Assay Detail
Binding
CHEMBL4775829
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GRK5 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 | 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 |
|---|---|---|---|
| IC50 | 31 | 6.73 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4786599 | — | — | 1 | 8.42 |
| CHEMBL4785430 | — | — | 1 | 8.07 |
| CHEMBL4800665 | — | — | 1 | 7.82 |
| CHEMBL4780266 | — | — | 1 | 7.82 |
| CHEMBL4782014 | — | — | 1 | 7.68 |
| CHEMBL4794078 | — | — | 1 | 7.54 |
| CHEMBL4781735 | — | — | 1 | 7.32 |
| CHEMBL4787507 | — | — | 1 | 7.10 |
| CHEMBL4779427 | — | — | 1 | 7.06 |
| CHEMBL4786185 | — | — | 1 | 7.04 |
| CHEMBL4786846 | — | — | 1 | 7.02 |
| CHEMBL4799210 | — | — | 1 | 6.96 |
| CHEMBL4784634 | — | — | 1 | 6.89 |
| CHEMBL4777196 | — | — | 1 | 6.89 |
| CHEMBL4798127 | — | — | 1 | 6.85 |
| CHEMBL4791260 | — | — | 1 | 6.66 |
| CHEMBL3808660 | — | — | 1 | 6.55 |
| CHEMBL4786913 | — | — | 1 | 6.55 |
| CHEMBL4793010 | — | — | 1 | 6.44 |
| CHEMBL4788756 | — | — | 1 | 6.35 |
| CHEMBL4796116 | — | — | 1 | 6.14 |
| CHEMBL4791163 | — | — | 1 | 6.13 |
| CHEMBL4796861 | — | — | 1 | 6.13 |
| CHEMBL4796154 | — | — | 1 | 6.11 |
| CHEMBL4782275 | — | — | 1 | 6.09 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.08 |
| CHEMBL4789095 | — | — | 1 | 5.89 |
| CHEMBL4798092 | — | — | 1 | 5.71 |
| CHEMBL4783464 | — | — | 1 | 5.60 |
| CHEMBL4794588 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4786599 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4785430 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4800665 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4780266 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4782014 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4794078 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4781735 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4787507 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4779427 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4786185 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4786846 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4799210 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4784634 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4777196 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4798127 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4791260 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3808660 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4786913 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4793010 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4788756 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4796116 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4791163 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4796861 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4796154 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4782275 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL535 | SUNITINIB | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4789095 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4798092 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4783464 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4794588 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL490 | PAROXETINE | IC50 | - | — | - |