Assay Detail
Binding
CHEMBL5162129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length RET kinase expressed in human HEK293 cells and measured by NanoBRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Design and development of photoswitchable DFG-Out RET kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.45 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.89 |
| CHEMBL5191715 | — | — | 1 | 6.04 |
| CHEMBL5193068 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5191715 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5193068 | — | IC50 | = | 3890.0 | nM | 5.41 |