Assay Detail
Binding
CHEMBL2378508
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T-cell |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.18 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.51 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.77 |
| CHEMBL2376143 | — | — | 1 | 6.64 |
| CHEMBL2325895 | — | — | 1 | 6.54 |
| CHEMBL2376040 | — | — | 1 | 6.31 |
| CHEMBL2376147 | — | — | 1 | 5.87 |
| CHEMBL2376149 | — | — | 1 | 5.58 |
| CHEMBL2376157 | — | — | 1 | 5.54 |
| CHEMBL2376158 | — | — | 1 | 4.89 |
| CHEMBL2376152 | — | — | 1 | - |
| CHEMBL2376144 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2376143 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2325895 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2376040 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2376147 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL2376149 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL2376157 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL2376158 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL2376152 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2376144 | — | IC50 | > | 30000.0 | nM | - |