Assay Detail
Binding
CHEMBL808202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]pentazocine binding to Sigma receptor type 1 in guinea pig brain membrane without cerebellum
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| 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 of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.78 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555790 | — | — | 1 | 9.47 |
| CHEMBL543821 | — | — | 1 | 9.07 |
| CHEMBL418484 | — | — | 1 | 9.07 |
| CHEMBL539776 | — | — | 1 | 8.96 |
| CHEMBL542873 | — | — | 1 | 8.93 |
| CHEMBL555090 | — | — | 1 | 8.85 |
| CHEMBL543105 | — | — | 1 | 8.77 |
| CHEMBL540289 | — | — | 1 | 8.75 |
| CHEMBL542392 | — | — | 1 | 8.74 |
| CHEMBL543581 | — | — | 1 | 8.74 |
| CHEMBL545691 | — | — | 1 | 8.66 |
| CHEMBL544992 | — | — | 1 | 8.60 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.57 |
| CHEMBL544524 | — | — | 1 | 8.57 |
| CHEMBL545451 | — | — | 1 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555790 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL543821 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL418484 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL539776 | — | Ki | = | 1.09 | nM | 8.96 |
| CHEMBL542873 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL555090 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL543105 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL540289 | — | Ki | = | 1.78 | nM | 8.75 |
| CHEMBL542392 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL543581 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL545691 | — | Ki | = | 2.21 | nM | 8.66 |
| CHEMBL544992 | — | Ki | = | 2.51 | nM | 8.60 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL544524 | — | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL545451 | — | Ki | = | 12.6 | nM | 7.90 |