Assay Detail
Binding
CHEMBL1056845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine ((+)-[2S-(2R,6R,11R)]-1,2,3,4,5,6-hexahydro-6,11-dimethyl- 3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocine- 8-ol) from sigma 1 receptor in Dunkin guinea pig brain membrane by radioreceptor binding assay
24
Total Activities
24
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 | Intermediate |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.86 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573234 | — | — | 1 | 9.96 |
| CHEMBL574821 | — | — | 1 | 9.60 |
| CHEMBL576193 | — | — | 1 | 9.17 |
| CHEMBL573932 | — | — | 1 | 8.96 |
| CHEMBL573703 | — | — | 1 | 8.69 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.48 |
| CHEMBL134607 | — | — | 1 | 8.47 |
| CHEMBL573704 | — | — | 1 | 8.45 |
| CHEMBL573695 | — | — | 1 | 8.26 |
| CHEMBL583945 | — | — | 1 | 8.04 |
| CHEMBL575238 | — | — | 1 | 7.21 |
| CHEMBL582875 | — | — | 1 | 7.20 |
| CHEMBL574155 | — | — | 1 | 7.04 |
| CHEMBL583580 | — | — | 1 | 6.84 |
| CHEMBL50079 | — | — | 1 | 6.66 |
| CHEMBL584767 | — | — | 1 | 6.63 |
| CHEMBL574598 | — | — | 1 | 6.47 |
| CHEMBL575262 | — | — | 1 | 5.41 |
| CHEMBL573461 | — | — | 1 | - |
| CHEMBL575253 | — | — | 1 | - |
| CHEMBL574182 | — | — | 1 | - |
| CHEMBL574165 | — | — | 1 | - |
| CHEMBL575239 | — | — | 1 | - |
| CHEMBL573248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573234 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL574821 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL576193 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL573932 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL573703 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.31 | nM | 8.48 |
| CHEMBL134607 | — | Ki | = | 3.38 | nM | 8.47 |
| CHEMBL573704 | — | Ki | = | 3.59 | nM | 8.45 |
| CHEMBL573695 | — | Ki | = | 5.56 | nM | 8.26 |
| CHEMBL583945 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL575238 | — | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL582875 | — | Ki | = | 63.7 | nM | 7.20 |
| CHEMBL574155 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL583580 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL50079 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL584767 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL574598 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL575262 | — | Ki | = | 3910.0 | nM | 5.41 |
| CHEMBL573461 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL575253 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL574182 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL574165 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL575239 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL573248 | — | Ki | > | 5000.0 | nM | - |