Assay Detail
Binding
CHEMBL5099989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]HOCPCA from native CaMK2alpha in rat brain cortical membrane homogenates measured after 1 hr by TopCount scintillation counting method
14
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | 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
Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.89 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | — | 1 | 7.66 |
| CHEMBL5170394 | — | — | 2 | 7.30 |
| CHEMBL5176248 | — | — | 2 | 7.30 |
| CHEMBL5182678 | — | — | 2 | 7.10 |
| CHEMBL5170093 | — | — | 2 | 6.90 |
| CHEMBL2431324 | — | — | 1 | 6.89 |
| CHEMBL472694 | — | — | 2 | 6.23 |
| CHEMBL1342 | OXYBATE | 4.0 | 1 | 5.52 |
| CHEMBL5201182 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5170394 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5176248 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL5176248 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5170394 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL5182678 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5182678 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL5170093 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL2431324 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL5170093 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL472694 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL472694 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1342 | OXYBATE | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5201182 | — | Ki | - | — | - |