Assay Detail
Binding
CHEMBL660040
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Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Muscle tissue |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL2830) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.87 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 9.00 |
| CHEMBL1202818 | — | — | 1 | 6.70 |
| CHEMBL1202819 | — | — | 1 | 6.30 |
| CHEMBL1204266 | — | — | 1 | 6.22 |
| CHEMBL1202823 | — | — | 1 | 6.22 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.00 |
| CHEMBL1202820 | — | — | 1 | 5.96 |
| CHEMBL1202825 | — | — | 1 | 5.89 |
| CHEMBL1202826 | — | — | 1 | 5.82 |
| CHEMBL1202814 | — | — | 1 | 5.80 |
| CHEMBL1204277 | — | — | 1 | 5.60 |
| CHEMBL1204272 | — | — | 1 | 5.57 |
| CHEMBL1202815 | — | — | 1 | 5.52 |
| CHEMBL1202824 | — | — | 1 | 5.51 |
| CHEMBL1202821 | — | — | 1 | 5.22 |
| CHEMBL1204265 | — | — | 1 | 5.22 |
| CHEMBL1202807 | — | — | 1 | 5.21 |
| CHEMBL1202813 | — | — | 1 | 5.16 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 4.66 |
| CHEMBL1202817 | — | — | 1 | - |
| CHEMBL79 | LIDOCAINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1202818 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1202819 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1204266 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1202823 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1202820 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1202825 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1202826 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1202814 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1204277 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1204272 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1202815 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1202824 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1202821 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1204265 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1202807 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL1202813 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1008 | BEPRIDIL | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1202817 | — | IC50 | = | - | nM | - |
| CHEMBL79 | LIDOCAINE | IC50 | > | 1000000.0 | nM | - |