Assay Detail
Functional
CHEMBL5367803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.00 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423601 | — | — | 1 | 8.30 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 7.91 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423601 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 12.28 | nM | 7.91 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 16.7 | nM | 7.78 |