Assay Detail
Binding
CHEMBL5319087
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Inhibition of JAK1/JAK3 in human M07E cells assessed as reduction of IL-15 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-15 stimulation and measured after 15 mins by flow cytometry analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | M07E |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.54 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 8.30 |
| CHEMBL4297507 | DELGOCITINIB | 3.0 | 1 | 8.05 |
| CHEMBL3622821 | UPADACITINIB | 4.0 | 1 | 7.89 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.75 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.66 |
| CHEMBL5403330 | — | — | 1 | 7.39 |
| CHEMBL5409666 | — | — | 1 | 7.35 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 7.33 |
| CHEMBL4747591 | — | — | 1 | 7.27 |
| CHEMBL5270549 | — | — | 1 | 7.27 |
| CHEMBL5433426 | — | — | 1 | 7.18 |
| CHEMBL5415586 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4297507 | DELGOCITINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3622821 | UPADACITINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5403330 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5409666 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4747591 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5270549 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5433426 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5415586 | — | IC50 | = | 85.0 | nM | 7.07 |