Assay Detail
Binding
CHEMBL5367752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKA G595R mutant (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 | 7.32 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.31 |
| CHEMBL5423601 | — | — | 1 | 8.17 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.12 |
| CHEMBL5410884 | — | — | 1 | 7.97 |
| CHEMBL5432219 | — | — | 1 | 7.51 |
| CHEMBL5416521 | — | — | 1 | 7.41 |
| CHEMBL5421829 | — | — | 1 | 7.26 |
| CHEMBL5422091 | — | — | 1 | 7.20 |
| CHEMBL5439833 | — | — | 1 | 7.07 |
| CHEMBL5422195 | — | — | 1 | 7.04 |
| CHEMBL5415833 | — | — | 1 | 6.96 |
| CHEMBL5394378 | — | — | 1 | 6.91 |
| CHEMBL5195469 | — | — | 1 | 6.31 |
| CHEMBL5408929 | — | — | 1 | 6.25 |
| CHEMBL5404881 | — | — | 1 | - |
| CHEMBL5420615 | — | — | 1 | - |
| CHEMBL5410147 | — | — | 1 | - |
| CHEMBL5396972 | — | — | 1 | - |
| CHEMBL5405759 | — | — | 1 | - |
| CHEMBL5429379 | — | — | 1 | - |
| CHEMBL5438621 | — | — | 1 | - |
| CHEMBL5433110 | — | — | 1 | - |
| CHEMBL5394049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 4.86 | nM | 8.31 |
| CHEMBL5423601 | — | IC50 | = | 6.77 | nM | 8.17 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5410884 | — | IC50 | = | 10.69 | nM | 7.97 |
| CHEMBL5432219 | — | IC50 | = | 30.62 | nM | 7.51 |
| CHEMBL5416521 | — | IC50 | = | 39.02 | nM | 7.41 |
| CHEMBL5421829 | — | IC50 | = | 54.77 | nM | 7.26 |
| CHEMBL5422091 | — | IC50 | = | 63.35 | nM | 7.20 |
| CHEMBL5439833 | — | IC50 | = | 85.15 | nM | 7.07 |
| CHEMBL5422195 | — | IC50 | = | 91.75 | nM | 7.04 |
| CHEMBL5415833 | — | IC50 | = | 108.8 | nM | 6.96 |
| CHEMBL5394378 | — | IC50 | = | 123.5 | nM | 6.91 |
| CHEMBL5195469 | — | IC50 | = | 493.7 | nM | 6.31 |
| CHEMBL5408929 | — | IC50 | = | 561.7 | nM | 6.25 |
| CHEMBL5404881 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5420615 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5410147 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5396972 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5405759 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5429379 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5438621 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5433110 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5394049 | — | IC50 | > | 1000.0 | nM | - |