Assay Detail
ADMET
CHEMBL4416474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 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 | ADMET |
| 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 | 8.02 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4536396 | — | — | 1 | 9.52 |
| CHEMBL4469844 | — | — | 1 | 9.22 |
| CHEMBL4450301 | — | — | 1 | 9.15 |
| CHEMBL4471599 | — | — | 1 | 9.10 |
| CHEMBL3393066 | VS-5584 | 1.0 | 1 | 8.92 |
| CHEMBL4448906 | — | — | 1 | 8.92 |
| CHEMBL4482927 | — | — | 1 | 8.89 |
| CHEMBL4463007 | — | — | 1 | 8.82 |
| CHEMBL4550310 | — | — | 1 | 8.77 |
| CHEMBL4536419 | — | — | 1 | 8.72 |
| CHEMBL4460058 | — | — | 1 | 8.70 |
| CHEMBL4526498 | — | — | 1 | 8.64 |
| CHEMBL4443416 | — | — | 1 | 8.62 |
| CHEMBL4558494 | — | — | 1 | 8.49 |
| CHEMBL4526485 | — | — | 1 | 8.44 |
| CHEMBL4556988 | — | — | 1 | 8.37 |
| CHEMBL4517586 | — | — | 1 | 8.32 |
| CHEMBL4574559 | — | — | 1 | 8.32 |
| CHEMBL4458055 | — | — | 1 | 8.28 |
| CHEMBL4467200 | — | — | 1 | 8.27 |
| CHEMBL4587709 | — | — | 1 | 8.13 |
| CHEMBL4549136 | — | — | 1 | 7.89 |
| CHEMBL4520559 | — | — | 1 | 7.62 |
| CHEMBL4571980 | — | — | 1 | 7.17 |
| CHEMBL4476445 | — | — | 1 | 7.13 |
| CHEMBL4441275 | — | — | 1 | 7.12 |
| CHEMBL4467503 | — | — | 1 | 7.11 |
| CHEMBL4446722 | — | — | 1 | 7.09 |
| CHEMBL4463215 | — | — | 1 | 7.08 |
| CHEMBL4568482 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4536396 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4469844 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4450301 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4471599 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3393066 | VS-5584 | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4448906 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4482927 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4463007 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4550310 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4536419 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4460058 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4526498 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4443416 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4558494 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4526485 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4556988 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4574559 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4517586 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4458055 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4467200 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4587709 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4549136 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4520559 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4571980 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4476445 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4441275 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4467503 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4446722 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4463215 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4568482 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4476802 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4438810 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4440240 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4536380 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4441500 | — | IC50 | = | 800.0 | nM | 6.10 |