Assay Detail
Binding
CHEMBL808283
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Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.29 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.47 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.19 |
| CHEMBL138103 | — | — | 1 | 7.08 |
| CHEMBL138083 | — | — | 1 | 7.00 |
| CHEMBL138560 | — | — | 1 | 6.97 |
| CHEMBL137979 | — | — | 1 | 6.52 |
| CHEMBL138458 | — | — | 1 | 6.51 |
| CHEMBL141278 | — | — | 1 | 6.51 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.41 |
| CHEMBL141743 | — | — | 1 | 6.39 |
| CHEMBL137990 | — | — | 1 | 6.29 |
| CHEMBL138533 | — | — | 1 | 6.12 |
| CHEMBL138286 | — | — | 1 | 5.94 |
| CHEMBL138809 | — | — | 1 | 5.89 |
| CHEMBL343793 | — | — | 1 | 5.84 |
| CHEMBL138102 | — | — | 1 | 5.53 |
| CHEMBL141209 | — | — | 1 | 5.46 |
| CHEMBL138457 | — | — | 1 | 5.40 |
| CHEMBL140030 | — | — | 1 | 5.00 |
| CHEMBL138857 | — | — | 1 | - |
| CHEMBL139455 | — | — | 1 | - |
| CHEMBL138856 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 34.2 | nM | 7.47 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 63.9 | nM | 7.19 |
| CHEMBL138103 | — | Ki | = | 83.1 | nM | 7.08 |
| CHEMBL138083 | — | Ki | = | 99.7 | nM | 7.00 |
| CHEMBL138560 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL137979 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL138458 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL141278 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL60859 | BMY-14802 | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL141743 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL137990 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL138533 | — | Ki | = | 761.0 | nM | 6.12 |
| CHEMBL138286 | — | Ki | = | 1157.0 | nM | 5.94 |
| CHEMBL138809 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL343793 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL138102 | — | Ki | = | 2960.0 | nM | 5.53 |
| CHEMBL141209 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL138457 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL140030 | — | Ki | = | 9890.0 | nM | 5.00 |
| CHEMBL138857 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL139455 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL138856 | — | Ki | > | 10000.0 | nM | - |