Assay Detail
Binding
CHEMBL700074
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Inhibition of [3H](+)-PN200-110 binding to L-type calcium channel 1,4-DHP binding site of rat ventricular myocytes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Ventricular myocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL3762) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.46 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3350845 | — | — | 1 | 8.67 |
| CHEMBL3350842 | — | — | 1 | 8.62 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.46 |
| CHEMBL3350846 | — | — | 1 | 7.87 |
| CHEMBL3350843 | — | — | 1 | 7.80 |
| CHEMBL3350844 | — | — | 1 | 7.78 |
| CHEMBL122740 | — | — | 1 | 7.76 |
| CHEMBL410937 | — | — | 1 | 7.76 |
| CHEMBL125814 | — | — | 1 | 7.20 |
| CHEMBL3350841 | — | — | 1 | 7.06 |
| CHEMBL331446 | — | — | 1 | 6.63 |
| CHEMBL125651 | — | — | 1 | 5.93 |
| CHEMBL122220 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3350845 | — | Ki | = | 2.15 | nM | 8.67 |
| CHEMBL3350842 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3350846 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL3350843 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL3350844 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL122740 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL410937 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL125814 | — | Ki | = | 63.6 | nM | 7.20 |
| CHEMBL3350841 | — | Ki | = | 86.7 | nM | 7.06 |
| CHEMBL331446 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL125651 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL122220 | — | Ki | = | 3320.0 | nM | 5.48 |