Assay Detail
Functional
CHEMBL5250520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-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 | 7.09 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | 4.0 | 1 | 8.36 |
| CHEMBL5284144 | — | — | 1 | 8.29 |
| CHEMBL5291008 | — | — | 1 | 8.25 |
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 8.13 |
| CHEMBL5269214 | — | — | 1 | 8.11 |
| CHEMBL5284208 | — | — | 1 | 8.06 |
| CHEMBL5268831 | — | — | 1 | 7.95 |
| CHEMBL5279026 | — | — | 1 | 7.93 |
| CHEMBL5279334 | — | — | 1 | 7.90 |
| CHEMBL5280596 | — | — | 1 | 7.86 |
| CHEMBL5273620 | — | — | 1 | 7.86 |
| CHEMBL5270601 | — | — | 1 | 7.73 |
| CHEMBL5287259 | — | — | 1 | 7.67 |
| CHEMBL5275850 | — | — | 1 | 7.62 |
| CHEMBL5289571 | — | — | 1 | 6.85 |
| CHEMBL5274689 | — | — | 1 | 6.82 |
| CHEMBL5285965 | — | — | 1 | 6.75 |
| CHEMBL5275312 | — | — | 1 | 6.69 |
| CHEMBL5272928 | — | — | 1 | 6.55 |
| CHEMBL5284668 | — | — | 1 | 6.39 |
| CHEMBL5282607 | — | — | 1 | 5.93 |
| CHEMBL5290506 | — | — | 1 | 5.81 |
| CHEMBL5287431 | — | — | 1 | 5.66 |
| CHEMBL5288736 | — | — | 1 | 5.65 |
| CHEMBL5278993 | — | — | 1 | 5.53 |
| CHEMBL5286410 | — | — | 1 | 5.53 |
| CHEMBL5284865 | — | — | 1 | 5.51 |
| CHEMBL5278045 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5284144 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5291008 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5269214 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5284208 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5268831 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL5279026 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL5279334 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL5280596 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5273620 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL5270601 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL5287259 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL5275850 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5289571 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5274689 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL5285965 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL5275312 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5272928 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL5284668 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5282607 | — | IC50 | = | 1161.0 | nM | 5.93 |
| CHEMBL5290506 | — | IC50 | = | 1562.0 | nM | 5.81 |
| CHEMBL5287431 | — | IC50 | = | 2185.0 | nM | 5.66 |
| CHEMBL5288736 | — | IC50 | = | 2255.0 | nM | 5.65 |
| CHEMBL5278993 | — | IC50 | = | 2981.0 | nM | 5.53 |
| CHEMBL5286410 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL5284865 | — | IC50 | = | 3055.0 | nM | 5.51 |
| CHEMBL5278045 | — | IC50 | > | 10000.0 | nM | - |