Assay Detail
Binding
CHEMBL1000140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane without cerebellum
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.08 | 8.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190883 | — | — | 1 | 8.99 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 8.70 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.62 |
| CHEMBL486136 | — | — | 1 | 8.54 |
| CHEMBL511680 | — | — | 1 | 8.20 |
| CHEMBL487359 | — | — | 1 | 8.11 |
| CHEMBL53325 | — | — | 1 | 7.87 |
| CHEMBL511857 | — | — | 1 | 7.61 |
| CHEMBL457508 | — | — | 1 | 7.51 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL456437 | — | — | 1 | 6.98 |
| CHEMBL521350 | — | — | 1 | 6.75 |
| CHEMBL457731 | — | — | 1 | 6.75 |
| CHEMBL457720 | — | — | 1 | 6.72 |
| CHEMBL457721 | — | — | 1 | 6.72 |
| CHEMBL485929 | — | — | 1 | 6.71 |
| CHEMBL513936 | — | — | 1 | 6.67 |
| CHEMBL140287 | — | — | 1 | 6.66 |
| CHEMBL487360 | — | — | 1 | 6.62 |
| CHEMBL458361 | — | — | 1 | 6.54 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 6.51 |
| CHEMBL138900 | — | — | 1 | 6.45 |
| CHEMBL485729 | — | — | 1 | 6.43 |
| CHEMBL458553 | — | — | 1 | 6.10 |
| CHEMBL456435 | — | — | 1 | 6.00 |
| CHEMBL458802 | — | — | 1 | 5.96 |
| CHEMBL511507 | — | — | 1 | 5.29 |
| CHEMBL457722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190883 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 2.41 | nM | 8.62 |
| CHEMBL486136 | — | Ki | = | 2.86 | nM | 8.54 |
| CHEMBL511680 | — | Ki | = | 6.32 | nM | 8.20 |
| CHEMBL487359 | — | Ki | = | 7.71 | nM | 8.11 |
| CHEMBL53325 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL511857 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL457508 | — | Ki | = | 30.7 | nM | 7.51 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 88.5 | nM | 7.05 |
| CHEMBL456437 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL521350 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL457731 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL457720 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL457721 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL485929 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL513936 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL140287 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL487360 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL458361 | — | Ki | = | 291.0 | nM | 6.54 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL138900 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL485729 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL458553 | — | Ki | = | 802.0 | nM | 6.10 |
| CHEMBL456435 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL458802 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL511507 | — | Ki | = | 5170.0 | nM | 5.29 |
| CHEMBL457722 | — | Ki | > | 6000.0 | nM | - |