Assay Detail
Binding
CHEMBL664887
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Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| 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
Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.89 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 9.60 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 9.00 |
| CHEMBL159854 | — | — | 1 | 9.00 |
| CHEMBL2110302 | — | — | 1 | 7.52 |
| CHEMBL161165 | — | — | 1 | 7.10 |
| CHEMBL2110168 | — | — | 1 | 6.60 |
| CHEMBL2110303 | — | — | 1 | 6.30 |
| CHEMBL2110169 | — | — | 1 | 6.19 |
| CHEMBL2110298 | — | — | 1 | 5.52 |
| CHEMBL2110170 | — | — | 1 | 5.30 |
| CHEMBL2110167 | — | — | 1 | 5.30 |
| CHEMBL2110301 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL159854 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2110302 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL161165 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2110168 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2110303 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2110169 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL2110298 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2110170 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2110167 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2110301 | — | Ki | = | 6000.0 | nM | 5.22 |