Assay Detail
Binding
CHEMBL5123183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma 2 receptor in rat liver membrane measured after 120 mins by microbeta counting analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.74 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187386 | — | — | 1 | 8.23 |
| CHEMBL5175585 | — | — | 1 | 8.22 |
| CHEMBL493054 | — | — | 1 | 8.19 |
| CHEMBL5204491 | — | — | 1 | 8.18 |
| CHEMBL5188049 | — | — | 1 | 8.05 |
| CHEMBL5203681 | — | — | 1 | 8.00 |
| CHEMBL5202363 | — | — | 1 | 8.00 |
| CHEMBL5187130 | — | — | 1 | 8.00 |
| CHEMBL5186790 | — | — | 1 | 7.96 |
| CHEMBL5170944 | — | — | 1 | 7.96 |
| CHEMBL5181463 | — | — | 1 | 7.96 |
| CHEMBL5198365 | — | — | 1 | 7.96 |
| CHEMBL5170135 | — | — | 1 | 7.92 |
| CHEMBL5201372 | — | — | 1 | 7.85 |
| CHEMBL5208719 | — | — | 1 | 7.82 |
| CHEMBL5177115 | — | — | 1 | 7.82 |
| CHEMBL5209286 | — | — | 1 | 7.82 |
| CHEMBL5189302 | — | — | 1 | 7.72 |
| CHEMBL5195784 | — | — | 1 | 7.68 |
| CHEMBL5170176 | — | — | 1 | 7.66 |
| CHEMBL5202239 | — | — | 1 | 7.66 |
| CHEMBL5185741 | — | — | 1 | 7.64 |
| CHEMBL5185838 | — | — | 1 | 7.57 |
| CHEMBL5175714 | — | — | 1 | 7.57 |
| CHEMBL5185178 | — | — | 1 | 7.54 |
| CHEMBL5194969 | — | — | 1 | 7.52 |
| CHEMBL5173021 | — | — | 1 | 7.33 |
| CHEMBL5195175 | — | — | 1 | 7.33 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187386 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL5175585 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL493054 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5204491 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL5188049 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5203681 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5202363 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5187130 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5186790 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5170944 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5181463 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5198365 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5170135 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5201372 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5177115 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5209286 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5208719 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5189302 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5195784 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5170176 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5202239 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5185741 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5175714 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5185838 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5185178 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL5194969 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL5173021 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5195175 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL28564 | ELIPRODIL | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL5205672 | — | Ki | = | 101.0 | nM | 7.00 |