Assay Detail
Binding
CHEMBL3270057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat Cav1.2 channel in rat mesenteric artery assessed as relaxation of 70 mM K+ induced contraction
28
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Artery |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL3762) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 24 | - | - |
| IC50 | 4 | 6.25 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 2 | 8.85 |
| CHEMBL1164066 | — | — | 2 | 6.47 |
| CHEMBL3260892 | — | — | 2 | 4.97 |
| CHEMBL3221247 | — | — | 2 | 4.69 |
| CHEMBL3221248 | — | — | 1 | - |
| CHEMBL3221238 | — | — | 1 | - |
| CHEMBL3260888 | — | — | 1 | - |
| CHEMBL3221241 | — | — | 1 | - |
| CHEMBL3221240 | — | — | 1 | - |
| CHEMBL3221239 | — | — | 1 | - |
| CHEMBL3260889 | — | — | 1 | - |
| CHEMBL3260890 | — | — | 1 | - |
| CHEMBL3221242 | — | — | 1 | - |
| CHEMBL3260891 | — | — | 1 | - |
| CHEMBL3221243 | — | — | 1 | - |
| CHEMBL3221244 | — | — | 1 | - |
| CHEMBL3221245 | — | — | 1 | - |
| CHEMBL3260893 | — | — | 1 | - |
| CHEMBL3260894 | — | — | 1 | - |
| CHEMBL3260895 | — | — | 1 | - |
| CHEMBL3260896 | — | — | 1 | - |
| CHEMBL3221246 | — | — | 1 | - |
| CHEMBL3261115 | — | — | 1 | - |
| CHEMBL1164407 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL1164066 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3260892 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL3221247 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL3221248 | — | Inhibition | - | % | - | |
| CHEMBL3221238 | — | Inhibition | - | % | - | |
| CHEMBL3260888 | — | Inhibition | - | % | - | |
| CHEMBL3221241 | — | Inhibition | - | % | - | |
| CHEMBL3221240 | — | Inhibition | - | % | - | |
| CHEMBL3221239 | — | Inhibition | - | % | - | |
| CHEMBL3260889 | — | Inhibition | - | % | - | |
| CHEMBL3260890 | — | Inhibition | - | % | - | |
| CHEMBL3221242 | — | Inhibition | - | % | - | |
| CHEMBL3260891 | — | Inhibition | - | % | - | |
| CHEMBL3221243 | — | Inhibition | - | % | - | |
| CHEMBL3221244 | — | Inhibition | - | % | - | |
| CHEMBL3221245 | — | Inhibition | - | % | - | |
| CHEMBL3260892 | — | Inhibition | - | % | - | |
| CHEMBL3260893 | — | Inhibition | - | % | - | |
| CHEMBL3260894 | — | Inhibition | - | % | - | |
| CHEMBL3260895 | — | Inhibition | - | % | - | |
| CHEMBL3260896 | — | Inhibition | - | % | - | |
| CHEMBL3221246 | — | Inhibition | - | % | - | |
| CHEMBL3261115 | — | Inhibition | - | % | - | |
| CHEMBL3221247 | — | Inhibition | - | % | - | |
| CHEMBL1164407 | — | Inhibition | - | % | - | |
| CHEMBL1164066 | — | Inhibition | - | % | - | |
| CHEMBL193 | NIFEDIPINE | Inhibition | - | % | - |