Assay Detail
Functional
CHEMBL5367755
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant 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 | 8.17 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416521 | — | — | 1 | 8.90 |
| CHEMBL5423601 | — | — | 1 | 8.85 |
| CHEMBL5405759 | — | — | 1 | 8.66 |
| CHEMBL5420615 | — | — | 1 | 8.65 |
| CHEMBL5422091 | — | — | 1 | 8.64 |
| CHEMBL5421829 | — | — | 1 | 8.54 |
| CHEMBL5415833 | — | — | 1 | 8.42 |
| CHEMBL5410884 | — | — | 1 | 8.41 |
| CHEMBL5394378 | — | — | 1 | 8.26 |
| CHEMBL5432219 | — | — | 1 | 8.22 |
| CHEMBL5195469 | — | — | 1 | 8.22 |
| CHEMBL5422195 | — | — | 1 | 8.18 |
| CHEMBL5438621 | — | — | 1 | 8.09 |
| CHEMBL5433110 | — | — | 1 | 8.07 |
| CHEMBL5396972 | — | — | 1 | 8.07 |
| CHEMBL5394049 | — | — | 1 | 8.05 |
| CHEMBL5410147 | — | — | 1 | 7.99 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 7.80 |
| CHEMBL5408929 | — | — | 1 | 7.76 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.65 |
| CHEMBL5404881 | — | — | 1 | 7.58 |
| CHEMBL5439833 | — | — | 1 | 7.50 |
| CHEMBL5429379 | — | — | 1 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416521 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL5423601 | — | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL5405759 | — | IC50 | = | 2.17 | nM | 8.66 |
| CHEMBL5420615 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL5422091 | — | IC50 | = | 2.28 | nM | 8.64 |
| CHEMBL5421829 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5415833 | — | IC50 | = | 3.78 | nM | 8.42 |
| CHEMBL5410884 | — | IC50 | = | 3.85 | nM | 8.41 |
| CHEMBL5394378 | — | IC50 | = | 5.51 | nM | 8.26 |
| CHEMBL5432219 | — | IC50 | = | 5.96 | nM | 8.22 |
| CHEMBL5195469 | — | IC50 | = | 6.02 | nM | 8.22 |
| CHEMBL5422195 | — | IC50 | = | 6.55 | nM | 8.18 |
| CHEMBL5438621 | — | IC50 | = | 8.21 | nM | 8.09 |
| CHEMBL5433110 | — | IC50 | = | 8.54 | nM | 8.07 |
| CHEMBL5396972 | — | IC50 | = | 8.59 | nM | 8.07 |
| CHEMBL5394049 | — | IC50 | = | 8.86 | nM | 8.05 |
| CHEMBL5410147 | — | IC50 | = | 10.24 | nM | 7.99 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 15.66 | nM | 7.80 |
| CHEMBL5408929 | — | IC50 | = | 17.16 | nM | 7.76 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 22.23 | nM | 7.65 |
| CHEMBL5404881 | — | IC50 | = | 26.49 | nM | 7.58 |
| CHEMBL5439833 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL5429379 | — | IC50 | = | 40.94 | nM | 7.39 |