Assay Detail
Functional
CHEMBL5141282
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Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| Confidence | 1 — Organism |
| 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 | 11 | 7.36 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174210 | — | — | 1 | 7.82 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 7.71 |
| CHEMBL5193702 | — | — | 1 | 7.70 |
| CHEMBL5176661 | — | — | 1 | 7.52 |
| CHEMBL5192736 | — | — | 1 | 7.47 |
| CHEMBL5191734 | — | — | 1 | 7.45 |
| CHEMBL5201705 | — | — | 1 | 7.39 |
| CHEMBL5186937 | — | — | 1 | 7.36 |
| CHEMBL5180117 | — | — | 1 | 7.30 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.91 |
| CHEMBL5185440 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174210 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL5193702 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL5176661 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5192736 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL5191734 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL5201705 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL5186937 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5180117 | — | IC50 | = | 50.3 | nM | 7.30 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 122.4 | nM | 6.91 |
| CHEMBL5185440 | — | IC50 | = | 527.4 | nM | 6.28 |