Assay Detail
Binding
CHEMBL4614396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.49 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4634992 | — | — | 1 | 8.86 |
| CHEMBL4163691 | POSELTINIB | 2.0 | 1 | 7.84 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.79 |
| CHEMBL4645014 | — | — | 1 | 7.34 |
| CHEMBL4639986 | — | — | 1 | 7.23 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 7.18 |
| CHEMBL4637985 | — | — | 1 | 7.07 |
| CHEMBL4645703 | — | — | 1 | 7.05 |
| CHEMBL4649751 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4634992 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL4163691 | POSELTINIB | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL4645014 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4639986 | — | IC50 | = | 59.39 | nM | 7.23 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL4637985 | — | IC50 | = | 85.3 | nM | 7.07 |
| CHEMBL4645703 | — | IC50 | = | 89.2 | nM | 7.05 |
| CHEMBL4649751 | — | IC50 | = | 90.8 | nM | 7.04 |