Assay Detail
Binding
CHEMBL3428795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RET (unknown origin)
7
Total Activities
7
Compounds Tested
2
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
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.47 | 8.30 |
| Ki | 1 | 8.82 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 8.82 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.30 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.22 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.59 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 7.05 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.00 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289601 | LENVATINIB | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL572881 | MOTESANIB | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL535 | SUNITINIB | IC50 | = | 220.0 | nM | 6.66 |