Assay Detail
Binding
CHEMBL1000141
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma 2-type opioid receptor in rat liver membrane in presence of (+)-pentazocine
25
Total Activities
25
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
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 | 25 | 7.15 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53325 | — | — | 1 | 9.47 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 8.64 |
| CHEMBL511857 | — | — | 1 | 7.66 |
| CHEMBL513936 | — | — | 1 | 7.60 |
| CHEMBL456437 | — | — | 1 | 7.57 |
| CHEMBL457720 | — | — | 1 | 7.54 |
| CHEMBL457508 | — | — | 1 | 7.53 |
| CHEMBL486136 | — | — | 1 | 7.52 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.51 |
| CHEMBL521350 | — | — | 1 | 7.44 |
| CHEMBL511680 | — | — | 1 | 7.22 |
| CHEMBL458553 | — | — | 1 | 7.21 |
| CHEMBL485929 | — | — | 1 | 7.20 |
| CHEMBL456435 | — | — | 1 | 7.15 |
| CHEMBL457731 | — | — | 1 | 6.95 |
| CHEMBL457721 | — | — | 1 | 6.86 |
| CHEMBL458802 | — | — | 1 | 6.82 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 6.71 |
| CHEMBL190883 | — | — | 1 | 6.67 |
| CHEMBL458361 | — | — | 1 | 6.65 |
| CHEMBL485729 | — | — | 1 | 6.62 |
| CHEMBL511507 | — | — | 1 | 6.36 |
| CHEMBL457722 | — | — | 1 | 6.16 |
| CHEMBL138900 | — | — | 1 | 5.90 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53325 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL511857 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL513936 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL456437 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL457720 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL457508 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL486136 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL521350 | — | Ki | = | 36.1 | nM | 7.44 |
| CHEMBL511680 | — | Ki | = | 60.2 | nM | 7.22 |
| CHEMBL458553 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL485929 | — | Ki | = | 63.8 | nM | 7.20 |
| CHEMBL456435 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL457731 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL457721 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL458802 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL190883 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL458361 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL485729 | — | Ki | = | 242.0 | nM | 6.62 |
| CHEMBL511507 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL457722 | — | Ki | = | 687.0 | nM | 6.16 |
| CHEMBL138900 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 1860.0 | nM | 5.73 |