Assay Detail
Functional
CHEMBL948245
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at L-type calcium channel in rat aorta
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.17 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL257288 | — | — | 3 | 5.68 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 5.16 |
| CHEMBL403689 | — | — | 1 | 4.92 |
| CHEMBL269980 | — | — | 1 | 4.92 |
| CHEMBL272128 | — | — | 1 | 4.82 |
| CHEMBL272127 | — | — | 1 | 4.77 |
| CHEMBL402197 | — | — | 1 | - |
| CHEMBL404329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL257288 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL257288 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL257288 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL403689 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL269980 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL272128 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL272127 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL402197 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL404329 | — | IC50 | > | 30000.0 | nM | - |