Assay Detail
Functional
CHEMBL5367756
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R 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 | 7.17 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.99 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 7.97 |
| CHEMBL5423601 | — | — | 1 | 7.57 |
| CHEMBL5410884 | — | — | 1 | 7.37 |
| CHEMBL5416521 | — | — | 1 | 7.32 |
| CHEMBL5422091 | — | — | 1 | 7.28 |
| CHEMBL5421829 | — | — | 1 | 7.28 |
| CHEMBL5432219 | — | — | 1 | 7.18 |
| CHEMBL5415833 | — | — | 1 | 7.17 |
| CHEMBL5422195 | — | — | 1 | 7.04 |
| CHEMBL5195469 | — | — | 1 | 6.95 |
| CHEMBL5394378 | — | — | 1 | 6.76 |
| CHEMBL5439833 | — | — | 1 | 5.39 |
| CHEMBL5429379 | — | — | 1 | - |
| CHEMBL5410147 | — | — | 1 | - |
| CHEMBL5404881 | — | — | 1 | - |
| CHEMBL5420615 | — | — | 1 | - |
| CHEMBL5396972 | — | — | 1 | - |
| CHEMBL5405759 | — | — | 1 | - |
| CHEMBL5438621 | — | — | 1 | - |
| CHEMBL5433110 | — | — | 1 | - |
| CHEMBL5408929 | — | — | 1 | - |
| CHEMBL5394049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 10.28 | nM | 7.99 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 10.67 | nM | 7.97 |
| CHEMBL5423601 | — | IC50 | = | 27.2 | nM | 7.57 |
| CHEMBL5410884 | — | IC50 | = | 42.3 | nM | 7.37 |
| CHEMBL5416521 | — | IC50 | = | 48.45 | nM | 7.32 |
| CHEMBL5422091 | — | IC50 | = | 51.96 | nM | 7.28 |
| CHEMBL5421829 | — | IC50 | = | 52.56 | nM | 7.28 |
| CHEMBL5432219 | — | IC50 | = | 65.6 | nM | 7.18 |
| CHEMBL5415833 | — | IC50 | = | 67.69 | nM | 7.17 |
| CHEMBL5422195 | — | IC50 | = | 90.82 | nM | 7.04 |
| CHEMBL5195469 | — | IC50 | = | 113.6 | nM | 6.95 |
| CHEMBL5394378 | — | IC50 | = | 171.9 | nM | 6.76 |
| CHEMBL5439833 | — | IC50 | = | 4082.0 | nM | 5.39 |
| CHEMBL5429379 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5410147 | — | IC50 | - | — | - | |
| CHEMBL5404881 | — | IC50 | - | — | - | |
| CHEMBL5420615 | — | IC50 | - | — | - | |
| CHEMBL5396972 | — | IC50 | - | — | - | |
| CHEMBL5405759 | — | IC50 | - | — | - | |
| CHEMBL5438621 | — | IC50 | - | — | - | |
| CHEMBL5433110 | — | IC50 | - | — | - | |
| CHEMBL5408929 | — | IC50 | - | — | - | |
| CHEMBL5394049 | — | IC50 | - | — | - |