Assay Detail
Binding
CHEMBL4040375
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubated for 60 mins followed by substrate addition measured after 10 mins by Lance TR-FRET assay
92
Total Activities
92
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 |
|---|---|---|---|
| IC50 | 92 | 7.08 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738878 | — | — | 1 | 8.92 |
| CHEMBL4073882 | — | — | 1 | 8.77 |
| CHEMBL4072828 | — | — | 1 | 8.74 |
| CHEMBL4086046 | — | — | 1 | 8.72 |
| CHEMBL4095659 | — | — | 1 | 8.52 |
| CHEMBL4077447 | — | — | 1 | 8.41 |
| CHEMBL4071398 | — | — | 1 | 8.26 |
| CHEMBL4082775 | — | — | 1 | 8.21 |
| CHEMBL4103972 | — | — | 1 | 8.17 |
| CHEMBL4083276 | — | — | 1 | 8.12 |
| CHEMBL4094447 | — | — | 1 | 8.11 |
| CHEMBL4065690 | — | — | 1 | 8.00 |
| CHEMBL4060973 | — | — | 1 | 7.92 |
| CHEMBL4093075 | — | — | 1 | 7.92 |
| CHEMBL4061438 | — | — | 1 | 7.92 |
| CHEMBL4082559 | — | — | 1 | 7.85 |
| CHEMBL4087117 | — | — | 1 | 7.85 |
| CHEMBL4064232 | — | — | 1 | 7.80 |
| CHEMBL4082853 | — | — | 1 | 7.77 |
| CHEMBL1738877 | — | — | 1 | 7.75 |
| CHEMBL4082805 | — | — | 1 | 7.72 |
| CHEMBL4082713 | — | — | 1 | 7.70 |
| CHEMBL4067877 | — | — | 1 | 7.68 |
| CHEMBL4075063 | — | — | 1 | 7.64 |
| CHEMBL4089087 | — | — | 1 | 7.62 |
| CHEMBL4070100 | — | — | 1 | 7.50 |
| CHEMBL4101739 | — | — | 1 | 7.42 |
| CHEMBL4091573 | — | — | 1 | 7.41 |
| CHEMBL4062560 | — | — | 1 | 7.39 |
| CHEMBL4062649 | — | — | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738878 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4073882 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4072828 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4086046 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4095659 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4077447 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4071398 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4082775 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4103972 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4083276 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4094447 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4065690 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4061438 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4093075 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4060973 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4082559 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4087117 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4064232 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4082853 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1738877 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4082805 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4082713 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4067877 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4075063 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4089087 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4070100 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4101739 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4091573 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4062560 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4062649 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4085247 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4072686 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4075992 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4086619 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4063774 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4105466 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3728772 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4072224 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4076320 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4066027 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4085317 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4095595 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4096791 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4095742 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4091451 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4091566 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4088026 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4063621 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4072308 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4098177 | — | IC50 | = | 130.0 | nM | 6.89 |