Assay Detail
Binding
CHEMBL4411097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of BODIPY TR-ADP from human GRK2 preincubated for 10 mins followed by compound addition and measured after 10 to 15 mins by fluorescence polarization displacement assay
3
Total Activities
3
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 |
Publication
Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.00 | 5.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517171 | GSK-1713088A | — | 1 | 5.20 |
| CHEMBL476259 | GSK-1326255A | — | 1 | 5.10 |
| CHEMBL463931 | GSK-2163632A | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517171 | GSK-1713088A | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL476259 | GSK-1326255A | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL463931 | GSK-2163632A | IC50 | = | 20000.0 | nM | 4.70 |