Assay Detail
Binding
CHEMBL805221
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Affinity at sigma-2 site by inhibition of [3H]1,3-di(2-tolyl)guanidine (DTG) binding in guinea pig brain.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 6.88 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 6.25 |
| CHEMBL61946 | CARAMIPHEN | 2.0 | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL61946 | CARAMIPHEN | Ki | = | 658.0 | nM | 6.18 |