Assay Detail
Binding
CHEMBL5099988
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NCS-382 from CaMK2alpha in rat brain cortical membrane homogenates measured after 1 hr by TopCount scintillation counting method
32
Total Activities
18
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 | 32 | 6.57 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5176248 | — | — | 2 | 7.50 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | — | 1 | 7.46 |
| CHEMBL5170394 | — | — | 2 | 7.40 |
| CHEMBL5182530 | — | — | 2 | 7.30 |
| CHEMBL5189628 | — | — | 2 | 7.30 |
| CHEMBL5177983 | — | — | 2 | 7.30 |
| CHEMBL5170093 | — | — | 2 | 7.11 |
| CHEMBL5175633 | — | — | 2 | 7.00 |
| CHEMBL5198432 | — | — | 2 | 7.00 |
| CHEMBL2431324 | — | — | 1 | 6.80 |
| CHEMBL5201182 | — | — | 2 | 6.70 |
| CHEMBL5208394 | — | — | 2 | 6.50 |
| CHEMBL472694 | — | — | 1 | 6.47 |
| CHEMBL5196579 | — | — | 2 | 6.42 |
| CHEMBL1342 | OXYBATE | 4.0 | 1 | 5.37 |
| CHEMBL5196334 | — | — | 2 | 5.01 |
| CHEMBL5183075 | — | — | 2 | 4.90 |
| CHEMBL5182678 | — | — | 2 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5176248 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5176248 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5170394 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL5182530 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5177983 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5170394 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL5189628 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5177983 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL5189628 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL5182530 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL5170093 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL5170093 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5198432 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5175633 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5175633 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL5198432 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2431324 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL5201182 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL5201182 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL5208394 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL5208394 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL472694 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL5196579 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL5196579 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1342 | OXYBATE | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL5196334 | — | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL5196334 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL5183075 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL5182678 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL5183075 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL5182678 | — | Ki | = | 14000.0 | nM | 4.85 |