Assay Detail
Binding
CHEMBL3784139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2 (unknown origin)
6
Total Activities
6
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
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.28 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.92 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.85 |
| CHEMBL3780091 | — | — | 1 | 8.40 |
| CHEMBL3781427 | — | — | 1 | 8.30 |
| CHEMBL3780467 | — | — | 1 | 7.40 |
| CHEMBL3782012 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3780091 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3781427 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3780467 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3782012 | — | IC50 | = | 150.0 | nM | 6.82 |