Assay Detail
Binding
CHEMBL5375116
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Inhibition of JAK1/2-mediated STAT1 phosphorylation in human M07E cells preincubated for 30 mins followed by IFN-alpha stimulation measured after 15 mins by flow cytometry
17
Total Activities
17
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
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.04 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5422886 | — | — | 1 | 7.85 |
| CHEMBL5409953 | — | — | 1 | 7.43 |
| CHEMBL5396554 | — | — | 1 | 7.36 |
| CHEMBL5404574 | — | — | 1 | 7.35 |
| CHEMBL5407260 | — | — | 1 | 7.32 |
| CHEMBL5412967 | — | — | 1 | 7.24 |
| CHEMBL5420083 | — | — | 1 | 7.24 |
| CHEMBL5403897 | — | — | 1 | 7.22 |
| CHEMBL5279787 | — | — | 1 | 7.15 |
| CHEMBL5270549 | — | — | 1 | 7.07 |
| CHEMBL5424439 | — | — | 1 | 6.94 |
| CHEMBL5395839 | — | — | 1 | 6.73 |
| CHEMBL5417474 | — | — | 1 | 6.73 |
| CHEMBL5420971 | — | — | 1 | 6.54 |
| CHEMBL5431257 | — | — | 1 | 5.41 |
| CHEMBL5407329 | — | — | 1 | - |
| CHEMBL5271559 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5422886 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5409953 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5396554 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5404574 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5407260 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5412967 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5420083 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5403897 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5279787 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5270549 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5424439 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5395839 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL5417474 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL5420971 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL5431257 | — | IC50 | = | 3861.0 | nM | 5.41 |
| CHEMBL5407329 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5271559 | — | IC50 | > | 10000.0 | nM | - |