Assay Detail
Binding
CHEMBL5223479
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Trk-A F595R mutant (unknown origin) incubated for 30 mins by caliper mobility shift assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.97 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 9.70 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.70 |
| CHEMBL5266269 | — | — | 1 | 8.28 |
| CHEMBL5282675 | — | — | 1 | 8.21 |
| CHEMBL5288589 | — | — | 1 | 7.98 |
| CHEMBL5287060 | — | — | 1 | 7.97 |
| CHEMBL5275171 | — | — | 1 | 7.80 |
| CHEMBL5275881 | — | — | 1 | 7.64 |
| CHEMBL5287847 | — | — | 1 | 7.60 |
| CHEMBL5291020 | — | — | 1 | 7.53 |
| CHEMBL5271403 | — | — | 1 | 7.49 |
| CHEMBL5287063 | — | — | 1 | 7.48 |
| CHEMBL5291305 | — | — | 1 | 7.22 |
| CHEMBL5271251 | — | — | 1 | - |
| CHEMBL5288203 | — | — | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
| CHEMBL5282907 | — | — | 1 | - |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5266269 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5282675 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5288589 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5287060 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5275171 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL5275881 | — | IC50 | = | 22.9 | nM | 7.64 |
| CHEMBL5287847 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL5291020 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL5271403 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL5287063 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5291305 | — | IC50 | = | 59.9 | nM | 7.22 |
| CHEMBL5271251 | — | IC50 | - | — | - | |
| CHEMBL5288203 | — | IC50 | - | — | - | |
| CHEMBL1983268 | ENTRECTINIB | IC50 | > | 700.0 | nM | - |
| CHEMBL5282907 | — | IC50 | - | — | - | |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | > | 2000.0 | nM | - |