Assay Detail
Binding
CHEMBL5319083
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Inhibition of JAK1 JH1 domain (unknown origin) using FITC-Ahx-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology
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 and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.99 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622821 | UPADACITINIB | 4.0 | 1 | 9.10 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 8.62 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.28 |
| CHEMBL4297507 | DELGOCITINIB | 3.0 | 1 | 8.05 |
| CHEMBL5409666 | — | — | 1 | 8.05 |
| CHEMBL4747591 | — | — | 1 | 7.96 |
| CHEMBL5415586 | — | — | 1 | 7.85 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.77 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 7.70 |
| CHEMBL5403330 | — | — | 1 | 7.66 |
| CHEMBL5433426 | — | — | 1 | 7.54 |
| CHEMBL5270549 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622821 | UPADACITINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2105759 | BARICITINIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4297507 | DELGOCITINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5409666 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4747591 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5415586 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5403330 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5433426 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5270549 | — | IC50 | = | 50.0 | nM | 7.30 |