Assay Detail
Binding
CHEMBL4124181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human JAK1 using poly[Glu:Tyr] (4:1) 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 | 7.68 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.30 |
| CHEMBL4125719 | — | — | 1 | 8.40 |
| CHEMBL4128266 | — | — | 1 | 7.92 |
| CHEMBL4127590 | — | — | 1 | 7.80 |
| CHEMBL4128410 | — | — | 1 | 7.72 |
| CHEMBL4126514 | — | — | 1 | 7.35 |
| CHEMBL4128181 | — | — | 1 | 7.28 |
| CHEMBL4125861 | — | — | 1 | 6.93 |
| CHEMBL1650951 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4125719 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4128266 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4127590 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4128410 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4126514 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4128181 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4125861 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1650951 | — | IC50 | = | 344.0 | nM | 6.46 |