Assay Detail
Binding
CHEMBL5139763
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal human TRKA (436 to 790 residues) expressed in baculovirus expression system using TK as substrate measured after 30 mins in presence of ATP by HTRF assay
39
Total Activities
39
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 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 | 39 | 7.08 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4856292 | — | — | 1 | 8.39 |
| CHEMBL5175892 | — | — | 1 | 8.33 |
| CHEMBL5174615 | — | — | 1 | 8.12 |
| CHEMBL5206613 | — | — | 1 | 7.92 |
| CHEMBL5184749 | — | — | 1 | 7.82 |
| CHEMBL5193032 | — | — | 1 | 7.77 |
| CHEMBL5192195 | — | — | 1 | 7.70 |
| CHEMBL5187391 | — | — | 1 | 7.70 |
| CHEMBL5186552 | — | — | 1 | 7.57 |
| CHEMBL5181484 | — | — | 1 | 7.40 |
| CHEMBL5188383 | — | — | 1 | 7.36 |
| CHEMBL5176640 | — | — | 1 | 7.28 |
| CHEMBL4856820 | — | — | 1 | 7.28 |
| CHEMBL5196903 | — | — | 1 | 7.24 |
| CHEMBL5207826 | — | — | 1 | 7.24 |
| CHEMBL5202428 | — | — | 1 | 7.23 |
| CHEMBL5204522 | — | — | 1 | 7.21 |
| CHEMBL5171077 | — | — | 1 | 7.17 |
| CHEMBL5194639 | — | — | 1 | 7.14 |
| CHEMBL5201795 | — | — | 1 | 7.13 |
| CHEMBL5201147 | — | — | 1 | 7.08 |
| CHEMBL5199537 | — | — | 1 | 6.96 |
| CHEMBL5183140 | — | — | 1 | 6.96 |
| CHEMBL5192947 | — | — | 1 | 6.96 |
| CHEMBL5191135 | — | — | 1 | 6.92 |
| CHEMBL5176675 | — | — | 1 | 6.92 |
| CHEMBL5169890 | — | — | 1 | 6.82 |
| CHEMBL5172802 | — | — | 1 | 6.80 |
| CHEMBL5203932 | — | — | 1 | 6.77 |
| CHEMBL5173092 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4856292 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5175892 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5174615 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5206613 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5184749 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5193032 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5192195 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5187391 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5186552 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5181484 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5188383 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5176640 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4856820 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5196903 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5207826 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5202428 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5204522 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5171077 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5194639 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5201795 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5201147 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5199537 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5183140 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5192947 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5191135 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5176675 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5169890 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5172802 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5203932 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5173092 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5181346 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5200768 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5185935 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5176616 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5179876 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5200327 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5179099 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL5199768 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5189091 | — | IC50 | = | 4100.0 | nM | 5.39 |