Assay Detail
Binding
CHEMBL3377097
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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
11
Total Activities
11
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
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.91 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.77 |
| CHEMBL3335691 | — | — | 1 | 6.30 |
| CHEMBL3335686 | — | — | 1 | 6.24 |
| CHEMBL3335685 | — | — | 1 | 6.20 |
| CHEMBL3335687 | — | — | 1 | 6.02 |
| CHEMBL3335690 | — | — | 1 | 5.86 |
| CHEMBL3335683 | — | — | 1 | 5.63 |
| CHEMBL3335684 | — | — | 1 | 5.54 |
| CHEMBL3335692 | — | — | 1 | 5.40 |
| CHEMBL3335689 | — | — | 1 | 5.16 |
| CHEMBL3335688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3335691 | — | EC50 | = | 505.0 | nM | 6.30 |
| CHEMBL3335686 | — | EC50 | = | 578.0 | nM | 6.24 |
| CHEMBL3335685 | — | EC50 | = | 633.0 | nM | 6.20 |
| CHEMBL3335687 | — | EC50 | = | 956.0 | nM | 6.02 |
| CHEMBL3335690 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL3335683 | — | EC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL3335684 | — | EC50 | = | 2865.0 | nM | 5.54 |
| CHEMBL3335692 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3335689 | — | EC50 | = | 6945.0 | nM | 5.16 |
| CHEMBL3335688 | — | EC50 | - | — | - |