Assay Detail
Functional
CHEMBL5367754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method
23
Total Activities
23
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 | 23 | 7.32 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.87 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.72 |
| CHEMBL5422091 | — | — | 1 | 7.95 |
| CHEMBL5422195 | — | — | 1 | 7.79 |
| CHEMBL5394378 | — | — | 1 | 7.77 |
| CHEMBL5423601 | — | — | 1 | 7.75 |
| CHEMBL5195469 | — | — | 1 | 7.63 |
| CHEMBL5415833 | — | — | 1 | 7.53 |
| CHEMBL5405759 | — | — | 1 | 7.50 |
| CHEMBL5438621 | — | — | 1 | 7.49 |
| CHEMBL5394049 | — | — | 1 | 7.48 |
| CHEMBL5421829 | — | — | 1 | 7.47 |
| CHEMBL5416521 | — | — | 1 | 7.32 |
| CHEMBL5396972 | — | — | 1 | 7.27 |
| CHEMBL5410147 | — | — | 1 | 7.15 |
| CHEMBL5410884 | — | — | 1 | 6.98 |
| CHEMBL5439833 | — | — | 1 | 6.97 |
| CHEMBL5433110 | — | — | 1 | 6.86 |
| CHEMBL5432219 | — | — | 1 | 6.79 |
| CHEMBL5429379 | — | — | 1 | 6.69 |
| CHEMBL5404881 | — | — | 1 | 6.49 |
| CHEMBL5408929 | — | — | 1 | 6.27 |
| CHEMBL5420615 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 1.36 | nM | 8.87 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5422091 | — | IC50 | = | 11.19 | nM | 7.95 |
| CHEMBL5422195 | — | IC50 | = | 16.35 | nM | 7.79 |
| CHEMBL5394378 | — | IC50 | = | 17.12 | nM | 7.77 |
| CHEMBL5423601 | — | IC50 | = | 17.67 | nM | 7.75 |
| CHEMBL5195469 | — | IC50 | = | 23.66 | nM | 7.63 |
| CHEMBL5415833 | — | IC50 | = | 29.49 | nM | 7.53 |
| CHEMBL5405759 | — | IC50 | = | 31.58 | nM | 7.50 |
| CHEMBL5438621 | — | IC50 | = | 32.18 | nM | 7.49 |
| CHEMBL5394049 | — | IC50 | = | 32.99 | nM | 7.48 |
| CHEMBL5421829 | — | IC50 | = | 33.71 | nM | 7.47 |
| CHEMBL5416521 | — | IC50 | = | 48.38 | nM | 7.32 |
| CHEMBL5396972 | — | IC50 | = | 53.88 | nM | 7.27 |
| CHEMBL5410147 | — | IC50 | = | 70.22 | nM | 7.15 |
| CHEMBL5410884 | — | IC50 | = | 104.2 | nM | 6.98 |
| CHEMBL5439833 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5433110 | — | IC50 | = | 139.5 | nM | 6.86 |
| CHEMBL5432219 | — | IC50 | = | 160.9 | nM | 6.79 |
| CHEMBL5429379 | — | IC50 | = | 202.3 | nM | 6.69 |
| CHEMBL5404881 | — | IC50 | = | 326.6 | nM | 6.49 |
| CHEMBL5408929 | — | IC50 | = | 540.7 | nM | 6.27 |
| CHEMBL5420615 | — | IC50 | = | 3032.0 | nM | 5.52 |