Assay Detail
Binding
CHEMBL5362824
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human recombinant TRKA G595R mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay
40
Total Activities
40
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 | 40 | 6.13 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.10 |
| CHEMBL5431992 | — | — | 1 | 8.00 |
| CHEMBL5402022 | — | — | 1 | 7.85 |
| CHEMBL5412694 | — | — | 1 | 7.44 |
| CHEMBL5411653 | — | — | 1 | 6.80 |
| CHEMBL5405520 | — | — | 1 | 6.52 |
| CHEMBL5403006 | — | — | 1 | 6.51 |
| CHEMBL2037226 | — | — | 1 | 6.50 |
| CHEMBL5412950 | — | — | 1 | 6.47 |
| CHEMBL5429071 | — | — | 1 | 6.44 |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | 6.40 |
| CHEMBL5426432 | — | — | 1 | 6.27 |
| CHEMBL5435508 | — | — | 1 | 6.27 |
| CHEMBL5421895 | — | — | 1 | 6.22 |
| CHEMBL5416004 | — | — | 1 | 6.20 |
| CHEMBL5436311 | — | — | 1 | 6.19 |
| CHEMBL5424554 | — | — | 1 | 6.11 |
| CHEMBL5412491 | — | — | 1 | 6.09 |
| CHEMBL5402630 | — | — | 1 | 6.09 |
| CHEMBL5393854 | — | — | 1 | 6.07 |
| CHEMBL5409228 | — | — | 1 | 5.97 |
| CHEMBL5393979 | — | — | 1 | 5.87 |
| CHEMBL5434909 | — | — | 1 | 5.79 |
| CHEMBL5422996 | — | — | 1 | 5.73 |
| CHEMBL5418831 | — | — | 1 | 5.72 |
| CHEMBL5415584 | — | — | 1 | 5.69 |
| CHEMBL5429205 | — | — | 1 | 5.68 |
| CHEMBL5430182 | — | — | 1 | 5.64 |
| CHEMBL5406744 | — | — | 1 | 5.61 |
| CHEMBL5406403 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5431992 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5402022 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5412694 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5411653 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5405520 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5403006 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2037226 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5412950 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5429071 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1983268 | ENTRECTINIB | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5426432 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5435508 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5421895 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5416004 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5436311 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5424554 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5412491 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5402630 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5393854 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL5409228 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL5393979 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5434909 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL5422996 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL5418831 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL5415584 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL5429205 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5430182 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL5406744 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL5406403 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL5406562 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL5399429 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL5412443 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL5423414 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5426605 | — | IC50 | = | 4620.0 | nM | 5.33 |
| CHEMBL5439400 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL5432702 | — | IC50 | = | 13320.0 | nM | 4.88 |
| CHEMBL5421856 | — | IC50 | - | — | - | |
| CHEMBL5404415 | — | IC50 | - | — | - | |
| CHEMBL5401510 | — | IC50 | - | — | - |