Assay Detail
Binding
CHEMBL4411101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GRK5 using tubulin as substrate measured after 60 mins by [gamma-32P]-ATP assay
6
Total Activities
6
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 Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.75 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4475305 | — | — | 1 | 6.57 |
| CHEMBL4456539 | — | — | 1 | 6.46 |
| CHEMBL4450181 | — | — | 1 | 5.26 |
| CHEMBL4543927 | — | — | 1 | 5.23 |
| CHEMBL4464632 | — | — | 1 | 5.21 |
| CHEMBL4449730 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4475305 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4456539 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4450181 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4543927 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4464632 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4449730 | — | IC50 | > | 100000.0 | nM | - |