Assay Detail
Binding
CHEMBL5503705
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Binding affinity to recombinant human JAK2 kinase domain (840 to 1132 residues) assessed as dissociation constant by ITC analysis
6
Total Activities
6
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 | 6 | 8.19 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 8.40 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 8.35 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.31 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 8.05 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 8.05 |
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 7.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4303389 | NS-018 | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL4116008 | CERDULATINIB | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL3622820 | ITACITINIB | Kd | = | 10.7 | nM | 7.97 |