Assay Detail
Binding
CHEMBL4775830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of bovine GRK2 using porcine brain tubulin as substrate incubated for 3 to 5 mins by [gamma32P]ATP based radiometric assay
31
Total Activities
31
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
Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.09 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799210 | — | — | 1 | 6.16 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 6.11 |
| CHEMBL4800665 | — | — | 1 | 5.96 |
| CHEMBL4777196 | — | — | 1 | 5.77 |
| CHEMBL4796154 | — | — | 1 | 5.68 |
| CHEMBL4780266 | — | — | 1 | 5.44 |
| CHEMBL4786599 | — | — | 1 | 5.32 |
| CHEMBL4787507 | — | — | 1 | 5.17 |
| CHEMBL4796116 | — | — | 1 | 5.14 |
| CHEMBL4788756 | — | — | 1 | 5.02 |
| CHEMBL4794078 | — | — | 1 | 4.96 |
| CHEMBL4785430 | — | — | 1 | 4.92 |
| CHEMBL4784634 | — | — | 1 | 4.89 |
| CHEMBL4786846 | — | — | 1 | 4.82 |
| CHEMBL4793010 | — | — | 1 | 4.77 |
| CHEMBL4798127 | — | — | 1 | 4.72 |
| CHEMBL4781735 | — | — | 1 | 4.66 |
| CHEMBL4779427 | — | — | 1 | 4.64 |
| CHEMBL4782014 | — | — | 1 | 4.36 |
| CHEMBL4789095 | — | — | 1 | 4.36 |
| CHEMBL4782275 | — | — | 1 | 4.06 |
| CHEMBL4794588 | — | — | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL3808660 | — | — | 1 | - |
| CHEMBL4791163 | — | — | 1 | - |
| CHEMBL4786913 | — | — | 1 | - |
| CHEMBL4791260 | — | — | 1 | - |
| CHEMBL4796861 | — | — | 1 | - |
| CHEMBL4783464 | — | — | 1 | - |
| CHEMBL4798092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799210 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL490 | PAROXETINE | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4800665 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4777196 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4796154 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4780266 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4786599 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4787507 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4796116 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4788756 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4794078 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4785430 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4784634 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4786846 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4793010 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4798127 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4781735 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4779427 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4782014 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4789095 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4782275 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4794588 | — | IC50 | = | 190000.0 | nM | - |
| CHEMBL535 | SUNITINIB | IC50 | = | 130000.0 | nM | - |
| CHEMBL3808660 | — | IC50 | - | — | - | |
| CHEMBL4791163 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4786913 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL4791260 | — | IC50 | = | 350000.0 | nM | - |
| CHEMBL4796861 | — | IC50 | = | 280000.0 | nM | - |
| CHEMBL4783464 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL4798092 | — | IC50 | = | 630000.0 | nM | - |
| CHEMBL4786185 | — | IC50 | = | 130000.0 | nM | - |