Assay Detail
Binding
CHEMBL1104726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ditolylguanidine from sigma2 receptor in rat liver membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.08 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.38 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL1095183 | — | — | 1 | 6.21 |
| CHEMBL1095520 | — | — | 1 | 6.06 |
| CHEMBL1094860 | — | — | 1 | 5.96 |
| CHEMBL1096475 | — | — | 1 | 5.82 |
| CHEMBL1096473 | — | — | 1 | 5.77 |
| CHEMBL1095184 | — | — | 1 | 5.68 |
| CHEMBL1095521 | — | — | 1 | 5.50 |
| CHEMBL1096474 | — | — | 1 | 5.29 |
| CHEMBL1094237 | — | — | 1 | - |
| CHEMBL1094236 | — | — | 1 | - |
| CHEMBL1094880 | — | — | 1 | - |
| CHEMBL1096675 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL1095183 | — | Ki | = | 624.0 | nM | 6.21 |
| CHEMBL1095520 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL1094860 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1096475 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1096473 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL1095184 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1095521 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL1096474 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL1094237 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094236 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094880 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096675 | — | Ki | > | 1000.0 | nM | - |