Assay Detail
Binding
CHEMBL4040376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PKCalpha active using MBP as substrate after 60 mins in presence of [gamma-32]ATP by scintillation counting
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 | 5.46 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738878 | — | — | 1 | 6.60 |
| CHEMBL4076320 | — | — | 1 | 6.17 |
| CHEMBL4077447 | — | — | 1 | 5.96 |
| CHEMBL4086046 | — | — | 1 | 5.92 |
| CHEMBL4093075 | — | — | 1 | 5.77 |
| CHEMBL4089087 | — | — | 1 | 5.60 |
| CHEMBL4088026 | — | — | 1 | 5.60 |
| CHEMBL4082805 | — | — | 1 | 5.57 |
| CHEMBL4083276 | — | — | 1 | 5.54 |
| CHEMBL4060973 | — | — | 1 | 5.50 |
| CHEMBL4095659 | — | — | 1 | 5.48 |
| CHEMBL4067877 | — | — | 1 | 5.44 |
| CHEMBL4065690 | — | — | 1 | 5.32 |
| CHEMBL4091067 | — | — | 1 | 5.32 |
| CHEMBL4070100 | — | — | 1 | 5.24 |
| CHEMBL4082775 | — | — | 1 | 5.20 |
| CHEMBL4082853 | — | — | 1 | 5.15 |
| CHEMBL4087117 | — | — | 1 | 5.14 |
| CHEMBL4064232 | — | — | 1 | 5.13 |
| CHEMBL4071398 | — | — | 1 | 5.12 |
| CHEMBL1738877 | — | — | 1 | 5.09 |
| CHEMBL4105466 | — | — | 1 | 5.08 |
| CHEMBL4072308 | — | — | 1 | 5.08 |
| CHEMBL4061438 | — | — | 1 | 5.06 |
| CHEMBL4095742 | — | — | 1 | - |
| CHEMBL4059737 | — | — | 1 | - |
| CHEMBL4066027 | — | — | 1 | - |
| CHEMBL4069432 | — | — | 1 | - |
| CHEMBL4090462 | — | — | 1 | - |
| CHEMBL4080151 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738878 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4076320 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4077447 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4086046 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4093075 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4089087 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4088026 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4082805 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4083276 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4060973 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4095659 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4067877 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4065690 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4091067 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4070100 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4082775 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4082853 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4087117 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4064232 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4071398 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL1738877 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4105466 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4072308 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4061438 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4091972 | — | IC50 | - | — | - | |
| CHEMBL4075992 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4091573 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4063774 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4081217 | — | IC50 | - | — | - | |
| CHEMBL4072362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4100175 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4082173 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4096791 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4078768 | — | IC50 | - | — | - | |
| CHEMBL4104512 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4086619 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4072224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4072828 | — | IC50 | - | — | - | |
| CHEMBL4073882 | — | IC50 | - | — | - | |
| CHEMBL4094447 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4103972 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4099309 | — | IC50 | - | — | - | |
| CHEMBL4098177 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4100779 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4080151 | — | IC50 | - | — | - | |
| CHEMBL4090462 | — | IC50 | - | — | - | |
| CHEMBL4069432 | — | IC50 | - | — | - | |
| CHEMBL4066027 | — | IC50 | - | — | - | |
| CHEMBL4059737 | — | IC50 | - | — | - | |
| CHEMBL4095742 | — | IC50 | > | 10000.0 | nM | - |