Assay Detail
Binding
CHEMBL4709992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-HIS6 fused CCDC6-RET fusion protein (Met1 to Ser503 residues) expressed in Sf9 insect cells using TRK-C-derived peptide as substrate in presence of [33P]-ATP by filter binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET (CHEMBL3430904) ↗| Type | CHIMERIC PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.46 | 8.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.65 |
| CHEMBL4790634 | — | — | 1 | 8.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 2.22 | nM | 8.65 |
| CHEMBL4790634 | — | IC50 | = | 5.43 | nM | 8.27 |