Assay Detail
Binding
CHEMBL5166478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NCS-382 from CaMK2alpha in rat brain cerebral cortex membrane homogenates assessed as inhibition constant measured after 60 mins by TopCount scintillation counting method
38
Total Activities
21
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 | 38 | 6.59 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206854 | — | — | 2 | 7.85 |
| CHEMBL5191835 | — | — | 2 | 7.60 |
| CHEMBL5196669 | — | — | 2 | 7.51 |
| CHEMBL5178954 | — | — | 2 | 7.50 |
| CHEMBL5175277 | — | — | 1 | 7.46 |
| CHEMBL5181927 | — | — | 2 | 7.33 |
| CHEMBL5172225 | — | — | 2 | 7.20 |
| CHEMBL5198167 | — | — | 2 | 7.20 |
| CHEMBL5200347 | — | — | 2 | 7.13 |
| CHEMBL5181512 | — | — | 2 | 7.11 |
| CHEMBL5190371 | — | — | 2 | 6.40 |
| CHEMBL5194429 | — | — | 2 | 6.30 |
| CHEMBL5192513 | — | — | 2 | 6.10 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | — | 2 | 6.10 |
| CHEMBL5192904 | — | — | 2 | 5.92 |
| CHEMBL5181959 | — | — | 2 | 5.92 |
| CHEMBL139 | DICLOFENAC | 4.0 | 1 | 5.29 |
| CHEMBL5182248 | — | — | 2 | 4.70 |
| CHEMBL5207563 | — | — | 2 | 4.70 |
| CHEMBL5181640 | — | — | 1 | - |
| CHEMBL5203615 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206854 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5206854 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL5191835 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL5191835 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5196669 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5196669 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL5178954 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL5178954 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5175277 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5181927 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5181927 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5198167 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL5172225 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL5172225 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL5198167 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL5200347 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL5181512 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5200347 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5181512 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5190371 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL5190371 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL5194429 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5194429 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL5192513 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL5192513 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL1031 | 5-HYDROXY-DICLOFENAC | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL5181959 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL5192904 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL5192904 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL5181959 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL139 | DICLOFENAC | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL5207563 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL5182248 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL5207563 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL5182248 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL5203615 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5181640 | — | Ki | > | 100000.0 | nM | - |