Assay Detail
Binding
CHEMBL5367749
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal hexa his tagged TRKA (485 to 795 residues) (unknown origin) expressed in baculovirus expression system Sf9 cells using Ser/Thr 06 as peptide substrate incubated for 1 hr in presence of ATP by FRET based Z-LYTE assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.68 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.72 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.52 |
| CHEMBL5423601 | — | — | 1 | 8.28 |
| CHEMBL5410884 | — | — | 1 | 8.11 |
| CHEMBL5416521 | — | — | 1 | 7.99 |
| CHEMBL5195469 | — | — | 1 | 7.86 |
| CHEMBL5420615 | — | — | 1 | 7.82 |
| CHEMBL5421829 | — | — | 1 | 7.80 |
| CHEMBL5394378 | — | — | 1 | 7.76 |
| CHEMBL5405759 | — | — | 1 | 7.74 |
| CHEMBL5432219 | — | — | 1 | 7.72 |
| CHEMBL5422195 | — | — | 1 | 7.68 |
| CHEMBL5439833 | — | — | 1 | 7.68 |
| CHEMBL5429379 | — | — | 1 | 7.61 |
| CHEMBL5415833 | — | — | 1 | 7.58 |
| CHEMBL5422091 | — | — | 1 | 7.48 |
| CHEMBL5394049 | — | — | 1 | 7.47 |
| CHEMBL5396972 | — | — | 1 | 7.40 |
| CHEMBL5408929 | — | — | 1 | 7.29 |
| CHEMBL5433110 | — | — | 1 | 7.24 |
| CHEMBL5438621 | — | — | 1 | 7.20 |
| CHEMBL5404881 | — | — | 1 | 6.99 |
| CHEMBL5410147 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.92 | nM | 8.72 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 3.03 | nM | 8.52 |
| CHEMBL5423601 | — | IC50 | = | 5.21 | nM | 8.28 |
| CHEMBL5410884 | — | IC50 | = | 7.85 | nM | 8.11 |
| CHEMBL5416521 | — | IC50 | = | 10.15 | nM | 7.99 |
| CHEMBL5195469 | — | IC50 | = | 13.73 | nM | 7.86 |
| CHEMBL5420615 | — | IC50 | = | 15.12 | nM | 7.82 |
| CHEMBL5421829 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL5394378 | — | IC50 | = | 17.41 | nM | 7.76 |
| CHEMBL5405759 | — | IC50 | = | 18.42 | nM | 7.74 |
| CHEMBL5432219 | — | IC50 | = | 18.98 | nM | 7.72 |
| CHEMBL5422195 | — | IC50 | = | 21.06 | nM | 7.68 |
| CHEMBL5439833 | — | IC50 | = | 21.03 | nM | 7.68 |
| CHEMBL5429379 | — | IC50 | = | 24.81 | nM | 7.61 |
| CHEMBL5415833 | — | IC50 | = | 26.06 | nM | 7.58 |
| CHEMBL5422091 | — | IC50 | = | 33.36 | nM | 7.48 |
| CHEMBL5394049 | — | IC50 | = | 34.07 | nM | 7.47 |
| CHEMBL5396972 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5408929 | — | IC50 | = | 51.55 | nM | 7.29 |
| CHEMBL5433110 | — | IC50 | = | 58.15 | nM | 7.24 |
| CHEMBL5438621 | — | IC50 | = | 63.42 | nM | 7.20 |
| CHEMBL5404881 | — | IC50 | = | 103.4 | nM | 6.99 |
| CHEMBL5410147 | — | IC50 | = | 163.7 | nM | 6.79 |