Assay Detail
Binding
CHEMBL809836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand.
23
Total Activities
23
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
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.67 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138083 | — | — | 1 | 9.16 |
| CHEMBL138809 | — | — | 1 | 8.94 |
| CHEMBL141209 | — | — | 1 | 8.89 |
| CHEMBL137979 | — | — | 1 | 8.73 |
| CHEMBL138458 | — | — | 1 | 8.68 |
| CHEMBL137990 | — | — | 1 | 8.66 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.45 |
| CHEMBL138102 | — | — | 1 | 8.23 |
| CHEMBL141743 | — | — | 1 | 8.18 |
| CHEMBL138533 | — | — | 1 | 8.13 |
| CHEMBL141278 | — | — | 1 | 7.99 |
| CHEMBL138103 | — | — | 1 | 7.91 |
| CHEMBL138457 | — | — | 1 | 7.88 |
| CHEMBL343793 | — | — | 1 | 7.67 |
| CHEMBL138286 | — | — | 1 | 7.53 |
| CHEMBL138560 | — | — | 1 | 7.36 |
| CHEMBL140030 | — | — | 1 | 7.02 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.79 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.58 |
| CHEMBL138856 | — | — | 1 | 5.36 |
| CHEMBL138857 | — | — | 1 | 5.00 |
| CHEMBL139455 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138083 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL138809 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL141209 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL137979 | — | Ki | = | 1.87 | nM | 8.73 |
| CHEMBL138458 | — | Ki | = | 2.07 | nM | 8.68 |
| CHEMBL137990 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.58 | nM | 8.45 |
| CHEMBL138102 | — | Ki | = | 5.83 | nM | 8.23 |
| CHEMBL141743 | — | Ki | = | 6.64 | nM | 8.18 |
| CHEMBL138533 | — | Ki | = | 7.33 | nM | 8.13 |
| CHEMBL141278 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL138103 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL138457 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL343793 | — | Ki | = | 21.3 | nM | 7.67 |
| CHEMBL138286 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL138560 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL140030 | — | Ki | = | 95.3 | nM | 7.02 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL60859 | BMY-14802 | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL138856 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL138857 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL139455 | — | Ki | = | 19800.0 | nM | 4.70 |