Assay Detail
Binding
CHEMBL4043634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of bovine GRK2 S670A mutant 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 |
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 | 5.94 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738878 | — | — | 1 | 7.70 |
| CHEMBL1738877 | — | — | 1 | 7.52 |
| CHEMBL4097393 | — | — | 1 | 7.52 |
| CHEMBL4090144 | — | — | 1 | 7.52 |
| CHEMBL3809020 | — | — | 1 | 6.89 |
| CHEMBL4087244 | — | — | 1 | 6.41 |
| CHEMBL4075712 | — | — | 1 | 6.22 |
| CHEMBL4070885 | — | — | 1 | 6.21 |
| CHEMBL4070290 | — | — | 1 | 6.20 |
| CHEMBL4075475 | — | — | 1 | 6.12 |
| CHEMBL384073 | GSK-180736A | — | 1 | 6.11 |
| CHEMBL4099398 | — | — | 1 | 6.11 |
| CHEMBL4076529 | — | — | 1 | 6.11 |
| CHEMBL4079362 | — | — | 1 | 5.90 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 5.86 |
| CHEMBL4077197 | — | — | 1 | 5.82 |
| CHEMBL4091281 | — | — | 1 | 5.82 |
| CHEMBL4063014 | — | — | 1 | 5.75 |
| CHEMBL4072898 | — | — | 1 | 5.69 |
| CHEMBL4064274 | — | — | 1 | 5.69 |
| CHEMBL4090923 | — | — | 1 | 5.69 |
| CHEMBL4077133 | — | — | 1 | 5.68 |
| CHEMBL4105100 | — | — | 1 | 5.68 |
| CHEMBL4098656 | — | — | 1 | 5.66 |
| CHEMBL4083142 | — | — | 1 | 5.62 |
| CHEMBL4073639 | — | — | 1 | 5.57 |
| CHEMBL4074476 | — | — | 1 | 5.52 |
| CHEMBL4077459 | — | — | 1 | 5.49 |
| CHEMBL4076131 | — | — | 1 | 5.48 |
| CHEMBL4084465 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738878 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1738877 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4090144 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4097393 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3809020 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4087244 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4075712 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4070885 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4070290 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4075475 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL384073 | GSK-180736A | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4099398 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4076529 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4079362 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL490 | PAROXETINE | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4077197 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL4091281 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4063014 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL4072898 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4064274 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL4090923 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4077133 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4105100 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL4098656 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4083142 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL4073639 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL4074476 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4077459 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4076131 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL4084465 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4062790 | — | IC50 | = | 6010.0 | nM | 5.22 |
| CHEMBL4071638 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL4081802 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL4101136 | — | IC50 | = | 37700.0 | nM | 4.42 |