Assay Detail
Binding
CHEMBL801235
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was evaluated for affinity at sigma-1 site by inhibition of [3H](+)-pentazocine (PENT) 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 | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.49 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.68 |
| CHEMBL61946 | CARAMIPHEN | 2.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL61946 | CARAMIPHEN | Ki | = | 26.0 | nM | 7.58 |