Assay Detail
Binding
CHEMBL4411104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of bovine GRK2 using tubulin as substrate measured after 4 hrs by [gamma-32P]-ATP assay
16
Total Activities
16
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 Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.48 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456539 | — | — | 1 | 6.17 |
| CHEMBL4576822 | — | — | 1 | 5.68 |
| CHEMBL4475305 | — | — | 1 | 5.57 |
| CHEMBL4569321 | — | — | 1 | 5.54 |
| CHEMBL4456130 | — | — | 1 | 5.50 |
| CHEMBL4450181 | — | — | 1 | 4.41 |
| CHEMBL4449730 | — | — | 1 | - |
| CHEMBL4464632 | — | — | 1 | - |
| CHEMBL4543927 | — | — | 1 | - |
| CHEMBL4536595 | — | — | 1 | - |
| CHEMBL4578499 | — | — | 1 | - |
| CHEMBL4517792 | — | — | 1 | - |
| CHEMBL4557065 | — | — | 1 | - |
| CHEMBL4447191 | — | — | 1 | - |
| CHEMBL4524355 | — | — | 1 | - |
| CHEMBL4592746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456539 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4576822 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4475305 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4569321 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4456130 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4450181 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4449730 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464632 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4543927 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4536595 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4578499 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4517792 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4557065 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4447191 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4524355 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4592746 | — | IC50 | > | 100000.0 | nM | - |