Assay Detail
Binding
CHEMBL5141276
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Inhibition of GST tagged recombinant human JAK3 expressed in baculovirus infection system by FRET assay
22
Total Activities
22
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 | 22 | 8.54 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193702 | — | — | 1 | 8.92 |
| CHEMBL5189603 | — | — | 1 | 8.92 |
| CHEMBL5192736 | — | — | 1 | 8.92 |
| CHEMBL5176661 | — | — | 1 | 8.89 |
| CHEMBL5180117 | — | — | 1 | 8.89 |
| CHEMBL5186937 | — | — | 1 | 8.89 |
| CHEMBL5201705 | — | — | 1 | 8.89 |
| CHEMBL5184187 | — | — | 1 | 8.82 |
| CHEMBL5205480 | — | — | 1 | 8.82 |
| CHEMBL5182065 | — | — | 1 | 8.80 |
| CHEMBL5208026 | — | — | 1 | 8.77 |
| CHEMBL5191734 | — | — | 1 | 8.74 |
| CHEMBL5190599 | — | — | 1 | 8.72 |
| CHEMBL5174210 | — | — | 1 | 8.72 |
| CHEMBL5184019 | — | — | 1 | 8.66 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 8.64 |
| CHEMBL5185016 | — | — | 1 | 8.60 |
| CHEMBL5207354 | — | — | 1 | 8.26 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.17 |
| CHEMBL5185440 | — | — | 1 | 7.75 |
| CHEMBL5182374 | — | — | 1 | 7.50 |
| CHEMBL5203904 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193702 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5189603 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5192736 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5176661 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5180117 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5186937 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5201705 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5184187 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5205480 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5182065 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5208026 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5191734 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5190599 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5174210 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5184019 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5185016 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5207354 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5185440 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5182374 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5203904 | — | IC50 | = | 268.0 | nM | 6.57 |