Assay Detail
Binding
CHEMBL5123465
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Inhibition of TRKA F589L 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.31 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 9.70 |
| CHEMBL5196625 | — | — | 1 | 9.22 |
| CHEMBL5203484 | — | — | 1 | 9.10 |
| CHEMBL5195177 | — | — | 1 | 9.10 |
| CHEMBL5170146 | — | — | 1 | 8.48 |
| CHEMBL5200318 | — | — | 1 | 8.39 |
| CHEMBL5203998 | — | — | 1 | 8.37 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.24 |
| CHEMBL5195033 | — | — | 1 | 7.90 |
| CHEMBL5171308 | — | — | 1 | 7.46 |
| CHEMBL5181767 | — | — | 1 | 7.41 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 7.37 |
| CHEMBL5187607 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5196625 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5203484 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5195177 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5170146 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5200318 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5203998 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5195033 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL5171308 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL5181767 | — | IC50 | = | 38.8 | nM | 7.41 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 43.1 | nM | 7.37 |
| CHEMBL5187607 | — | IC50 | = | 57.3 | nM | 7.24 |