Assay Detail
Functional
CHEMBL660041
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Calcium channel blocking activity in rabbit
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.98 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 9.00 |
| CHEMBL346747 | — | — | 1 | 6.52 |
| CHEMBL160865 | — | — | 1 | 6.40 |
| CHEMBL160470 | — | — | 1 | 6.30 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 6.00 |
| CHEMBL345843 | — | — | 1 | 5.96 |
| CHEMBL158853 | — | — | 1 | 5.92 |
| CHEMBL160440 | — | — | 1 | 5.80 |
| CHEMBL156971 | — | — | 1 | 5.77 |
| CHEMBL422696 | — | — | 1 | 5.52 |
| CHEMBL351149 | — | — | 1 | 5.00 |
| CHEMBL158103 | — | — | 1 | 4.92 |
| CHEMBL158550 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL346747 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL160865 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL160470 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL345843 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL158853 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL160440 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL156971 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL422696 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL351149 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL158103 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL158550 | — | IC50 | = | 22000.0 | nM | 4.66 |