Assay Detail
Binding
CHEMBL4158749
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method
41
Total Activities
41
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, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 41 | 7.07 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 9.92 |
| CHEMBL53325 | — | — | 1 | 9.17 |
| CHEMBL4167670 | — | — | 1 | 8.12 |
| CHEMBL291439 | — | — | 1 | 8.09 |
| CHEMBL4169479 | — | — | 1 | 7.57 |
| CHEMBL4170683 | — | — | 1 | 7.35 |
| CHEMBL4174683 | — | — | 1 | 7.31 |
| CHEMBL4159233 | — | — | 1 | 7.29 |
| CHEMBL4168095 | — | — | 1 | 7.27 |
| CHEMBL4160820 | — | — | 1 | 7.24 |
| CHEMBL4175947 | — | — | 1 | 7.21 |
| CHEMBL4172875 | — | — | 1 | 7.18 |
| CHEMBL4167468 | — | — | 1 | 7.11 |
| CHEMBL4161557 | — | — | 1 | 7.00 |
| CHEMBL4161237 | — | — | 1 | 6.98 |
| CHEMBL4176252 | — | — | 1 | 6.80 |
| CHEMBL4172125 | — | — | 1 | 6.76 |
| CHEMBL4164248 | — | — | 1 | 6.75 |
| CHEMBL4169156 | — | — | 1 | 6.74 |
| CHEMBL4171436 | — | — | 1 | 6.67 |
| CHEMBL4171757 | — | — | 1 | 6.64 |
| CHEMBL4159559 | — | — | 1 | 6.52 |
| CHEMBL4165358 | — | — | 1 | 6.52 |
| CHEMBL4170826 | — | — | 1 | 6.52 |
| CHEMBL4167697 | — | — | 1 | 6.46 |
| CHEMBL4168393 | — | — | 1 | 6.45 |
| CHEMBL4175566 | — | — | 1 | 6.42 |
| CHEMBL4170858 | — | — | 1 | 6.37 |
| CHEMBL4160847 | — | — | 1 | 6.30 |
| CHEMBL4174291 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL53325 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL4167670 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL291439 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL4169479 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4170683 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4174683 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4159233 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4168095 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4160820 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4175947 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4172875 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL4167468 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4161557 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL4161237 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4176252 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL4172125 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL4164248 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL4169156 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL4171436 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL4171757 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL4165358 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL4170826 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL4159559 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL4167697 | — | Ki | = | 343.0 | nM | 6.46 |
| CHEMBL4168393 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4175566 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL4170858 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL4160847 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL4174291 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL4165978 | — | Ki | = | 527.0 | nM | 6.28 |
| CHEMBL4161150 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4169879 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4164220 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4164032 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4166375 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4162917 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4159761 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4162745 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4175973 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4168777 | — | Ki | > | 1000.0 | nM | - |