Assay Detail
Binding
CHEMBL4040378
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Inhibition of human GRK2 expressed in HEK-B2 cells assessed as isoproterenol-stimulated cAMP accumulation preincubation for 20 mins followed by isoproterenol stimulation measured after 20 mins by cAMP ALPHA-screen assay
23
Total Activities
23
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
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 4.75 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072828 | — | — | 1 | 5.82 |
| CHEMBL4086046 | — | — | 1 | 5.52 |
| CHEMBL4094447 | — | — | 1 | 5.13 |
| CHEMBL1738877 | — | — | 1 | 5.00 |
| CHEMBL4071398 | — | — | 1 | 4.92 |
| CHEMBL4073882 | — | — | 1 | 4.64 |
| CHEMBL4070100 | — | — | 1 | 4.58 |
| CHEMBL4061438 | — | — | 1 | 4.48 |
| CHEMBL4082775 | — | — | 1 | 4.39 |
| CHEMBL4064232 | — | — | 1 | 4.35 |
| CHEMBL4095659 | — | — | 1 | 4.12 |
| CHEMBL4083276 | — | — | 1 | 4.06 |
| CHEMBL1738878 | — | — | 1 | - |
| CHEMBL4103972 | — | — | 1 | - |
| CHEMBL4091972 | — | — | 1 | - |
| CHEMBL4091067 | — | — | 1 | - |
| CHEMBL4075992 | — | — | 1 | - |
| CHEMBL4091573 | — | — | 1 | - |
| CHEMBL4063774 | — | — | 1 | - |
| CHEMBL4077447 | — | — | 1 | - |
| CHEMBL4060973 | — | — | 1 | - |
| CHEMBL4082853 | — | — | 1 | - |
| CHEMBL4086619 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072828 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4086046 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4094447 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL1738877 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4071398 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4073882 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4070100 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4061438 | — | EC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4082775 | — | EC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL4064232 | — | EC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4095659 | — | EC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL4083276 | — | EC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL1738878 | — | EC50 | - | — | - | |
| CHEMBL4103972 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4091972 | — | EC50 | - | — | - | |
| CHEMBL4091067 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4075992 | — | EC50 | - | — | - | |
| CHEMBL4091573 | — | EC50 | = | 220000.0 | nM | - |
| CHEMBL4063774 | — | EC50 | = | 930000.0 | nM | - |
| CHEMBL4077447 | — | EC50 | = | 120000.0 | nM | - |
| CHEMBL4060973 | — | EC50 | - | — | - | |
| CHEMBL4082853 | — | EC50 | - | — | - | |
| CHEMBL4086619 | — | EC50 | = | 1900000.0 | nM | - |