Assay Detail
Binding
CHEMBL656597
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration 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 |
|---|---|---|---|
| IC50 | 22 | 6.66 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25676 | — | — | 1 | 8.59 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.57 |
| CHEMBL150872 | — | — | 1 | 8.00 |
| CHEMBL149907 | — | — | 1 | 7.57 |
| CHEMBL150618 | — | — | 1 | 7.40 |
| CHEMBL150486 | — | — | 1 | 7.23 |
| CHEMBL433514 | — | — | 1 | 7.17 |
| CHEMBL346151 | — | — | 1 | 7.14 |
| CHEMBL358157 | — | — | 1 | 7.07 |
| CHEMBL151447 | — | — | 1 | 6.30 |
| CHEMBL150802 | — | — | 1 | 6.30 |
| CHEMBL150632 | — | — | 1 | 6.23 |
| CHEMBL150319 | — | — | 1 | 6.21 |
| CHEMBL150921 | — | — | 1 | 6.14 |
| CHEMBL151643 | — | — | 1 | 6.11 |
| CHEMBL348676 | — | — | 1 | 6.09 |
| CHEMBL150433 | — | — | 1 | 6.06 |
| CHEMBL150851 | — | — | 1 | 6.01 |
| CHEMBL150469 | — | — | 1 | 5.82 |
| CHEMBL151759 | — | — | 1 | 5.70 |
| CHEMBL345530 | — | — | 1 | 5.44 |
| CHEMBL151273 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25676 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL150872 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL149907 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL150618 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL150486 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL433514 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL346151 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL358157 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL151447 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL150802 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL150632 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL150319 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL150921 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL151643 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL348676 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL150433 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL150851 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL150469 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL151759 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL345530 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL151273 | — | IC50 | = | 5100.0 | nM | 5.29 |