Assay Detail
Binding
CHEMBL5507218
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Inhibition of JAK2 (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 | 7.24 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5557208 | — | — | 1 | 9.00 |
| CHEMBL5562462 | — | — | 1 | 8.66 |
| CHEMBL5564520 | — | — | 1 | 8.18 |
| CHEMBL5532094 | — | — | 1 | 7.78 |
| CHEMBL5556990 | — | — | 1 | 7.65 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.42 |
| CHEMBL3137308 | PEFICITINIB | 4.0 | 1 | 7.25 |
| CHEMBL5558857 | — | — | 1 | 6.91 |
| CHEMBL5556716 | — | — | 1 | 6.86 |
| CHEMBL5542947 | — | — | 1 | 6.79 |
| CHEMBL5532584 | — | — | 1 | 6.28 |
| CHEMBL5542400 | — | — | 1 | 6.25 |
| CHEMBL5566342 | — | — | 1 | 6.21 |
| CHEMBL5563563 | — | — | 1 | 6.07 |
| CHEMBL5560549 | — | — | 1 | - |
| CHEMBL5561392 | — | — | 1 | - |
| CHEMBL5564970 | — | — | 1 | - |
| CHEMBL5563202 | — | — | 1 | - |
| CHEMBL5559604 | — | — | 1 | - |
| CHEMBL5561136 | — | — | 1 | - |
| CHEMBL5561548 | — | — | 1 | - |
| CHEMBL5568368 | — | — | 1 | - |
| CHEMBL5559823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5557208 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5562462 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5564520 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5532094 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL5556990 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 38.3 | nM | 7.42 |
| CHEMBL3137308 | PEFICITINIB | IC50 | = | 56.4 | nM | 7.25 |
| CHEMBL5558857 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL5556716 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5542947 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL5532584 | — | IC50 | = | 529.0 | nM | 6.28 |
| CHEMBL5542400 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL5566342 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL5563563 | — | IC50 | = | 845.0 | nM | 6.07 |
| CHEMBL5560549 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5561392 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5564970 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5563202 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5559604 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5561136 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5561548 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5568368 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5559823 | — | IC50 | > | 10000.0 | nM | - |