Assay Detail
Binding
CHEMBL5658246
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Inhibition of human His-tagged/TEV fused recombinant JAK3 kinase domain (781 to 1124 residues) expressed in Sf9 cells in presence of ATP by ELISA assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.25 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.46 |
| CHEMBL4564280 | — | — | 1 | 8.05 |
| CHEMBL5188882 | — | — | 1 | 7.77 |
| CHEMBL4128410 | — | — | 1 | 7.29 |
| CHEMBL2322138 | — | — | 1 | 7.20 |
| CHEMBL4127174 | — | — | 1 | 6.65 |
| CHEMBL4125935 | — | — | 1 | 6.33 |
| CHEMBL4125798 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4564280 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5188882 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4128410 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2322138 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4127174 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4125935 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4125798 | — | IC50 | = | 548.0 | nM | 6.26 |