Assay Detail
Binding
CHEMBL4733429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method
16
Total Activities
16
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, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σR/TMEM97 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.47 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744466 | — | — | 1 | 9.42 |
| CHEMBL4746910 | — | — | 1 | 8.88 |
| CHEMBL4739972 | — | — | 1 | 8.52 |
| CHEMBL4778377 | — | — | 1 | 8.29 |
| CHEMBL4744206 | — | — | 1 | 7.90 |
| CHEMBL4760742 | — | — | 1 | 7.71 |
| CHEMBL4747537 | — | — | 1 | 7.65 |
| CHEMBL4796195 | — | — | 1 | 7.47 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.45 |
| CHEMBL4761905 | — | — | 1 | 7.40 |
| CHEMBL4763056 | — | — | 1 | 7.38 |
| CHEMBL4778965 | — | — | 1 | 6.02 |
| CHEMBL4749663 | — | — | 1 | 5.50 |
| CHEMBL4759158 | — | — | 1 | 4.94 |
| CHEMBL4740343 | — | — | 1 | - |
| CHEMBL4765186 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744466 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL4746910 | — | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL4739972 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4778377 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL4744206 | — | Ki | = | 12.58 | nM | 7.90 |
| CHEMBL4760742 | — | Ki | = | 19.67 | nM | 7.71 |
| CHEMBL4747537 | — | Ki | = | 22.37 | nM | 7.65 |
| CHEMBL4796195 | — | Ki | = | 34.22 | nM | 7.47 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 35.22 | nM | 7.45 |
| CHEMBL4761905 | — | Ki | = | 40.04 | nM | 7.40 |
| CHEMBL4763056 | — | Ki | = | 41.76 | nM | 7.38 |
| CHEMBL4778965 | — | Ki | = | 956.0 | nM | 6.02 |
| CHEMBL4749663 | — | Ki | = | 3184.0 | nM | 5.50 |
| CHEMBL4759158 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL4740343 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4765186 | — | Ki | > | 1000.0 | nM | - |