Assay Detail
Binding
CHEMBL5503710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2-mediated erythropoietin-induced STAT5 phosphorylation in human TF-1 cells pretreated for 60 mins followed by erythropoietin addition and measured after 15 mins by pacific orange/pacific blue NHS esters based Beckmann coulter flow cytometer
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | TF-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.09 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.30 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.68 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.58 |
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 7.39 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 7.07 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 7.00 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | 6.81 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.45 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.34 |
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL495727 | AT-9283 | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL603469 | LESTAURTINIB | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4303389 | NS-018 | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1078178 | MOMELOTINIB | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4116008 | CERDULATINIB | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2107823 | GANDOTINIB | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2035187 | PACRITINIB | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL3622820 | ITACITINIB | IC50 | = | 488.0 | nM | 6.31 |