Assay Detail
Binding
CHEMBL5581995
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TRKA G595R mutant (unknown origin) using TK as substrate incubated for 30 mins in presence of ATP by HTRF assay
32
Total Activities
32
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 indazole derivatives as second-generation TRK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.48 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | 2.0 | 1 | 8.10 |
| CHEMBL5592878 | — | — | 1 | 8.05 |
| CHEMBL5594048 | — | — | 1 | 7.72 |
| CHEMBL5590602 | — | — | 1 | 7.52 |
| CHEMBL5594742 | — | — | 1 | 7.50 |
| CHEMBL5594862 | — | — | 1 | 7.46 |
| CHEMBL5593896 | — | — | 1 | 7.20 |
| CHEMBL5595598 | — | — | 1 | 7.04 |
| CHEMBL5595302 | — | — | 1 | 6.96 |
| CHEMBL5592996 | — | — | 1 | 6.85 |
| CHEMBL5589917 | — | — | 1 | 6.77 |
| CHEMBL5593467 | — | — | 1 | 6.70 |
| CHEMBL5593077 | — | — | 1 | 6.68 |
| CHEMBL5592403 | — | — | 1 | 6.62 |
| CHEMBL5594297 | — | — | 1 | 6.60 |
| CHEMBL5591390 | — | — | 1 | 6.54 |
| CHEMBL5591824 | — | — | 1 | 6.46 |
| CHEMBL5594945 | — | — | 1 | 6.44 |
| CHEMBL5594313 | — | — | 1 | 6.42 |
| CHEMBL5593345 | — | — | 1 | 6.26 |
| CHEMBL5593208 | — | — | 1 | 6.24 |
| CHEMBL5593324 | — | — | 1 | 6.17 |
| CHEMBL5593667 | — | — | 1 | 5.95 |
| CHEMBL5590989 | — | — | 1 | 5.93 |
| CHEMBL5593663 | — | — | 1 | 5.87 |
| CHEMBL5594622 | — | — | 1 | 5.44 |
| CHEMBL5590944 | — | — | 1 | 5.32 |
| CHEMBL5592040 | — | — | 1 | 5.25 |
| CHEMBL5595137 | — | — | 1 | 5.24 |
| CHEMBL5593391 | — | — | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297627 | SELITRECTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5592878 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5594048 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5590602 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5594742 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5594862 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5593896 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5595598 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5595302 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5592996 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5589917 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5593467 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5593077 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5592403 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5594297 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5591390 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5591824 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5594945 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5594313 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5593345 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5593208 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5593324 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5593667 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL5590989 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL5593663 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL5594622 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL5590944 | — | IC50 | = | 4830.0 | nM | 5.32 |
| CHEMBL5592040 | — | IC50 | = | 5580.0 | nM | 5.25 |
| CHEMBL5595137 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL5593391 | — | IC50 | = | 8590.0 | nM | 5.07 |
| CHEMBL5595502 | — | IC50 | = | 33130.0 | nM | 4.48 |
| CHEMBL5594550 | — | IC50 | > | 50000.0 | nM | - |