Assay Detail
Functional
CHEMBL5367757
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Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method
9
Total Activities
9
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 | 9 | 7.86 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.79 |
| CHEMBL5423601 | — | — | 1 | 8.21 |
| CHEMBL5416521 | — | — | 1 | 8.06 |
| CHEMBL5405759 | — | — | 1 | 7.66 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.50 |
| CHEMBL5410884 | — | — | 1 | 7.49 |
| CHEMBL5432219 | — | — | 1 | 7.34 |
| CHEMBL5396972 | — | — | 1 | - |
| CHEMBL5415833 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL5423601 | — | IC50 | = | 6.13 | nM | 8.21 |
| CHEMBL5416521 | — | IC50 | = | 8.68 | nM | 8.06 |
| CHEMBL5405759 | — | IC50 | = | 22.14 | nM | 7.66 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL5410884 | — | IC50 | = | 32.71 | nM | 7.49 |
| CHEMBL5432219 | — | IC50 | = | 45.35 | nM | 7.34 |
| CHEMBL5396972 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5415833 | — | IC50 | > | 1000.0 | nM | - |