Assay Detail
Binding
CHEMBL4714135
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Inhibition of human JAK2 by radiometric assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293F |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.95 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4743499 | — | — | 1 | 10.00 |
| CHEMBL4753959 | — | — | 1 | 9.89 |
| CHEMBL4750568 | — | — | 1 | 9.82 |
| CHEMBL4745155 | — | — | 1 | 9.59 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.40 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 9.12 |
| CHEMBL2002099 | — | — | 1 | 9.04 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.54 |
| CHEMBL4762807 | — | — | 1 | 8.44 |
| CHEMBL1287854 | — | — | 1 | 8.30 |
| CHEMBL4785050 | — | — | 1 | 8.19 |
| CHEMBL4744236 | — | — | 1 | 8.09 |
| CHEMBL4760892 | — | — | 1 | 7.94 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL4788363 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4743499 | — | IC50 | = | 0.099 | nM | 10.00 |
| CHEMBL4753959 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4750568 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4745155 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL2002099 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4762807 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1287854 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4785050 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4744236 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4760892 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL2105759 | BARICITINIB | IC50 | = | 0.29 | nM | - |
| CHEMBL4788363 | — | IC50 | < | 0.05 | nM | - |