Assay Detail
Binding
CHEMBL5367750
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKC (unknown origin) using Ser/Thr 06 as peptide substrate incubated for 1 hr in presence of ATP by FRET based Z-LYTE assay
23
Total Activities
23
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
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.11 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.96 |
| CHEMBL4298138 | REPOTRECTINIB | 4.0 | 1 | 8.93 |
| CHEMBL5410884 | — | — | 1 | 8.55 |
| CHEMBL5416521 | — | — | 1 | 8.39 |
| CHEMBL5423601 | — | — | 1 | 8.35 |
| CHEMBL5432219 | — | — | 1 | 8.28 |
| CHEMBL5421829 | — | — | 1 | 8.26 |
| CHEMBL5439833 | — | — | 1 | 8.25 |
| CHEMBL5394378 | — | — | 1 | 8.22 |
| CHEMBL5429379 | — | — | 1 | 8.15 |
| CHEMBL5415833 | — | — | 1 | 8.07 |
| CHEMBL5405759 | — | — | 1 | 8.04 |
| CHEMBL5408929 | — | — | 1 | 8.03 |
| CHEMBL5422195 | — | — | 1 | 8.02 |
| CHEMBL5394049 | — | — | 1 | 7.96 |
| CHEMBL5195469 | — | — | 1 | 7.96 |
| CHEMBL5422091 | — | — | 1 | 7.95 |
| CHEMBL5420615 | — | — | 1 | 7.94 |
| CHEMBL5410147 | — | — | 1 | 7.87 |
| CHEMBL5396972 | — | — | 1 | 7.83 |
| CHEMBL5433110 | — | — | 1 | 7.69 |
| CHEMBL5438621 | — | — | 1 | 7.56 |
| CHEMBL5404881 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4298138 | REPOTRECTINIB | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL5410884 | — | IC50 | = | 2.83 | nM | 8.55 |
| CHEMBL5416521 | — | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL5423601 | — | IC50 | = | 4.51 | nM | 8.35 |
| CHEMBL5432219 | — | IC50 | = | 5.22 | nM | 8.28 |
| CHEMBL5421829 | — | IC50 | = | 5.48 | nM | 8.26 |
| CHEMBL5439833 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5394378 | — | IC50 | = | 5.95 | nM | 8.22 |
| CHEMBL5429379 | — | IC50 | = | 7.06 | nM | 8.15 |
| CHEMBL5415833 | — | IC50 | = | 8.51 | nM | 8.07 |
| CHEMBL5405759 | — | IC50 | = | 9.17 | nM | 8.04 |
| CHEMBL5408929 | — | IC50 | = | 9.45 | nM | 8.03 |
| CHEMBL5422195 | — | IC50 | = | 9.56 | nM | 8.02 |
| CHEMBL5394049 | — | IC50 | = | 10.84 | nM | 7.96 |
| CHEMBL5195469 | — | IC50 | = | 11.01 | nM | 7.96 |
| CHEMBL5422091 | — | IC50 | = | 11.29 | nM | 7.95 |
| CHEMBL5420615 | — | IC50 | = | 11.44 | nM | 7.94 |
| CHEMBL5410147 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5396972 | — | IC50 | = | 14.66 | nM | 7.83 |
| CHEMBL5433110 | — | IC50 | = | 20.26 | nM | 7.69 |
| CHEMBL5438621 | — | IC50 | = | 27.75 | nM | 7.56 |
| CHEMBL5404881 | — | IC50 | = | 42.4 | nM | 7.37 |