Assay Detail
Binding
CHEMBL4723819
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Inhibition of human JAK1 (866 to end residues) using GEEPLYWSFPAKKK as substrate after 40 mins by [gamma-33ATP] radiometric assay
8
Total Activities
8
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
N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.38 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789273 | — | — | 1 | 7.62 |
| CHEMBL4754856 | — | — | 1 | 7.58 |
| CHEMBL4741075 | — | — | 1 | 7.52 |
| CHEMBL4753549 | — | — | 1 | 7.38 |
| CHEMBL4798378 | — | — | 1 | 7.37 |
| CHEMBL4748354 | — | — | 1 | 7.33 |
| CHEMBL4759953 | — | — | 1 | 7.22 |
| CHEMBL4756422 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789273 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4754856 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4741075 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4753549 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4798378 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4748354 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4759953 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4756422 | — | IC50 | = | 91.0 | nM | 7.04 |