Assay Detail
Binding
CHEMBL3377096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a 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 | 9 — Direct 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 | 5.85 | 6.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.74 |
| CHEMBL3335685 | — | — | 1 | 6.34 |
| CHEMBL3335686 | — | — | 1 | 6.11 |
| CHEMBL3335687 | — | — | 1 | 6.10 |
| CHEMBL3335691 | — | — | 1 | 5.74 |
| CHEMBL3335683 | — | — | 1 | 5.69 |
| CHEMBL3335692 | — | — | 1 | 5.57 |
| CHEMBL3335690 | — | — | 1 | 5.43 |
| CHEMBL3335684 | — | — | 1 | 5.40 |
| CHEMBL3335689 | — | — | 1 | 5.40 |
| CHEMBL3335688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | EC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3335685 | — | EC50 | = | 452.0 | nM | 6.34 |
| CHEMBL3335686 | — | EC50 | = | 778.0 | nM | 6.11 |
| CHEMBL3335687 | — | EC50 | = | 798.0 | nM | 6.10 |
| CHEMBL3335691 | — | EC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL3335683 | — | EC50 | = | 2045.0 | nM | 5.69 |
| CHEMBL3335692 | — | EC50 | = | 2665.0 | nM | 5.57 |
| CHEMBL3335690 | — | EC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL3335684 | — | EC50 | = | 3995.0 | nM | 5.40 |
| CHEMBL3335689 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL3335688 | — | EC50 | - | — | - |