Assay Detail
Binding
CHEMBL3784147
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Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CD34+ cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.09 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.10 |
| CHEMBL3780091 | — | — | 1 | 7.32 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.15 |
| CHEMBL3780467 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3780091 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3780467 | — | IC50 | = | 1699.0 | nM | 5.77 |