Assay Detail
Binding
CHEMBL1111777
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Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane homogenates after 90 mins by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.73 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1204035 | — | — | 1 | 8.03 |
| CHEMBL1204032 | — | — | 1 | 7.80 |
| CHEMBL1204048 | — | — | 1 | 7.70 |
| CHEMBL20730 | VESAMICOL | — | 1 | 7.59 |
| CHEMBL1204034 | — | — | 1 | 7.53 |
| CHEMBL1204047 | — | — | 1 | 7.30 |
| CHEMBL1204049 | — | — | 1 | 6.93 |
| CHEMBL1204037 | — | — | 1 | 6.89 |
| CHEMBL1204038 | — | — | 1 | 6.71 |
| CHEMBL1204030 | — | — | 1 | 6.55 |
| CHEMBL1204031 | — | — | 1 | 6.52 |
| CHEMBL1204040 | — | — | 1 | 6.40 |
| CHEMBL1204045 | — | — | 1 | 6.32 |
| CHEMBL1204043 | — | — | 1 | 6.30 |
| CHEMBL1204050 | — | — | 1 | 6.00 |
| CHEMBL1204046 | — | — | 1 | 6.00 |
| CHEMBL1204044 | — | — | 1 | 6.00 |
| CHEMBL1204042 | — | — | 1 | 6.00 |
| CHEMBL1204041 | — | — | 1 | 6.00 |
| CHEMBL1204039 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1204035 | — | Ki | = | 9.39 | nM | 8.03 |
| CHEMBL1204032 | — | Ki | = | 15.91 | nM | 7.80 |
| CHEMBL1204048 | — | Ki | = | 19.88 | nM | 7.70 |
| CHEMBL20730 | VESAMICOL | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL1204034 | — | Ki | = | 29.46 | nM | 7.53 |
| CHEMBL1204047 | — | Ki | = | 50.24 | nM | 7.30 |
| CHEMBL1204049 | — | Ki | = | 118.12 | nM | 6.93 |
| CHEMBL1204037 | — | Ki | = | 128.92 | nM | 6.89 |
| CHEMBL1204038 | — | Ki | = | 194.03 | nM | 6.71 |
| CHEMBL1204030 | — | Ki | = | 280.8 | nM | 6.55 |
| CHEMBL1204031 | — | Ki | = | 302.79 | nM | 6.52 |
| CHEMBL1204040 | — | Ki | = | 395.11 | nM | 6.40 |
| CHEMBL1204045 | — | Ki | = | 483.24 | nM | 6.32 |
| CHEMBL1204043 | — | Ki | = | 497.1 | nM | 6.30 |
| CHEMBL1204050 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1204046 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1204044 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1204042 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1204041 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1204039 | — | Ki | = | 1000.0 | nM | 6.00 |