Assay Detail
Binding
CHEMBL3854636
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant bovine GRK3 expressed in Sf9 insect cells assessed as decrease in phosphorylation of urea-washed bovine rod outer segments in presence of Gbetagamma subunits and [gamma-32P]-ATP after 5 to 60 mins by SDS-PAGE analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G protein-coupled receptor kinase 3 (CHEMBL3711487) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.90 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3950887 | — | — | 1 | 5.82 |
| CHEMBL3931500 | — | — | 1 | 5.21 |
| CHEMBL3942164 | — | — | 1 | 4.94 |
| CHEMBL3953837 | — | — | 1 | 4.65 |
| CHEMBL3900757 | — | — | 1 | 4.52 |
| CHEMBL3971763 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3950887 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3931500 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3942164 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL3953837 | — | IC50 | = | 22600.0 | nM | 4.65 |
| CHEMBL3900757 | — | IC50 | = | 30400.0 | nM | 4.52 |
| CHEMBL3971763 | — | IC50 | = | 55500.0 | nM | 4.26 |