Assay Detail
Functional
CHEMBL5250531
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 V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method
3
Total Activities
3
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 | 3 | 6.30 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5291008 | — | — | 1 | 6.92 |
| CHEMBL4582651 | PRALSETINIB | 4.0 | 1 | 6.62 |
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5291008 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4582651 | PRALSETINIB | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 4340.0 | nM | 5.36 |