Assay Detail
Functional
CHEMBL703971
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Calcium antagonistic activity by measuring [3H]nitrendipine displacement at calcium channel in rat cortex homogenate
11
Total Activities
11
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 | 11 | 7.38 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277363 | — | — | 1 | 9.80 |
| CHEMBL136300 | — | — | 1 | 8.36 |
| CHEMBL136432 | — | — | 1 | 8.26 |
| CHEMBL24675 | — | — | 1 | 7.72 |
| CHEMBL275195 | — | — | 1 | 7.25 |
| CHEMBL282989 | — | — | 1 | 7.13 |
| CHEMBL277293 | — | — | 1 | 6.93 |
| CHEMBL274514 | — | — | 1 | 6.70 |
| CHEMBL287054 | — | — | 1 | 6.54 |
| CHEMBL281762 | — | — | 1 | 6.34 |
| CHEMBL280391 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277363 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL136300 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL136432 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL24675 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL275195 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL282989 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL277293 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL274514 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL287054 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL281762 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL280391 | — | Ki | = | 740.0 | nM | 6.13 |