Assay Detail
Binding
CHEMBL803934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Sigma receptor binding was determined by labeling with radioligand [3H](+)-pentazocine on frozen membranes obtained from frozen guinea pig brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.35 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26320 | — | — | 1 | 7.77 |
| CHEMBL163980 | — | — | 1 | 7.42 |
| CHEMBL159320 | — | — | 1 | 7.39 |
| CHEMBL159967 | — | — | 1 | 7.37 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.37 |
| CHEMBL286991 | — | — | 1 | 7.29 |
| CHEMBL164037 | — | — | 1 | 7.23 |
| CHEMBL159319 | — | — | 1 | 7.21 |
| CHEMBL159608 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26320 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL163980 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL159320 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL159967 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL286991 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL164037 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL159319 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL159608 | — | IC50 | = | 79.0 | nM | 7.10 |