Assay Detail
Binding
CHEMBL653728
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Inhibition of [3H]nitrendipine binding to L-type calcium channel in guinea pig ventricular myocardium membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Myocardium |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL1940) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 7.57 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 9.59 |
| CHEMBL3392281 | — | — | 1 | 8.59 |
| CHEMBL2398396 | — | — | 1 | 7.92 |
| CHEMBL39925 | — | — | 1 | 7.64 |
| CHEMBL3392285 | — | — | 1 | 7.46 |
| CHEMBL88149 | — | — | 1 | 6.98 |
| CHEMBL282279 | — | — | 1 | 6.92 |
| CHEMBL3392278 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | Kd | = | 0.26 | nM | 9.59 |
| CHEMBL3392281 | — | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL2398396 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL39925 | — | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL3392285 | — | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL88149 | — | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL282279 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL3392278 | — | Kd | = | 3400.0 | nM | 5.47 |