for 30 mins AlphaLISAassay
12
Total Activities
12
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 |
Publication
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.92 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588333 | — | — | 1 | 7.55 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.42 |
| CHEMBL4439418 | — | — | 1 | 7.41 |
| CHEMBL4537718 | — | — | 1 | 7.16 |
| CHEMBL4473572 | — | — | 1 | 7.08 |
| CHEMBL4563534 | — | — | 1 | 7.05 |
| CHEMBL4437638 | — | — | 1 | 6.90 |
| CHEMBL4514898 | — | — | 1 | 6.83 |
| CHEMBL4456630 | — | — | 1 | 6.61 |
| CHEMBL4582390 | — | — | 1 | 6.40 |
| CHEMBL4447497 | — | — | 1 | 5.71 |
| CHEMBL4470339 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588333 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4439418 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4537718 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4473572 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4563534 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4437638 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4514898 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4456630 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4582390 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL4447497 | — | IC50 | = | 1962.0 | nM | 5.71 |
| CHEMBL4470339 | — | IC50 | - | — | - |