Assay Detail
Binding
CHEMBL3854637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GRK5 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 | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.21 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3950887 | — | — | 1 | 5.80 |
| CHEMBL3942164 | — | — | 1 | 5.68 |
| CHEMBL3931500 | — | — | 1 | 5.41 |
| CHEMBL3953837 | — | — | 1 | 5.13 |
| CHEMBL3971763 | — | — | 1 | 5.03 |
| CHEMBL3900757 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3950887 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3942164 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3931500 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3953837 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3971763 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3900757 | — | IC50 | = | 61300.0 | nM | 4.21 |