Assay Detail
Functional
CHEMBL5141279
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Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein 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 | Mus musculus |
| Cell Type | BaF3 |
| 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 | 6.48 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191734 | — | — | 1 | 6.91 |
| CHEMBL5174210 | — | — | 1 | 6.88 |
| CHEMBL5193702 | — | — | 1 | 6.75 |
| CHEMBL5192736 | — | — | 1 | 6.75 |
| CHEMBL5176661 | — | — | 1 | 6.50 |
| CHEMBL5186937 | — | — | 1 | 6.47 |
| CHEMBL5201705 | — | — | 1 | 6.36 |
| CHEMBL5180117 | — | — | 1 | 6.34 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 5.38 |
| CHEMBL5185440 | — | — | 1 | - |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191734 | — | IC50 | = | 122.1 | nM | 6.91 |
| CHEMBL5174210 | — | IC50 | = | 132.8 | nM | 6.88 |
| CHEMBL5193702 | — | IC50 | = | 177.7 | nM | 6.75 |
| CHEMBL5192736 | — | IC50 | = | 179.7 | nM | 6.75 |
| CHEMBL5176661 | — | IC50 | = | 312.9 | nM | 6.50 |
| CHEMBL5186937 | — | IC50 | = | 335.7 | nM | 6.47 |
| CHEMBL5201705 | — | IC50 | = | 435.1 | nM | 6.36 |
| CHEMBL5180117 | — | IC50 | = | 460.8 | nM | 6.34 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 4154.3 | nM | 5.38 |
| CHEMBL5185440 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4085457 | RITLECITINIB | IC50 | > | 10000.0 | nM | - |