Assay Detail
Binding
CHEMBL5123466
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKA G623R mutant (unknown origin) using TK-sub biotin peptide substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins by FRET assay
13
Total Activities
13
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
Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.37 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196625 | — | — | 1 | 9.10 |
| CHEMBL5203484 | — | — | 1 | 9.10 |
| CHEMBL5195177 | — | — | 1 | 9.10 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.85 |
| CHEMBL5170146 | — | — | 1 | 8.72 |
| CHEMBL5200318 | — | — | 1 | 8.66 |
| CHEMBL5203998 | — | — | 1 | 8.40 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.26 |
| CHEMBL5195033 | — | — | 1 | 8.17 |
| CHEMBL5171308 | — | — | 1 | 7.85 |
| CHEMBL5181767 | — | — | 1 | 7.69 |
| CHEMBL5187607 | — | — | 1 | 7.46 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196625 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5203484 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5195177 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5170146 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5200318 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5203998 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5195033 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5171308 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5181767 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL5187607 | — | IC50 | = | 34.7 | nM | 7.46 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 38.6 | nM | 7.41 |