Assay Detail
Binding
CHEMBL5385205
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Inhibition of JAK3 (unknown origin)
5
Total Activities
5
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
Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.99 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.70 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.47 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.51 |
| CHEMBL5433552 | — | — | 1 | 6.23 |
| CHEMBL5395502 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 311.5 | nM | 6.51 |
| CHEMBL5433552 | — | IC50 | = | 594.8 | nM | 6.23 |
| CHEMBL5395502 | — | IC50 | = | 954.1 | nM | 6.02 |