Assay Detail
Binding
CHEMBL982306
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Displacement of [3H]diltiazem from benzodiazepine binding site of L-type calcium channel in Wistar rat cerebral cortex membrane
18
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.25 | 6.13 |
| pKi | 2 | - | - |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL176045 | FANCHININ | — | 1 | 6.13 |
| CHEMBL509109 | — | — | 1 | 5.82 |
| CHEMBL453024 | — | — | 1 | 5.75 |
| CHEMBL452763 | — | — | 1 | 5.74 |
| CHEMBL455620 | — | — | 1 | 5.70 |
| CHEMBL510364 | — | — | 1 | 5.60 |
| CHEMBL451988 | — | — | 1 | 5.57 |
| CHEMBL452500 | — | — | 1 | 5.38 |
| CHEMBL451722 | — | — | 1 | 5.02 |
| CHEMBL451987 | — | — | 1 | 4.90 |
| CHEMBL453293 | — | — | 1 | 4.86 |
| CHEMBL453292 | METHYL COCLAURINE | — | 1 | 4.64 |
| CHEMBL452762 | — | — | 1 | 4.61 |
| CHEMBL114853 | — | — | 1 | 4.51 |
| CHEMBL451723 | — | — | 1 | 4.49 |
| CHEMBL507843 | — | — | 1 | - |
| CHEMBL510363 | — | — | 1 | - |
| CHEMBL453291 | COCLAURINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL176045 | FANCHININ | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL509109 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL453024 | — | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL452763 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL455620 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL510364 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL451988 | — | Ki | = | 2691.53 | nM | 5.57 |
| CHEMBL452500 | — | Ki | = | 4168.69 | nM | 5.38 |
| CHEMBL451722 | — | Ki | = | 9549.93 | nM | 5.02 |
| CHEMBL451987 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL453293 | — | Ki | = | 13803.84 | nM | 4.86 |
| CHEMBL453292 | METHYL COCLAURINE | Ki | = | 22908.68 | nM | 4.64 |
| CHEMBL452762 | — | Ki | = | 24547.09 | nM | 4.61 |
| CHEMBL114853 | — | Ki | = | 30902.95 | nM | 4.51 |
| CHEMBL451723 | — | Ki | = | 32359.37 | nM | 4.49 |
| CHEMBL507843 | — | pKi | - | — | - | |
| CHEMBL510363 | — | pKi | - | — | - | |
| CHEMBL453291 | COCLAURINE | Activity | = | 30.0 | % | - |