Assay Detail
Functional
CHEMBL5367753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 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 | 7.42 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.87 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.86 |
| CHEMBL5423601 | — | — | 1 | 8.62 |
| CHEMBL5416521 | — | — | 1 | 8.17 |
| CHEMBL5422091 | — | — | 1 | 7.72 |
| CHEMBL5410884 | — | — | 1 | 7.69 |
| CHEMBL5420615 | — | — | 1 | 7.49 |
| CHEMBL5422195 | — | — | 1 | 7.47 |
| CHEMBL5195469 | — | — | 1 | 7.47 |
| CHEMBL5394378 | — | — | 1 | 7.47 |
| CHEMBL5432219 | — | — | 1 | 7.46 |
| CHEMBL5421829 | — | — | 1 | 7.44 |
| CHEMBL5405759 | — | — | 1 | 7.42 |
| CHEMBL5415833 | — | — | 1 | 7.29 |
| CHEMBL5438621 | — | — | 1 | 7.22 |
| CHEMBL5396972 | — | — | 1 | 7.03 |
| CHEMBL5439833 | — | — | 1 | 7.00 |
| CHEMBL5410147 | — | — | 1 | 6.99 |
| CHEMBL5433110 | — | — | 1 | 6.87 |
| CHEMBL5394049 | — | — | 1 | 6.84 |
| CHEMBL5429379 | — | — | 1 | 6.57 |
| CHEMBL5404881 | — | — | 1 | 6.42 |
| CHEMBL5408929 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL5423601 | — | IC50 | = | 2.37 | nM | 8.62 |
| CHEMBL5416521 | — | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL5422091 | — | IC50 | = | 18.82 | nM | 7.72 |
| CHEMBL5410884 | — | IC50 | = | 20.48 | nM | 7.69 |
| CHEMBL5420615 | — | IC50 | = | 32.1 | nM | 7.49 |
| CHEMBL5422195 | — | IC50 | = | 33.72 | nM | 7.47 |
| CHEMBL5195469 | — | IC50 | = | 33.59 | nM | 7.47 |
| CHEMBL5394378 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL5432219 | — | IC50 | = | 34.45 | nM | 7.46 |
| CHEMBL5421829 | — | IC50 | = | 36.32 | nM | 7.44 |
| CHEMBL5405759 | — | IC50 | = | 38.26 | nM | 7.42 |
| CHEMBL5415833 | — | IC50 | = | 51.11 | nM | 7.29 |
| CHEMBL5438621 | — | IC50 | = | 59.74 | nM | 7.22 |
| CHEMBL5396972 | — | IC50 | = | 93.46 | nM | 7.03 |
| CHEMBL5439833 | — | IC50 | = | 101.1 | nM | 7.00 |
| CHEMBL5410147 | — | IC50 | = | 103.3 | nM | 6.99 |
| CHEMBL5433110 | — | IC50 | = | 133.8 | nM | 6.87 |
| CHEMBL5394049 | — | IC50 | = | 144.4 | nM | 6.84 |
| CHEMBL5429379 | — | IC50 | = | 270.8 | nM | 6.57 |
| CHEMBL5404881 | — | IC50 | = | 379.1 | nM | 6.42 |
| CHEMBL5408929 | — | IC50 | = | 416.1 | nM | 6.38 |