Assay Detail
Binding
CHEMBL5110447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKA G667A mutant (unknown origin) using TK-sub-biotin peptide as substrate incubated for 30 mins followed by treated with ATP and substrate for 40 mins by FRET-based-Z'-lyte kinase assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.08 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195375 | — | — | 1 | 8.64 |
| CHEMBL5198983 | — | — | 1 | 8.46 |
| CHEMBL5170096 | — | — | 1 | 8.29 |
| CHEMBL5188045 | — | — | 1 | 8.28 |
| CHEMBL5169970 | — | — | 1 | 8.18 |
| CHEMBL5170464 | — | — | 1 | 8.12 |
| CHEMBL5205989 | — | — | 1 | 8.12 |
| CHEMBL5189971 | — | — | 1 | 8.11 |
| CHEMBL5173256 | — | — | 1 | 8.10 |
| CHEMBL5193919 | — | — | 1 | 8.07 |
| CHEMBL5196651 | — | — | 1 | 8.06 |
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 7.90 |
| CHEMBL5175608 | — | — | 1 | 7.82 |
| CHEMBL5184432 | — | — | 1 | 7.81 |
| CHEMBL5170412 | — | — | 1 | 7.80 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195375 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5198983 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5170096 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5188045 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5169970 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5170464 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5205989 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5189971 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL5173256 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5193919 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5196651 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5175608 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL5184432 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL5170412 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 32.2 | nM | 7.49 |