Assay Detail
Binding
CHEMBL977365
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of voltage-dependent L-type calcium channel in rat thoracic aorta ring assessed as effect on high K+ induced contraction by Magnus method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Thoracic 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
The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.29 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452076 | CILNIDIPINE | 3.0 | 1 | 8.96 |
| CHEMBL453084 | — | — | 1 | 8.15 |
| CHEMBL382072 | — | — | 1 | 7.70 |
| CHEMBL508181 | — | — | 1 | 7.34 |
| CHEMBL451817 | — | — | 1 | 6.27 |
| CHEMBL511062 | — | — | 1 | 6.16 |
| CHEMBL453088 | — | — | 1 | 6.00 |
| CHEMBL451813 | — | — | 1 | 5.89 |
| CHEMBL453604 | — | — | 1 | 5.85 |
| CHEMBL370409 | — | — | 1 | 5.75 |
| CHEMBL453605 | — | — | 1 | 5.70 |
| CHEMBL451811 | — | — | 1 | 5.70 |
| CHEMBL452072 | — | — | 1 | 5.50 |
| CHEMBL452073 | — | — | 1 | 5.36 |
| CHEMBL508180 | — | — | 1 | 5.23 |
| CHEMBL451812 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452076 | CILNIDIPINE | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL453084 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL382072 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL508181 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL451817 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL511062 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL453088 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL451813 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL453604 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL370409 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL453605 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL451811 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL452072 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL452073 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL508180 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL451812 | — | IC50 | = | 8100.0 | nM | 5.09 |