Assay Detail
Binding
CHEMBL3811362
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Inhibition of GRK5 (unknown origin) using tubulin as substrate by SDS-PAGE method
27
Total Activities
27
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, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.13 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3808660 | — | — | 1 | 6.42 |
| CHEMBL3809100 | — | — | 1 | 6.10 |
| CHEMBL3809796 | — | — | 1 | 5.75 |
| CHEMBL1738878 | — | — | 1 | 5.66 |
| CHEMBL3809965 | — | — | 1 | 5.64 |
| CHEMBL3810312 | — | — | 1 | 5.42 |
| CHEMBL3808840 | — | — | 1 | 5.33 |
| CHEMBL3808621 | — | — | 1 | 5.30 |
| CHEMBL3810107 | — | — | 1 | 5.21 |
| CHEMBL3810073 | — | — | 1 | 5.09 |
| CHEMBL3808565 | — | — | 1 | 4.40 |
| CHEMBL3808918 | — | — | 1 | 4.24 |
| CHEMBL3809913 | — | — | 1 | 4.20 |
| CHEMBL3809697 | — | — | 1 | 4.17 |
| CHEMBL3808499 | — | — | 1 | 4.06 |
| CHEMBL3810349 | — | — | 1 | - |
| CHEMBL3810250 | — | — | 1 | - |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | - |
| CHEMBL384073 | GSK-180736A | — | 1 | - |
| CHEMBL3810271 | — | — | 1 | - |
| CHEMBL3809020 | — | — | 1 | - |
| CHEMBL3809788 | — | — | 1 | - |
| CHEMBL3808657 | — | — | 1 | - |
| CHEMBL3809604 | — | — | 1 | - |
| CHEMBL3809124 | — | — | 1 | - |
| CHEMBL3809584 | — | — | 1 | - |
| CHEMBL3810383 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3808660 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3809100 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3809796 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1738878 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3809965 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3810312 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3808840 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3808621 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3810107 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3810073 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL3808565 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3808918 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL3809913 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL3809697 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL3808499 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL3810349 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3810250 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL490 | PAROXETINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL384073 | GSK-180736A | IC50 | > | 100000.0 | nM | - |
| CHEMBL3810271 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809020 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809788 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3808657 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809604 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809124 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3809584 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3810383 | — | IC50 | > | 100000.0 | nM | - |