Assay Detail
Binding
CHEMBL5053797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged TRKA (G443 to G796 residues) (unknown origin) expressed in Sf9 insect cells using poly (Glu, Tyr) 4:1 as substrate incubated for 180 mins in presence of ATP by ATP-Kinase-Glo assay
12
Total Activities
12
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
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 | 12 | 6.43 | 7.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089809 | — | — | 1 | 7.67 |
| CHEMBL5079032 | — | — | 1 | 7.64 |
| CHEMBL5082243 | — | — | 1 | 7.57 |
| CHEMBL4864729 | — | — | 1 | 7.43 |
| CHEMBL5089615 | — | — | 1 | 7.04 |
| CHEMBL5076428 | — | — | 1 | 6.21 |
| CHEMBL5090252 | — | — | 1 | 5.67 |
| CHEMBL5092254 | — | — | 1 | 5.58 |
| CHEMBL5075005 | — | — | 1 | 5.45 |
| CHEMBL5081247 | — | — | 1 | 5.35 |
| CHEMBL5077640 | — | — | 1 | 5.13 |
| CHEMBL5085280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5089809 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL5079032 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5082243 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL4864729 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL5089615 | — | IC50 | = | 91.4 | nM | 7.04 |
| CHEMBL5076428 | — | IC50 | = | 611.0 | nM | 6.21 |
| CHEMBL5090252 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5092254 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL5075005 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL5081247 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5077640 | — | IC50 | = | 7410.0 | nM | 5.13 |
| CHEMBL5085280 | — | IC50 | > | 9000.0 | nM | - |