Assay Detail
Binding
CHEMBL5053804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wildtype human TRKA using poly (Glu,Tyr) 4:1 as substrate in presence of [gamma-33P]ATP by hotspot kinase assay
6
Total Activities
6
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 and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.64 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 10.15 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 9.96 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.53 |
| CHEMBL4856292 | — | — | 1 | 8.41 |
| CHEMBL5089809 | — | — | 1 | 7.67 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 2.97 | nM | 8.53 |
| CHEMBL4856292 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5089809 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 72.3 | nM | 7.14 |