Assay Detail
Binding
CHEMBL4411099
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GRK5 using tubulin as substrate measured after 0 mins by [gamma-32P]-ATP assay
7
Total Activities
7
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 | 7 | 5.32 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4475305 | — | — | 1 | 6.66 |
| CHEMBL4456539 | — | — | 1 | 6.24 |
| CHEMBL4543927 | — | — | 1 | 4.75 |
| CHEMBL4450181 | — | — | 1 | 4.70 |
| CHEMBL4464632 | — | — | 1 | 4.23 |
| CHEMBL4449730 | — | — | 1 | - |
| CHEMBL4557065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4475305 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4456539 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4543927 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4450181 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4464632 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL4449730 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4557065 | — | IC50 | > | 100000.0 | nM | - |