Assay Detail
Binding
CHEMBL803923
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.14 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134313 | — | — | 1 | 8.87 |
| CHEMBL342223 | — | — | 1 | 8.83 |
| CHEMBL337818 | — | — | 1 | 8.76 |
| CHEMBL20377 | — | — | 1 | 8.68 |
| CHEMBL137348 | — | — | 1 | 8.64 |
| CHEMBL136981 | — | — | 1 | 8.57 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL137794 | — | — | 1 | 8.45 |
| CHEMBL342942 | — | — | 1 | 8.43 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.43 |
| CHEMBL343790 | — | — | 1 | 8.36 |
| CHEMBL106437 | — | — | 1 | 8.11 |
| CHEMBL138123 | — | — | 1 | 7.79 |
| CHEMBL316988 | — | — | 1 | 7.73 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.56 |
| CHEMBL430466 | — | — | 1 | 6.37 |
| CHEMBL102999 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134313 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL342223 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL337818 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL20377 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL137348 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL136981 | — | Ki | = | 2.67 | nM | 8.57 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL137794 | — | Ki | = | 3.56 | nM | 8.45 |
| CHEMBL342942 | — | Ki | = | 3.69 | nM | 8.43 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL343790 | — | Ki | = | 4.34 | nM | 8.36 |
| CHEMBL106437 | — | Ki | = | 7.78 | nM | 8.11 |
| CHEMBL138123 | — | Ki | = | 16.05 | nM | 7.79 |
| CHEMBL316988 | — | Ki | = | 18.68 | nM | 7.73 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 27.7 | nM | 7.56 |
| CHEMBL430466 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL102999 | — | Ki | = | 455.0 | nM | 6.34 |