Assay Detail
Binding
CHEMBL4775836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Covalent inhibition of GRK5 (unknown origin) using porcine brain tubulin as substrate by [gamma32P]ATP based radiometric assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 3 | 6.89 | 7.72 |
| Kinact | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4786599 | — | — | 2 | 7.72 |
| CHEMBL4785430 | — | — | 2 | 6.96 |
| CHEMBL4791260 | — | — | 2 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4786599 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4785430 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4791260 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4791260 | — | Kinact | > | 1.0 | /min | - |
| CHEMBL4785430 | — | Kinact | > | 1.0 | /min | - |
| CHEMBL4786599 | — | Kinact | > | 0.9 | /min | - |