Assay Detail
Functional
CHEMBL947231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent T-type calcium channel subunit alpha-1H (CHEMBL1859) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.52 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403689 | — | — | 1 | 6.96 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 6.89 |
| CHEMBL257288 | — | — | 3 | 6.75 |
| CHEMBL269980 | — | — | 1 | 6.75 |
| CHEMBL272128 | — | — | 1 | 6.62 |
| CHEMBL272127 | — | — | 1 | 6.38 |
| CHEMBL402197 | — | — | 1 | 6.27 |
| CHEMBL404329 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403689 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL269980 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL257288 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL272128 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL257288 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL272127 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL402197 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL257288 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL404329 | — | IC50 | = | 1700.0 | nM | 5.77 |