Assay Detail
Binding
CHEMBL5250521
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type rearranged during transfection kinase (unknown origin) preincubated for 1 hr followed by addition of development agent incubated for 1 hr measured by FRET-based Z'-Lyte assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.31 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | 4.0 | 1 | 8.62 |
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 8.55 |
| CHEMBL5279334 | — | — | 1 | 7.97 |
| CHEMBL5268831 | — | — | 1 | 7.95 |
| CHEMBL5284144 | — | — | 1 | 7.92 |
| CHEMBL5280596 | — | — | 1 | 7.86 |
| CHEMBL5291008 | — | — | 1 | 7.86 |
| CHEMBL5270601 | — | — | 1 | 7.83 |
| CHEMBL5284208 | — | — | 1 | 7.81 |
| CHEMBL5269214 | — | — | 1 | 7.79 |
| CHEMBL5275850 | — | — | 1 | 7.76 |
| CHEMBL5272928 | — | — | 1 | 7.55 |
| CHEMBL5279026 | — | — | 1 | 7.39 |
| CHEMBL5287259 | — | — | 1 | 7.34 |
| CHEMBL5273620 | — | — | 1 | 7.19 |
| CHEMBL5289571 | — | — | 1 | 6.87 |
| CHEMBL5288736 | — | — | 1 | 6.82 |
| CHEMBL5274689 | — | — | 1 | 6.77 |
| CHEMBL5285965 | — | — | 1 | 6.63 |
| CHEMBL5275312 | — | — | 1 | 6.55 |
| CHEMBL5282607 | — | — | 1 | 5.97 |
| CHEMBL5284668 | — | — | 1 | 5.64 |
| CHEMBL5287431 | — | — | 1 | 5.60 |
| CHEMBL5286410 | — | — | 1 | - |
| CHEMBL5284865 | — | — | 1 | - |
| CHEMBL5278045 | — | — | 1 | - |
| CHEMBL5290506 | — | — | 1 | - |
| CHEMBL5278993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4582651 | PRALSETINIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5279334 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5268831 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL5284144 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5280596 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL5291008 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL5270601 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL5284208 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5269214 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL5275850 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL5272928 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL5279026 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL5287259 | — | IC50 | = | 45.9 | nM | 7.34 |
| CHEMBL5273620 | — | IC50 | = | 64.3 | nM | 7.19 |
| CHEMBL5289571 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5288736 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5274689 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5285965 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL5275312 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL5282607 | — | IC50 | = | 1063.0 | nM | 5.97 |
| CHEMBL5284668 | — | IC50 | = | 2278.0 | nM | 5.64 |
| CHEMBL5287431 | — | IC50 | = | 2512.0 | nM | 5.60 |
| CHEMBL5286410 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5284865 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5278045 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5290506 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5278993 | — | IC50 | > | 10000.0 | nM | - |