Assay Detail
Binding
CHEMBL4124185
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human JAK3 using GEEEEYFELVKKKK as substrate in presence of 10 uM [gamma33P]ATP by radiometric method
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
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.85 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4128181 | — | — | 1 | 9.89 |
| CHEMBL4128266 | — | — | 1 | 9.68 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.54 |
| CHEMBL4125719 | — | — | 1 | 9.41 |
| CHEMBL4125861 | — | — | 1 | 9.13 |
| CHEMBL1650951 | — | — | 1 | 9.00 |
| CHEMBL4127590 | — | — | 1 | 8.00 |
| CHEMBL4128410 | — | — | 1 | 7.66 |
| CHEMBL4126514 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4128181 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4128266 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL4125719 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4125861 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL1650951 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4127590 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4128410 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4126514 | — | IC50 | = | 48.0 | nM | 7.32 |