Assay Detail
Binding
CHEMBL5166476
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]HOCPCA from CaMK2alpha in rat brain cerebral cortex membrane homogenates assessed as inhibition constant measured after 60 mins by TopCount scintillation counting method
7
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcium/calmodulin-dependent protein kinase type II subunit alpha (CHEMBL2359) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.44 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175277 | — | — | 1 | 7.66 |
| CHEMBL5191835 | — | — | 2 | 7.30 |
| CHEMBL5198167 | — | — | 2 | 7.03 |
| CHEMBL5182248 | — | — | 2 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175277 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5191835 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5191835 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL5198167 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL5198167 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5182248 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL5182248 | — | Ki | = | 39810.72 | nM | 4.40 |