Assay Detail
Binding
CHEMBL5152020
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant RET M918T (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform method
5
Total Activities
5
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
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.64 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171764 | — | — | 1 | 9.40 |
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 9.15 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 8.40 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.15 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171764 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2029988 | CEP-32496 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 8.0 | nM | 8.10 |