Assay Detail
Functional
CHEMBL5164767
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Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay
3
Total Activities
3
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
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.84 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195469 | — | — | 1 | 8.25 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.24 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 7.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195469 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 96.0 | nM | 7.02 |