Assay Detail
Binding
CHEMBL4416475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged JAK1 (866 to 1154 residues) expressed in baculovirus expression system using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay
35
Total Activities
35
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
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.13 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4469844 | — | — | 1 | 8.46 |
| CHEMBL4536396 | — | — | 1 | 8.26 |
| CHEMBL4463007 | — | — | 1 | 8.26 |
| CHEMBL4526498 | — | — | 1 | 8.06 |
| CHEMBL4550310 | — | — | 1 | 8.03 |
| CHEMBL4460058 | — | — | 1 | 7.92 |
| CHEMBL4471599 | — | — | 1 | 7.75 |
| CHEMBL4443416 | — | — | 1 | 7.70 |
| CHEMBL4448906 | — | — | 1 | 7.62 |
| CHEMBL4526485 | — | — | 1 | 7.60 |
| CHEMBL4558494 | — | — | 1 | 7.55 |
| CHEMBL4517586 | — | — | 1 | 7.51 |
| CHEMBL4587709 | — | — | 1 | 7.41 |
| CHEMBL4458055 | — | — | 1 | 7.39 |
| CHEMBL4556988 | — | — | 1 | 7.31 |
| CHEMBL4482927 | — | — | 1 | 7.27 |
| CHEMBL4450301 | — | — | 1 | 7.27 |
| CHEMBL3393066 | VS-5584 | 1.0 | 1 | 7.24 |
| CHEMBL4574559 | — | — | 1 | 7.13 |
| CHEMBL4549136 | — | — | 1 | 7.10 |
| CHEMBL4467200 | — | — | 1 | 6.82 |
| CHEMBL4536419 | — | — | 1 | 6.75 |
| CHEMBL4476445 | — | — | 1 | 6.43 |
| CHEMBL4463215 | — | — | 1 | 6.32 |
| CHEMBL4520559 | — | — | 1 | 6.12 |
| CHEMBL4467503 | — | — | 1 | 6.07 |
| CHEMBL4446722 | — | — | 1 | 5.92 |
| CHEMBL4568482 | — | — | 1 | 5.77 |
| CHEMBL4441275 | — | — | 1 | 5.68 |
| CHEMBL4536380 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4469844 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4536396 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4463007 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4526498 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4550310 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4460058 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4471599 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4443416 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4448906 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4526485 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4558494 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4517586 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4587709 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4458055 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4556988 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4482927 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4450301 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3393066 | VS-5584 | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4574559 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4549136 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4467200 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4536419 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4476445 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4463215 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4520559 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4467503 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4446722 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4568482 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4441275 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4536380 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4440240 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4441500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4438810 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4476802 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4571980 | — | IC50 | > | 10000.0 | nM | - |