Assay Detail
Binding
CHEMBL4223319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GRK5 (unknown origin) preincubated for 10 mins followed by peptide substrate and ATP addition measured after 1 hr by TR-FRET assay
40
Total Activities
40
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
Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 4.98 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4225427 | — | — | 1 | 6.58 |
| CHEMBL4228779 | — | — | 1 | 6.42 |
| CHEMBL4229039 | — | — | 1 | 5.77 |
| CHEMBL4227138 | — | — | 1 | 5.72 |
| CHEMBL4225489 | — | — | 1 | 5.62 |
| CHEMBL4227400 | — | — | 1 | 5.55 |
| CHEMBL4228945 | — | — | 1 | 5.46 |
| CHEMBL4229046 | — | — | 1 | 5.21 |
| CHEMBL4225917 | — | — | 1 | 5.20 |
| CHEMBL4228055 | — | — | 1 | 5.03 |
| CHEMBL4227081 | — | — | 1 | 5.02 |
| CHEMBL4227611 | — | — | 1 | 4.92 |
| CHEMBL4224755 | — | — | 1 | 4.89 |
| CHEMBL4226323 | — | — | 1 | 4.80 |
| CHEMBL4227666 | — | — | 1 | 4.75 |
| CHEMBL4227350 | — | — | 1 | 4.72 |
| CHEMBL4228896 | — | — | 1 | 4.72 |
| CHEMBL4226886 | — | — | 1 | 4.72 |
| CHEMBL4225645 | — | — | 1 | 4.68 |
| CHEMBL4228314 | — | — | 1 | 4.68 |
| CHEMBL4227283 | — | — | 1 | 4.60 |
| CHEMBL4226496 | — | — | 1 | 4.57 |
| CHEMBL4226287 | — | — | 1 | 4.57 |
| CHEMBL4226820 | — | — | 1 | 4.42 |
| CHEMBL4229100 | — | — | 1 | 4.36 |
| CHEMBL4227413 | — | — | 1 | 4.18 |
| CHEMBL4225012 | — | — | 1 | 4.15 |
| CHEMBL4228524 | — | — | 1 | 4.11 |
| CHEMBL4228272 | — | — | 1 | - |
| CHEMBL4229149 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4225427 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4228779 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4229039 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4227138 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4225489 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4227400 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4228945 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4229046 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4225917 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4228055 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4227081 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4227611 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4224755 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4226323 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4227666 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4227350 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4226886 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4228896 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4225645 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4228314 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4227283 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4226287 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4226496 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4226820 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4229100 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4227413 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL4225012 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL4228524 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL4227754 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4229210 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4224914 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4226879 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4228117 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4226551 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4226760 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4225310 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4224950 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4228575 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4229149 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4228272 | — | IC50 | > | 100000.0 | nM | - |