Assay Detail
Binding
CHEMBL5139765
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal human TRKC (456 to 825 residues) expressed in baculovirus expression system using TK as substrate measured after 40 mins in presence of ATP by HTRF assay
7
Total Activities
7
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 |
Publication
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.92 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174615 | — | — | 1 | 8.60 |
| CHEMBL4856292 | — | — | 1 | 8.57 |
| CHEMBL5196903 | — | — | 1 | 8.35 |
| CHEMBL5186552 | — | — | 1 | 7.92 |
| CHEMBL5184749 | — | — | 1 | 7.64 |
| CHEMBL5206613 | — | — | 1 | 7.21 |
| CHEMBL5175892 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174615 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4856292 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5196903 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5186552 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5184749 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5206613 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5175892 | — | IC50 | = | 75.0 | nM | 7.12 |