Assay Detail
Binding
CHEMBL5141274
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Inhibition of GST-tagged recombinant human JAK1 (866 to 1154 residues) expressed in baculovirus infection system by FRET assay
15
Total Activities
15
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
Discovery of Hexahydrofuro[3,2-<i>b</i>]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.30 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.66 |
| CHEMBL5205480 | — | — | 1 | 6.72 |
| CHEMBL5190599 | — | — | 1 | 6.57 |
| CHEMBL5184019 | — | — | 1 | 6.32 |
| CHEMBL5189603 | — | — | 1 | 6.25 |
| CHEMBL5182374 | — | — | 1 | 6.17 |
| CHEMBL5184187 | — | — | 1 | 6.10 |
| CHEMBL5207354 | — | — | 1 | 6.05 |
| CHEMBL5185016 | — | — | 1 | 5.98 |
| CHEMBL5182065 | — | — | 1 | 5.95 |
| CHEMBL5185440 | — | — | 1 | 5.82 |
| CHEMBL5191734 | — | — | 1 | 5.81 |
| CHEMBL5174210 | — | — | 1 | 5.54 |
| CHEMBL5203904 | — | — | 1 | - |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5205480 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5190599 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5184019 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL5189603 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL5182374 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL5184187 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5207354 | — | IC50 | = | 895.0 | nM | 6.05 |
| CHEMBL5185016 | — | IC50 | = | 1042.0 | nM | 5.98 |
| CHEMBL5182065 | — | IC50 | = | 1115.0 | nM | 5.95 |
| CHEMBL5185440 | — | IC50 | = | 1517.0 | nM | 5.82 |
| CHEMBL5191734 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL5174210 | — | IC50 | = | 2874.0 | nM | 5.54 |
| CHEMBL5203904 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4085457 | RITLECITINIB | IC50 | > | 10000.0 | nM | - |