Assay Detail
Binding
CHEMBL809879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H](+)-pentazocine binding to sigma receptor of guinea pig brain
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.30 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111684 | — | — | 1 | 8.03 |
| CHEMBL110319 | — | — | 1 | 7.63 |
| CHEMBL2111685 | — | — | 1 | 7.50 |
| CHEMBL322468 | — | — | 1 | 7.18 |
| CHEMBL109124 | — | — | 1 | 6.86 |
| CHEMBL2111686 | — | — | 1 | 6.12 |
| CHEMBL3350264 | — | — | 1 | 5.89 |
| CHEMBL38791 | — | — | 2 | 5.85 |
| CHEMBL2008608 | — | — | 1 | 5.50 |
| CHEMBL322329 | — | — | 1 | 5.28 |
| CHEMBL109160 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111684 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL110319 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL2111685 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL322468 | — | Ki | = | 65.3 | nM | 7.18 |
| CHEMBL109124 | — | Ki | = | 137.7 | nM | 6.86 |
| CHEMBL2111686 | — | Ki | = | 762.3 | nM | 6.12 |
| CHEMBL3350264 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL38791 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2008608 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL322329 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL109160 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL38791 | — | Ki | = | 31800.0 | nM | 4.50 |