Assay Detail
Functional
CHEMBL703969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Calcium antagonistic activity by measuring [3H]nitrendipine displacement at L-type [Ca2+] channel in rat cortex homogenate
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| 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 | 17 | 7.16 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139748 | — | — | 1 | 9.54 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 8.85 |
| CHEMBL139134 | — | — | 1 | 8.70 |
| CHEMBL282348 | — | — | 1 | 7.96 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.68 |
| CHEMBL282651 | — | — | 1 | 7.62 |
| CHEMBL24086 | — | — | 1 | 7.51 |
| CHEMBL26172 | — | — | 1 | 7.40 |
| CHEMBL24085 | — | — | 1 | 7.09 |
| CHEMBL278171 | — | — | 1 | 6.92 |
| CHEMBL26495 | — | — | 1 | 6.75 |
| CHEMBL282854 | — | — | 1 | 6.24 |
| CHEMBL24243 | — | — | 1 | 6.11 |
| CHEMBL136456 | — | — | 1 | 6.09 |
| CHEMBL26442 | — | — | 1 | 5.79 |
| CHEMBL138215 | — | — | 1 | 5.76 |
| CHEMBL26605 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139748 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL6966 | VERAPAMIL | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL139134 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL282348 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL23 | DILTIAZEM | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL282651 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL24086 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL26172 | — | Ki | = | 40.1 | nM | 7.40 |
| CHEMBL24085 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL278171 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL26495 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL282854 | — | Ki | = | 581.0 | nM | 6.24 |
| CHEMBL24243 | — | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL136456 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL26442 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL138215 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL26605 | — | Ki | = | 1830.0 | nM | 5.74 |