Assay Detail
Binding
CHEMBL827427
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Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine
31
Total Activities
31
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
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.00 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276784 | — | — | 1 | 9.31 |
| CHEMBL425867 | — | — | 1 | 8.85 |
| CHEMBL362699 | — | — | 1 | 8.83 |
| CHEMBL360351 | — | — | 1 | 8.80 |
| CHEMBL369091 | — | — | 1 | 8.77 |
| CHEMBL180327 | — | — | 1 | 8.60 |
| CHEMBL179648 | — | — | 1 | 8.52 |
| CHEMBL434905 | — | — | 1 | 8.47 |
| CHEMBL178519 | — | — | 1 | 8.47 |
| CHEMBL369133 | — | — | 1 | 8.33 |
| CHEMBL180180 | — | — | 1 | 8.32 |
| CHEMBL178650 | — | — | 1 | 8.32 |
| CHEMBL178988 | — | — | 1 | 8.27 |
| CHEMBL179373 | — | — | 1 | 8.22 |
| CHEMBL179397 | — | — | 1 | 8.10 |
| CHEMBL180119 | — | — | 1 | 8.00 |
| CHEMBL178680 | — | — | 1 | 7.96 |
| CHEMBL179145 | — | — | 1 | 7.91 |
| CHEMBL179651 | — | — | 1 | 7.85 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.80 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.68 |
| CHEMBL359663 | — | — | 1 | 7.59 |
| CHEMBL178700 | — | — | 1 | 7.55 |
| CHEMBL179530 | — | — | 1 | 7.51 |
| CHEMBL178600 | — | — | 1 | 7.48 |
| CHEMBL179808 | — | — | 1 | 7.33 |
| CHEMBL179371 | — | — | 1 | 7.12 |
| CHEMBL179697 | — | — | 1 | 7.05 |
| CHEMBL179062 | — | — | 1 | 6.54 |
| CHEMBL426958 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276784 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL425867 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL362699 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL360351 | — | Ki | = | 1.59 | nM | 8.80 |
| CHEMBL369091 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL180327 | — | Ki | = | 2.52 | nM | 8.60 |
| CHEMBL179648 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL434905 | — | Ki | = | 3.38 | nM | 8.47 |
| CHEMBL178519 | — | Ki | = | 3.38 | nM | 8.47 |
| CHEMBL369133 | — | Ki | = | 4.63 | nM | 8.33 |
| CHEMBL180180 | — | Ki | = | 4.75 | nM | 8.32 |
| CHEMBL178650 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL178988 | — | Ki | = | 5.35 | nM | 8.27 |
| CHEMBL179373 | — | Ki | = | 5.98 | nM | 8.22 |
| CHEMBL179397 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL180119 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL178680 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL179145 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL179651 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL359663 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL178700 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL179530 | — | Ki | = | 30.6 | nM | 7.51 |
| CHEMBL178600 | — | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL179808 | — | Ki | = | 47.3 | nM | 7.33 |
| CHEMBL179371 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL179697 | — | Ki | = | 89.3 | nM | 7.05 |
| CHEMBL179062 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL426958 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL178924 | — | Ki | > | 1000.0 | nM | - |