Assay Detail
Binding
CHEMBL5362826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human recombinant TRKA F589L mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay
6
Total Activities
6
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, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.38 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5431992 | — | — | 1 | 9.00 |
| CHEMBL5412694 | — | — | 1 | 8.70 |
| CHEMBL5402022 | — | — | 1 | 8.40 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.40 |
| CHEMBL2037226 | — | — | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5431992 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5412694 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5402022 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2037226 | — | IC50 | - | — | - | |
| CHEMBL1983268 | ENTRECTINIB | IC50 | - | — | - |