Assay Detail
Functional
CHEMBL653772
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro vasorelaxant activity (calcium channel blocking activity) was determined with potassium-depolarized rabbit thoracic aorta
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Thoracic aorta |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095229) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Dihydropyrimidine calcium channel blockers. 2. 3-substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.59 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 9.00 |
| CHEMBL2092901 | — | — | 1 | 8.70 |
| CHEMBL3392282 | — | — | 1 | 8.40 |
| CHEMBL440695 | — | — | 1 | 7.77 |
| CHEMBL3392280 | — | — | 1 | 7.58 |
| CHEMBL87921 | — | — | 1 | 7.58 |
| CHEMBL261982 | — | — | 1 | 7.30 |
| CHEMBL39925 | — | — | 1 | 6.89 |
| CHEMBL88449 | — | — | 1 | 6.57 |
| CHEMBL88149 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475534 | NITRENDIPINE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2092901 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3392282 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL440695 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3392280 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL87921 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL261982 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL39925 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL88449 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL88149 | — | IC50 | = | 710.0 | nM | 6.15 |