Assay Detail
Binding
CHEMBL5538137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKA (unknown origin) G595R mutant using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysis
43
Total Activities
43
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 |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.49 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.30 |
| CHEMBL5571549 | — | — | 1 | 7.80 |
| CHEMBL5567348 | — | — | 1 | 7.40 |
| CHEMBL5570911 | — | — | 1 | 7.30 |
| CHEMBL5564839 | — | — | 1 | 7.30 |
| CHEMBL5566495 | — | — | 1 | 7.21 |
| CHEMBL5591472 | — | — | 1 | 7.00 |
| CHEMBL5575629 | — | — | 1 | 7.00 |
| CHEMBL5579663 | — | — | 1 | 6.96 |
| CHEMBL5575222 | — | — | 1 | 6.96 |
| CHEMBL5570831 | — | — | 1 | 6.82 |
| CHEMBL5572827 | — | — | 1 | 6.57 |
| CHEMBL5572249 | — | — | 1 | 6.41 |
| CHEMBL5591904 | — | — | 1 | 6.32 |
| CHEMBL5575701 | — | — | 1 | 6.15 |
| CHEMBL5590994 | — | — | 1 | 6.11 |
| CHEMBL5570878 | — | — | 1 | 6.03 |
| CHEMBL5574486 | — | — | 1 | 5.82 |
| CHEMBL5564716 | — | — | 1 | 5.70 |
| CHEMBL5565619 | — | — | 1 | 5.69 |
| CHEMBL5575749 | — | — | 1 | 5.52 |
| CHEMBL5593271 | — | — | 1 | 4.75 |
| CHEMBL5583568 | — | — | 1 | 4.19 |
| CHEMBL5572303 | — | — | 1 | - |
| CHEMBL5574592 | — | — | 1 | - |
| CHEMBL5573049 | — | — | 1 | - |
| CHEMBL5593884 | — | — | 1 | - |
| CHEMBL5574570 | — | — | 1 | - |
| CHEMBL5564678 | — | — | 1 | - |
| CHEMBL5575451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5571549 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5567348 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5570911 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5564839 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5566495 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5591472 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5575629 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5579663 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5575222 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5570831 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5572827 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5572249 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5591904 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5575701 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5590994 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5570878 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5574486 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL5564716 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5565619 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL5575749 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL5593271 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL5583568 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL5563728 | — | IC50 | - | — | - | |
| CHEMBL5574463 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5569634 | — | IC50 | - | — | - | |
| CHEMBL5574290 | — | IC50 | - | — | - | |
| CHEMBL5575160 | — | IC50 | - | — | - | |
| CHEMBL5595899 | — | IC50 | - | — | - | |
| CHEMBL5575761 | — | IC50 | - | — | - | |
| CHEMBL5568832 | — | IC50 | - | — | - | |
| CHEMBL5573503 | — | IC50 | - | — | - | |
| CHEMBL5572829 | — | IC50 | - | — | - | |
| CHEMBL5573820 | — | IC50 | - | — | - | |
| CHEMBL5572418 | — | IC50 | - | — | - | |
| CHEMBL5567387 | — | IC50 | - | — | - | |
| CHEMBL5575451 | — | IC50 | - | — | - | |
| CHEMBL5564678 | — | IC50 | - | — | - | |
| CHEMBL5574570 | — | IC50 | - | — | - | |
| CHEMBL5593884 | — | IC50 | - | — | - | |
| CHEMBL5573049 | — | IC50 | - | — | - | |
| CHEMBL5574592 | — | IC50 | - | — | - | |
| CHEMBL5572303 | — | IC50 | - | — | - |