Assay Detail
Binding
CHEMBL660031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diltiazem from L-type calcium channel of guinea pig striated muscle
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Muscle tissue |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1S (CHEMBL3805) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
(cis)-3-methyl-1,5-benzothiazepine-4-ones: potent analogs of the calcium channel blocker diltiazen
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.67 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319525 | — | — | 1 | 7.38 |
| CHEMBL96454 | — | — | 1 | 7.07 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 6.42 |
| CHEMBL262509 | — | — | 1 | 6.27 |
| CHEMBL98189 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319525 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL96454 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL23 | DILTIAZEM | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL262509 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL98189 | — | Ki | = | 650.0 | nM | 6.19 |