Assay Detail
Binding
CHEMBL5265542
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Inhibition of TRKC (unknown origin) using TK as substrate in presence of ATP incubated for 40 mins by HTRF KinEASE assay
4
Total Activities
4
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
Design, synthesis and biological evaluation of pyrazolo[3,4-<i>b</i>]pyridine derivatives as TRK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.79 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 9.70 |
| CHEMBL5282566 | — | — | 1 | 7.24 |
| CHEMBL5276362 | — | — | 1 | 7.12 |
| CHEMBL5276440 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5282566 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5276362 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5276440 | — | IC50 | = | 83.0 | nM | 7.08 |