Assay Detail
Binding
CHEMBL3854629
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Inhibition of bovine GRK2 S670A mutant assessed as decrease in phosphorylation of tubulin after 5 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 |
| 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 | 5.50 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384073 | GSK-180736A | — | 1 | 6.60 |
| CHEMBL6067650 | PAROXETINE HYDROCHLORIDE | 4.0 | 1 | 5.89 |
| CHEMBL3918278 | — | — | 1 | 5.60 |
| CHEMBL374453 | GSK-299115A | — | 1 | 5.50 |
| CHEMBL441702 | GSK-270822A | — | 1 | 4.90 |
| CHEMBL427058 | GSK-466317A | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384073 | GSK-180736A | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL6067650 | PAROXETINE HYDROCHLORIDE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3918278 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL374453 | GSK-299115A | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL441702 | GSK-270822A | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL427058 | GSK-466317A | IC50 | = | 31600.0 | nM | 4.50 |