Assay Detail
Binding
CHEMBL656598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1D (CHEMBL4132) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.99 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25676 | — | — | 1 | 8.92 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.92 |
| CHEMBL150872 | — | — | 1 | 8.33 |
| CHEMBL150618 | — | — | 1 | 7.75 |
| CHEMBL149907 | — | — | 1 | 7.68 |
| CHEMBL150486 | — | — | 1 | 7.57 |
| CHEMBL433514 | — | — | 1 | 7.52 |
| CHEMBL346151 | — | — | 1 | 7.50 |
| CHEMBL358157 | — | — | 1 | 7.42 |
| CHEMBL150802 | — | — | 1 | 6.66 |
| CHEMBL151447 | — | — | 1 | 6.64 |
| CHEMBL150632 | — | — | 1 | 6.57 |
| CHEMBL150319 | — | — | 1 | 6.55 |
| CHEMBL150921 | — | — | 1 | 6.50 |
| CHEMBL151643 | — | — | 1 | 6.46 |
| CHEMBL348676 | — | — | 1 | 6.43 |
| CHEMBL150433 | — | — | 1 | 6.40 |
| CHEMBL150851 | — | — | 1 | 6.36 |
| CHEMBL150469 | — | — | 1 | 6.17 |
| CHEMBL151759 | — | — | 1 | 6.04 |
| CHEMBL345530 | — | — | 1 | 5.80 |
| CHEMBL151273 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25676 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL150872 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL150618 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL149907 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL150486 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL433514 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL346151 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL358157 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL150802 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL151447 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL150632 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL150319 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL150921 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL151643 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL348676 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL150433 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL150851 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL150469 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL151759 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL345530 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL151273 | — | Ki | = | 2300.0 | nM | 5.64 |