Assay Detail
Binding
CHEMBL2329052
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Inhibition of JAK2/JAK1 in human PBMC expressing CD14 assessed as inhibition of IFN-gamma-stimulated STAT1 phosphorylation after 30 mins by flow cytometric analysis
9
Total Activities
9
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
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.04 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325898 | — | — | 1 | 6.99 |
| CHEMBL2325896 | — | — | 1 | 6.85 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.77 |
| CHEMBL2325895 | — | — | 1 | 6.54 |
| CHEMBL2325912 | — | — | 1 | 5.65 |
| CHEMBL2325894 | — | — | 1 | 5.59 |
| CHEMBL2325906 | — | — | 1 | 5.59 |
| CHEMBL2325903 | — | — | 1 | 5.47 |
| CHEMBL2325904 | — | — | 1 | 4.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325898 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL2325896 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2325895 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL2325912 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL2325894 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2325906 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL2325903 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL2325904 | — | IC50 | = | 13200.0 | nM | 4.88 |