Assay Detail
Functional
CHEMBL703975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Calcium antagonistic activity by measuring [3H]nitrendipine displacement from rat heart L-type [Ca2+] channel
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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
Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.13 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24675 | — | — | 1 | 8.08 |
| CHEMBL24086 | — | — | 1 | 7.58 |
| CHEMBL139134 | — | — | 1 | 7.46 |
| CHEMBL277363 | — | — | 1 | 7.28 |
| CHEMBL275195 | — | — | 1 | 6.80 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 6.55 |
| CHEMBL136432 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24675 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL24086 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL139134 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL277363 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL275195 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL23 | DILTIAZEM | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL136432 | — | Ki | = | 640.0 | nM | 6.19 |