Assay Detail
Binding
CHEMBL704173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]nitrendipine binding at L-type [Ca2+] channel in rat cortex homogenate by 50%.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 35 | 6.83 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277363 | — | — | 1 | 9.38 |
| CHEMBL139748 | — | — | 1 | 9.11 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 8.43 |
| CHEMBL139134 | — | — | 1 | 8.36 |
| CHEMBL136300 | — | — | 1 | 7.92 |
| CHEMBL136432 | — | — | 1 | 7.82 |
| CHEMBL282348 | — | — | 1 | 7.52 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.34 |
| CHEMBL24675 | — | — | 1 | 7.28 |
| CHEMBL282651 | — | — | 1 | 7.19 |
| CHEMBL24086 | — | — | 1 | 7.09 |
| CHEMBL26172 | — | — | 1 | 6.97 |
| CHEMBL275195 | — | — | 1 | 6.82 |
| CHEMBL282989 | — | — | 1 | 6.70 |
| CHEMBL24085 | — | — | 1 | 6.66 |
| CHEMBL277293 | — | — | 1 | 6.50 |
| CHEMBL278171 | — | — | 1 | 6.50 |
| CHEMBL26495 | — | — | 1 | 6.33 |
| CHEMBL274514 | — | — | 1 | 6.27 |
| CHEMBL287054 | — | — | 1 | 6.11 |
| CHEMBL281762 | — | — | 1 | 5.91 |
| CHEMBL282854 | — | — | 1 | 5.81 |
| CHEMBL280391 | — | — | 1 | 5.80 |
| CHEMBL24243 | — | — | 1 | 5.69 |
| CHEMBL136456 | — | — | 1 | 5.67 |
| CHEMBL26442 | — | — | 1 | 5.36 |
| CHEMBL26605 | — | — | 1 | 5.33 |
| CHEMBL138215 | — | — | 1 | 5.33 |
| CHEMBL24620 | — | — | 1 | - |
| CHEMBL26239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277363 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL139748 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL139134 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL136300 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL136432 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL282348 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL24675 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL282651 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL24086 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL26172 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL275195 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL282989 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL24085 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL277293 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL278171 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL26495 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL274514 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL287054 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL281762 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL282854 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL280391 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL24243 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL136456 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL26442 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL26605 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL138215 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL24620 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL26239 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL137363 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL139477 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL344604 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL136673 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL18412 | — | IC50 | > | 5000.0 | nM | - |