Assay Detail
Binding
CHEMBL5503693
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Inhibition of recombinant human JAK1 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase 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 |
|---|---|---|---|
| IC50 | 10 | 7.68 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 8.47 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.46 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.24 |
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 8.15 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | 8.14 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 7.66 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.25 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.19 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.84 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622820 | ITACITINIB | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL603469 | LESTAURTINIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4303389 | NS-018 | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2107823 | GANDOTINIB | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4116008 | CERDULATINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL495727 | AT-9283 | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1078178 | MOMELOTINIB | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL2035187 | PACRITINIB | IC50 | = | 371.0 | nM | 6.43 |