Assay Detail
Binding
CHEMBL5035648
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wildtype TRKA (unknown origin) preincubated for 30 mins followed by biotinylated TK-peptide substrate addition and measured after 40 mins by FRET-based Z-lyte kinase assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.69 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5075273 | — | — | 1 | 9.40 |
| CHEMBL5078405 | — | — | 1 | 9.30 |
| CHEMBL5088000 | — | — | 1 | 9.15 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 8.92 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.21 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.03 |
| CHEMBL5092943 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5075273 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5078405 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5088000 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5092943 | — | IC50 | = | 14.3 | nM | 7.84 |