Assay Detail
Functional
CHEMBL5250522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method
28
Total Activities
28
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
1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.54 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | 4.0 | 1 | 8.46 |
| CHEMBL5284144 | — | — | 1 | 8.15 |
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 7.76 |
| CHEMBL5291008 | — | — | 1 | 7.61 |
| CHEMBL5268831 | — | — | 1 | 7.53 |
| CHEMBL5269214 | — | — | 1 | 7.27 |
| CHEMBL5284208 | — | — | 1 | 7.22 |
| CHEMBL5279026 | — | — | 1 | 7.21 |
| CHEMBL5273620 | — | — | 1 | 7.21 |
| CHEMBL5270601 | — | — | 1 | 7.15 |
| CHEMBL5287259 | — | — | 1 | 6.85 |
| CHEMBL5280596 | — | — | 1 | 6.79 |
| CHEMBL5279334 | — | — | 1 | 6.77 |
| CHEMBL5275850 | — | — | 1 | 6.63 |
| CHEMBL5284668 | — | — | 1 | 6.13 |
| CHEMBL5272928 | — | — | 1 | 6.05 |
| CHEMBL5286410 | — | — | 1 | 6.04 |
| CHEMBL5274689 | — | — | 1 | 5.99 |
| CHEMBL5287431 | — | — | 1 | 5.95 |
| CHEMBL5285965 | — | — | 1 | 5.87 |
| CHEMBL5289571 | — | — | 1 | 5.79 |
| CHEMBL5288736 | — | — | 1 | 5.76 |
| CHEMBL5278045 | — | — | 1 | 5.73 |
| CHEMBL5275312 | — | — | 1 | 5.68 |
| CHEMBL5278993 | — | — | 1 | 5.52 |
| CHEMBL5290506 | — | — | 1 | 5.49 |
| CHEMBL5284865 | — | — | 1 | 5.42 |
| CHEMBL5282607 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5284144 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL5291008 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL5268831 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL5269214 | — | IC50 | = | 53.4 | nM | 7.27 |
| CHEMBL5284208 | — | IC50 | = | 60.8 | nM | 7.22 |
| CHEMBL5279026 | — | IC50 | = | 62.2 | nM | 7.21 |
| CHEMBL5273620 | — | IC50 | = | 61.5 | nM | 7.21 |
| CHEMBL5270601 | — | IC50 | = | 70.3 | nM | 7.15 |
| CHEMBL5287259 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5280596 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5279334 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5275850 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL5284668 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL5272928 | — | IC50 | = | 888.0 | nM | 6.05 |
| CHEMBL5286410 | — | IC50 | = | 903.0 | nM | 6.04 |
| CHEMBL5274689 | — | IC50 | = | 1026.0 | nM | 5.99 |
| CHEMBL5287431 | — | IC50 | = | 1116.0 | nM | 5.95 |
| CHEMBL5285965 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5289571 | — | IC50 | = | 1624.0 | nM | 5.79 |
| CHEMBL5288736 | — | IC50 | = | 1719.0 | nM | 5.76 |
| CHEMBL5278045 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5275312 | — | IC50 | = | 2084.0 | nM | 5.68 |
| CHEMBL5278993 | — | IC50 | = | 3019.0 | nM | 5.52 |
| CHEMBL5290506 | — | IC50 | = | 3268.0 | nM | 5.49 |
| CHEMBL5284865 | — | IC50 | = | 3782.0 | nM | 5.42 |
| CHEMBL5282607 | — | IC50 | = | 6912.0 | nM | 5.16 |