Assay Detail
Binding
CHEMBL876248
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Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Heart |
| 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
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.97 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100709 | — | — | 1 | 7.92 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 7.41 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.27 |
| CHEMBL33609 | — | — | 1 | 6.82 |
| CHEMBL33083 | — | — | 1 | 6.66 |
| CHEMBL33165 | — | — | 1 | 6.47 |
| CHEMBL416040 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100709 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL33609 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL33083 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL33165 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL416040 | — | IC50 | = | 610.0 | nM | 6.21 |