Assay Detail
Binding
CHEMBL5503690
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Binding affinity to recombinant human JAK2 kinase domain by fluorescence polarization assay
10
Total Activities
10
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
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 10 | 8.31 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.10 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.54 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 8.48 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.37 |
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 8.35 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 8.32 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 8.18 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 8.17 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | 7.96 |
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 0.8 | nM | 9.10 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 2.9 | nM | 8.54 |
| CHEMBL495727 | AT-9283 | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 4.3 | nM | 8.37 |
| CHEMBL4303389 | NS-018 | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL4116008 | CERDULATINIB | Kd | = | 4.8 | nM | 8.32 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 6.6 | nM | 8.18 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 6.7 | nM | 8.17 |
| CHEMBL2107823 | GANDOTINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL3622820 | ITACITINIB | Kd | = | 26.0 | nM | 7.58 |