Assay Detail
Binding
CHEMBL4040380
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins followed by substrate addition measured after 10 mins by Lance TR-FRET assay
6
Total Activities
6
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 |
Target
G protein-coupled receptor kinase 3 (CHEMBL1075166) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| IC50 | 6 | 8.46 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072828 | — | — | 1 | 9.19 |
| CHEMBL4082775 | — | — | 1 | 8.74 |
| CHEMBL4083276 | — | — | 1 | 8.48 |
| CHEMBL4065690 | — | — | 1 | 8.37 |
| CHEMBL1738877 | — | — | 1 | 8.27 |
| CHEMBL4095595 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072828 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4082775 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4083276 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4065690 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1738877 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4095595 | — | IC50 | = | 21.0 | nM | 7.68 |