Assay Detail
Binding
CHEMBL5110450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type TRKA (unknown origin) using TK-sub-biotin peptide as substrate incubated for 30 mins followed by treated with ATP and substrate for 40 mins by FRET-based-Z'-lyte kinase assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.49 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175608 | — | — | 1 | 9.70 |
| CHEMBL5170464 | — | — | 1 | 9.70 |
| CHEMBL5170096 | — | — | 1 | 9.70 |
| CHEMBL5188045 | — | — | 1 | 9.70 |
| CHEMBL5173256 | — | — | 1 | 9.70 |
| CHEMBL5198983 | — | — | 1 | 9.70 |
| CHEMBL5169970 | — | — | 1 | 9.52 |
| CHEMBL5196651 | — | — | 1 | 9.52 |
| CHEMBL5193919 | — | — | 1 | 9.52 |
| CHEMBL5195375 | — | — | 1 | 9.52 |
| CHEMBL5170412 | — | — | 1 | 9.40 |
| CHEMBL5189971 | — | — | 1 | 9.40 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 9.40 |
| CHEMBL5205989 | — | — | 1 | 9.30 |
| CHEMBL5184432 | — | — | 1 | 8.55 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175608 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5170464 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5170096 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5188045 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5173256 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5198983 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5169970 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5196651 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5193919 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5195375 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5170412 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5189971 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5205989 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5184432 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | - | — | - |