Assay Detail
Binding
CHEMBL5164769
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Inhibition of TRKC (unknown origin) using Ser/Thr 06 peptide as substrate incubated for 1 hr in presence of 50 uM ATP by FRET based Z'-Lyte assay
10
Total Activities
10
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 the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.60 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.62 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 8.34 |
| CHEMBL5184321 | — | — | 1 | 8.07 |
| CHEMBL5195469 | — | — | 1 | 7.96 |
| CHEMBL5198838 | — | — | 1 | 7.67 |
| CHEMBL5184043 | — | — | 1 | 7.46 |
| CHEMBL5194130 | — | — | 1 | 7.42 |
| CHEMBL5183862 | — | — | 1 | 6.99 |
| CHEMBL5178374 | — | — | 1 | 6.96 |
| CHEMBL5198765 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5184321 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5195469 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5198838 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5184043 | — | IC50 | = | 34.8 | nM | 7.46 |
| CHEMBL5194130 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL5183862 | — | IC50 | = | 102.2 | nM | 6.99 |
| CHEMBL5178374 | — | IC50 | = | 109.8 | nM | 6.96 |
| CHEMBL5198765 | — | IC50 | = | 285.7 | nM | 6.54 |