Assay Detail
Binding
CHEMBL4840465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human TRKB (456 to 822 residues) expressed in baculovirus infected Sf21 cells using TK as substrate in presence of ATP measured after 40 mins by HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.43 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4856292 | — | — | 1 | 8.33 |
| CHEMBL4856835 | — | — | 1 | 7.64 |
| CHEMBL4862017 | — | — | 1 | 7.57 |
| CHEMBL4849505 | — | — | 1 | 7.55 |
| CHEMBL4866306 | — | — | 1 | 7.46 |
| CHEMBL4862580 | — | — | 1 | 6.77 |
| CHEMBL4858347 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4856292 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4856835 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4862017 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4849505 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4866306 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4862580 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4858347 | — | IC50 | = | 190.0 | nM | 6.72 |