Assay Detail
Binding
CHEMBL654580
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 |
|---|---|---|---|
| Ki | 8 | 7.52 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277363 | — | — | 1 | 9.80 |
| CHEMBL18988 | — | — | 1 | 8.26 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.80 |
| CHEMBL537031 | — | — | 1 | 7.72 |
| CHEMBL275195 | — | — | 1 | 7.25 |
| CHEMBL277293 | — | — | 1 | 6.93 |
| CHEMBL274514 | — | — | 1 | 6.70 |
| CHEMBL18412 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277363 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL18988 | — | Ki | = | 5.55 | nM | 8.26 |
| CHEMBL23 | DILTIAZEM | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL537031 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL275195 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL277293 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL274514 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL18412 | — | Ki | = | 2200.0 | nM | 5.66 |