Assay Detail
Binding
CHEMBL4043636
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of bovine GRK5 after 5 mins after 5 mins in presence of ATP by phosphorimaging assay
34
Total Activities
34
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 |
Target
G protein-coupled receptor kinase 5 (CHEMBL3879830) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
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 | 34 | 4.70 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738878 | — | — | 1 | 5.66 |
| CHEMBL4097393 | — | — | 1 | 5.40 |
| CHEMBL4090144 | — | — | 1 | 5.15 |
| CHEMBL1738877 | — | — | 1 | 5.04 |
| CHEMBL4064274 | — | — | 1 | 4.99 |
| CHEMBL4075475 | — | — | 1 | 4.83 |
| CHEMBL4070885 | — | — | 1 | 4.77 |
| CHEMBL4063014 | — | — | 1 | 4.48 |
| CHEMBL4091281 | — | — | 1 | 4.43 |
| CHEMBL4090923 | — | — | 1 | 4.42 |
| CHEMBL4098656 | — | — | 1 | 4.37 |
| CHEMBL4071638 | — | — | 1 | 4.12 |
| CHEMBL4077197 | — | — | 1 | 4.12 |
| CHEMBL4099398 | — | — | 1 | 4.07 |
| CHEMBL4073639 | — | — | 1 | - |
| CHEMBL4101136 | — | — | 1 | - |
| CHEMBL4083142 | — | — | 1 | - |
| CHEMBL4072898 | — | — | 1 | - |
| CHEMBL4076131 | — | — | 1 | - |
| CHEMBL4074476 | — | — | 1 | - |
| CHEMBL4077459 | — | — | 1 | - |
| CHEMBL4062790 | — | — | 1 | - |
| CHEMBL4084465 | — | — | 1 | - |
| CHEMBL4081802 | — | — | 1 | - |
| CHEMBL4075712 | — | — | 1 | - |
| CHEMBL4087244 | — | — | 1 | - |
| CHEMBL4105100 | — | — | 1 | - |
| CHEMBL4076529 | — | — | 1 | - |
| CHEMBL4079362 | — | — | 1 | - |
| CHEMBL4070290 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738878 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4097393 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4090144 | — | IC50 | = | 7090.0 | nM | 5.15 |
| CHEMBL1738877 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4064274 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL4075475 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4070885 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL4063014 | — | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL4091281 | — | IC50 | = | 37200.0 | nM | 4.43 |
| CHEMBL4090923 | — | IC50 | = | 38400.0 | nM | 4.42 |
| CHEMBL4098656 | — | IC50 | = | 42300.0 | nM | 4.37 |
| CHEMBL4077197 | — | IC50 | = | 76300.0 | nM | 4.12 |
| CHEMBL4071638 | — | IC50 | = | 75700.0 | nM | 4.12 |
| CHEMBL4099398 | — | IC50 | = | 84300.0 | nM | 4.07 |
| CHEMBL490 | PAROXETINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL384073 | GSK-180736A | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809020 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4077133 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4073639 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4101136 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4083142 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4072898 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4076131 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4074476 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4077459 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4062790 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4084465 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4081802 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4075712 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4087244 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4105100 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4076529 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4079362 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4070290 | — | IC50 | > | 100000.0 | nM | - |