Assay Detail
Binding
CHEMBL809834
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity against Sigma opioid receptor type 1 using [3H](+)-pentazocine in guinea pig brain membranes
18
Total Activities
18
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
Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.86 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143103 | — | — | 1 | 9.17 |
| CHEMBL140618 | — | — | 1 | 9.02 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL139900 | — | — | 1 | 8.47 |
| CHEMBL143585 | — | — | 1 | 8.24 |
| CHEMBL143660 | — | — | 1 | 7.93 |
| CHEMBL346665 | — | — | 1 | 7.92 |
| CHEMBL139774 | — | — | 1 | 7.83 |
| CHEMBL344813 | — | — | 1 | 7.78 |
| CHEMBL423548 | — | — | 1 | 7.76 |
| CHEMBL143050 | — | — | 1 | 7.74 |
| CHEMBL143486 | — | — | 1 | 7.71 |
| CHEMBL341874 | — | — | 1 | 7.57 |
| CHEMBL336235 | — | — | 1 | 7.50 |
| CHEMBL356486 | — | — | 1 | 7.44 |
| CHEMBL141070 | — | — | 1 | 7.08 |
| CHEMBL560 | — | — | 1 | 7.08 |
| CHEMBL435046 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143103 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL140618 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL139900 | — | Ki | = | 3.36 | nM | 8.47 |
| CHEMBL143585 | — | Ki | = | 5.74 | nM | 8.24 |
| CHEMBL143660 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL346665 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL139774 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL344813 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL423548 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL143050 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL143486 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL341874 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL336235 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL356486 | — | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL141070 | — | Ki | = | 82.9 | nM | 7.08 |
| CHEMBL560 | — | Ki | = | 83.1 | nM | 7.08 |
| CHEMBL435046 | — | Ki | = | 167.0 | nM | 6.78 |