Assay Detail
Binding
CHEMBL3376518
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Inhibition of JAK3/JAK1 in human PBMC expressing CD3 assessed as inhibition of IL-2-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 6.94 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.55 |
| CHEMBL3335691 | — | — | 1 | 7.31 |
| CHEMBL3335686 | — | — | 1 | 7.25 |
| CHEMBL3335685 | — | — | 1 | 7.15 |
| CHEMBL3335687 | — | — | 1 | 7.08 |
| CHEMBL3335690 | — | — | 1 | 7.04 |
| CHEMBL3335692 | — | — | 1 | 6.68 |
| CHEMBL3335684 | — | — | 1 | 6.67 |
| CHEMBL3335683 | — | — | 1 | 6.39 |
| CHEMBL3335689 | — | — | 1 | 6.28 |
| CHEMBL3335688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3335691 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3335686 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3335685 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3335687 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3335690 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3335692 | — | EC50 | = | 209.0 | nM | 6.68 |
| CHEMBL3335684 | — | EC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3335683 | — | EC50 | = | 406.0 | nM | 6.39 |
| CHEMBL3335689 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3335688 | — | EC50 | - | — | - |