Assay Detail
Binding
CHEMBL2329555
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Inhibition of JAK3/JAK1 in human whole blood expressing CD13 assessed as inhibition of IL-2-stimulated STAT5a 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 |
| Tissue | Blood |
| 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 | 5.92 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.27 |
| CHEMBL2325896 | — | — | 1 | 6.29 |
| CHEMBL2325894 | — | — | 1 | 6.09 |
| CHEMBL2325895 | — | — | 1 | 6.00 |
| CHEMBL2325906 | — | — | 1 | 5.96 |
| CHEMBL2325898 | — | — | 1 | 5.94 |
| CHEMBL2325903 | — | — | 1 | 5.61 |
| CHEMBL2325912 | — | — | 1 | 5.30 |
| CHEMBL2325904 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2325896 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL2325894 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL2325895 | — | IC50 | = | 1008.0 | nM | 6.00 |
| CHEMBL2325906 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL2325898 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL2325903 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL2325912 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL2325904 | — | IC50 | = | 15700.0 | nM | 4.80 |