Assay Detail
Binding
CHEMBL880938
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [3H](+)-pentazocine binding to guinea pig brain Sigma receptor type 1
26
Total Activities
12
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
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.75 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL110319 | — | — | 3 | 8.89 |
| CHEMBL356639 | — | — | 1 | 8.79 |
| CHEMBL145422 | — | — | 1 | 8.77 |
| CHEMBL143800 | — | — | 3 | 8.72 |
| CHEMBL146659 | — | — | 3 | 8.51 |
| CHEMBL322468 | — | — | 3 | 8.49 |
| CHEMBL145296 | — | — | 3 | 8.24 |
| CHEMBL145780 | — | — | 1 | 7.78 |
| CHEMBL141381 | — | — | 3 | 7.74 |
| CHEMBL358527 | — | — | 1 | 7.21 |
| CHEMBL109124 | — | — | 2 | 6.86 |
| CHEMBL38791 | — | — | 2 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL110319 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL356639 | — | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL145422 | — | Ki | = | 1.71 | nM | 8.77 |
| CHEMBL143800 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL146659 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL322468 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL145296 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL145296 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL143800 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL145296 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL110319 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL145780 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL143800 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL141381 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL110319 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL146659 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL322468 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL141381 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL146659 | — | Ki | = | 51.3 | nM | 7.29 |
| CHEMBL358527 | — | Ki | = | 62.3 | nM | 7.21 |
| CHEMBL322468 | — | Ki | = | 65.3 | nM | 7.18 |
| CHEMBL109124 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL109124 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL141381 | — | Ki | = | 759.3 | nM | 6.12 |
| CHEMBL38791 | — | Ki | = | 762.0 | nM | 6.12 |
| CHEMBL38791 | — | Ki | = | 31.8 | nM | - |