Assay Detail
Binding
CHEMBL5099990
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Displacement of [3H]HOCPCA from recombinant rat CaMK2alpha expressed in HEK293T cells measured after 1 hr by liquid scintillation counting method
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293T |
| 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 | 9 | 5.69 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170394 | — | — | 2 | 6.30 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | — | 1 | 6.10 |
| CHEMBL5170093 | — | — | 2 | 5.90 |
| CHEMBL2431324 | — | — | 1 | 5.75 |
| CHEMBL472694 | — | — | 2 | 5.41 |
| CHEMBL1342 | OXYBATE | 4.0 | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170394 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL5170394 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL5170093 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL5170093 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2431324 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL472694 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL472694 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL1342 | OXYBATE | Ki | = | 51000.0 | nM | 4.29 |