Assay Detail
Functional
CHEMBL798762
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Concentration required to block Ca+2-induced contraction of K+ depolarized rat aorta
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.80 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53020 | — | — | 1 | 8.60 |
| CHEMBL440296 | — | — | 1 | 8.50 |
| CHEMBL53374 | — | — | 1 | 8.50 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.40 |
| CHEMBL298799 | — | — | 1 | 8.30 |
| CHEMBL53019 | — | — | 1 | 8.30 |
| CHEMBL54964 | — | — | 1 | 8.30 |
| CHEMBL1491 | AMLODIPINE | 4.0 | 1 | 8.10 |
| CHEMBL52812 | — | — | 1 | 7.80 |
| CHEMBL301288 | — | — | 1 | 7.80 |
| CHEMBL52965 | — | — | 1 | 7.70 |
| CHEMBL300872 | — | — | 1 | 7.70 |
| CHEMBL54244 | — | — | 1 | 7.70 |
| CHEMBL52989 | — | — | 1 | 7.70 |
| CHEMBL416109 | — | — | 1 | 7.60 |
| CHEMBL54195 | — | — | 1 | 7.60 |
| CHEMBL298773 | — | — | 1 | 7.50 |
| CHEMBL300514 | — | — | 1 | 7.50 |
| CHEMBL300042 | — | — | 1 | 7.30 |
| CHEMBL298783 | — | — | 1 | 7.00 |
| CHEMBL300088 | — | — | 1 | 7.00 |
| CHEMBL300918 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53020 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL440296 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL53374 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL298799 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL53019 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL54964 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1491 | AMLODIPINE | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL52812 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL301288 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL52965 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL300872 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL54244 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL52989 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL416109 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL54195 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL298773 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL300514 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL300042 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL298783 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL300088 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL300918 | — | IC50 | = | 158.49 | nM | 6.80 |