Assay Detail
Binding
CHEMBL4666925
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Inhibition of recombinant human GST-tagged JAK1 (866 to 1154 residues) expressed in baculovirus expression system using Tyr 06 as substrate incubated for 60 mins by Z'-lyte assay
9
Total Activities
9
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
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.51 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744172 | — | — | 1 | 8.92 |
| CHEMBL4777342 | — | — | 1 | 8.77 |
| CHEMBL4760562 | — | — | 1 | 8.72 |
| CHEMBL4745474 | — | — | 1 | 8.66 |
| CHEMBL2178799 | — | — | 1 | 7.50 |
| CHEMBL4740778 | — | — | 1 | - |
| CHEMBL4742159 | — | — | 1 | - |
| CHEMBL4764019 | — | — | 1 | - |
| CHEMBL4746726 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744172 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4777342 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4760562 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4745474 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2178799 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4740778 | — | IC50 | - | — | - | |
| CHEMBL4742159 | — | IC50 | - | — | - | |
| CHEMBL4764019 | — | IC50 | - | — | - | |
| CHEMBL4746726 | — | IC50 | - | — | - |