Assay Detail
Binding
CHEMBL704175
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Displacement of [3H]nitrendipine from rat brain L-type [Ca2+] channel
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.81 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 8.34 |
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | 7.04 |
| CHEMBL290860 | — | — | 1 | 6.60 |
| CHEMBL5483012 | — | — | 2 | 6.43 |
| CHEMBL179334 | — | — | 1 | 6.17 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | - |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405355 | NIGULDIPINE | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL2051956 | DEXNIGULDIPINE | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL290860 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL5483012 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL5483012 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL179334 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL611 | TERAZOSIN | Ki | > | 10000.0 | nM | - |
| CHEMBL2 | PRAZOSIN | Ki | > | 10000.0 | nM | - |