Assay Detail
Binding
CHEMBL4043633
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Inhibition of GRK2 (unknown origin)
5
Total Activities
5
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 Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.82 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738878 | — | — | 1 | 7.70 |
| CHEMBL1738877 | — | — | 1 | 7.52 |
| CHEMBL3809020 | — | — | 1 | 6.89 |
| CHEMBL384073 | GSK-180736A | — | 1 | 6.11 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738878 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1738877 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3809020 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL384073 | GSK-180736A | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL490 | PAROXETINE | IC50 | = | 1380.0 | nM | 5.86 |