Assay Detail
Binding
CHEMBL654578
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nitrendipine from calcium channel receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and preliminary biological evaluation of 1-aminomethyl-4-substituted-4-H-pyrrolo[2,1-C][1,4] benzothiazines, a new class of calcium antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.09 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277363 | — | — | 1 | 9.38 |
| CHEMBL18988 | — | — | 1 | 7.83 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.38 |
| CHEMBL537031 | — | — | 1 | 7.28 |
| CHEMBL275195 | — | — | 1 | 6.82 |
| CHEMBL277293 | — | — | 1 | 6.50 |
| CHEMBL274514 | — | — | 1 | 6.27 |
| CHEMBL18412 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277363 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL18988 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL537031 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL275195 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL277293 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL274514 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL18412 | — | IC50 | = | 5870.0 | nM | 5.23 |