Assay Detail
Binding
CHEMBL5223478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type TRAK (unknown origin) incubated for 30 mins by caliper mobility shift assay
18
Total Activities
18
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
Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.67 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | 9.00 |
| CHEMBL5266269 | — | — | 1 | 8.96 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 8.92 |
| CHEMBL5282675 | — | — | 1 | 8.89 |
| CHEMBL5275171 | — | — | 1 | 8.82 |
| CHEMBL5288589 | — | — | 1 | 8.80 |
| CHEMBL5287060 | — | — | 1 | 8.68 |
| CHEMBL5287063 | — | — | 1 | 8.55 |
| CHEMBL5287847 | — | — | 1 | 8.52 |
| CHEMBL5291020 | — | — | 1 | 8.52 |
| CHEMBL5275881 | — | — | 1 | 8.49 |
| CHEMBL5271403 | — | — | 1 | 8.44 |
| CHEMBL5291305 | — | — | 1 | 8.08 |
| CHEMBL5271251 | — | — | 1 | - |
| CHEMBL5288203 | — | — | 1 | - |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | - |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | - |
| CHEMBL5282907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1983268 | ENTRECTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5266269 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5282675 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5275171 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5288589 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5287060 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5287063 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5287847 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5291020 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5275881 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5271403 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5291305 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5271251 | — | IC50 | - | — | - | |
| CHEMBL5288203 | — | IC50 | - | — | - | |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL4297627 | SELITRECTINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL5282907 | — | IC50 | - | — | - |