Assay Detail
Binding
CHEMBL5507217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hrs by TR-FRET assay
23
Total Activities
23
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
Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.14 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5542400 | — | — | 1 | 8.66 |
| CHEMBL5563563 | — | — | 1 | 8.62 |
| CHEMBL5562462 | — | — | 1 | 8.28 |
| CHEMBL5532094 | — | — | 1 | 8.07 |
| CHEMBL5566342 | — | — | 1 | 8.06 |
| CHEMBL5560549 | — | — | 1 | 8.00 |
| CHEMBL5556990 | — | — | 1 | 7.94 |
| CHEMBL5558857 | — | — | 1 | 7.72 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.43 |
| CHEMBL5568368 | — | — | 1 | 7.41 |
| CHEMBL5563202 | — | — | 1 | 7.38 |
| CHEMBL3137308 | PEFICITINIB | 4.0 | 1 | 7.31 |
| CHEMBL5542947 | — | — | 1 | 7.10 |
| CHEMBL5556716 | — | — | 1 | 7.09 |
| CHEMBL5559823 | — | — | 1 | 6.81 |
| CHEMBL5561548 | — | — | 1 | 6.49 |
| CHEMBL5559604 | — | — | 1 | 6.24 |
| CHEMBL5532584 | — | — | 1 | 6.19 |
| CHEMBL5564520 | — | — | 1 | 5.97 |
| CHEMBL5561136 | — | — | 1 | 5.62 |
| CHEMBL5564970 | — | — | 1 | 5.59 |
| CHEMBL5561392 | — | — | 1 | 5.20 |
| CHEMBL5557208 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5542400 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5563563 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5562462 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5532094 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5566342 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5560549 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5556990 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5558857 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL5568368 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5563202 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL3137308 | PEFICITINIB | IC50 | = | 49.1 | nM | 7.31 |
| CHEMBL5542947 | — | IC50 | = | 78.9 | nM | 7.10 |
| CHEMBL5556716 | — | IC50 | = | 81.7 | nM | 7.09 |
| CHEMBL5559823 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5561548 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL5559604 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL5532584 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL5564520 | — | IC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL5561136 | — | IC50 | = | 2393.0 | nM | 5.62 |
| CHEMBL5564970 | — | IC50 | = | 2561.0 | nM | 5.59 |
| CHEMBL5561392 | — | IC50 | = | 6295.0 | nM | 5.20 |
| CHEMBL5557208 | — | IC50 | > | 10000.0 | nM | - |