Assay Detail
Functional
CHEMBL5164775
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Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay
10
Total Activities
10
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 | 10 | 6.35 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.89 |
| CHEMBL5195469 | — | — | 1 | 6.96 |
| CHEMBL5184321 | — | — | 1 | 6.28 |
| CHEMBL5183862 | — | — | 1 | 6.26 |
| CHEMBL5184043 | — | — | 1 | 6.17 |
| CHEMBL5198765 | — | — | 1 | 6.14 |
| CHEMBL5198838 | — | — | 1 | 6.11 |
| CHEMBL5178374 | — | — | 1 | 6.08 |
| CHEMBL5194130 | — | — | 1 | 5.84 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5195469 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5184321 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5183862 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5184043 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5198765 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5198838 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5178374 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL5194130 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 1550.0 | nM | 5.81 |