Assay Detail
Binding
CHEMBL808200
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand
22
Total Activities
22
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
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.74 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313179 | — | — | 1 | 7.96 |
| CHEMBL87841 | — | — | 1 | 7.88 |
| CHEMBL61946 | CARAMIPHEN | 2.0 | 1 | 7.81 |
| CHEMBL73234 | CARBETAPENTANE | 4.0 | 1 | 7.71 |
| CHEMBL84971 | — | — | 1 | 7.53 |
| CHEMBL86830 | — | — | 1 | 7.49 |
| CHEMBL305881 | — | — | 1 | 7.33 |
| CHEMBL330021 | — | — | 1 | 7.18 |
| CHEMBL316244 | — | — | 1 | 7.01 |
| CHEMBL86477 | — | — | 1 | 6.98 |
| CHEMBL433340 | — | — | 1 | 6.91 |
| CHEMBL314433 | — | — | 1 | 6.86 |
| CHEMBL7549 | PRECLAMOL | 2.0 | 1 | 6.63 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.50 |
| CHEMBL314424 | — | — | 1 | 6.43 |
| CHEMBL316444 | — | — | 1 | 6.26 |
| CHEMBL89832 | — | — | 1 | 6.22 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.04 |
| CHEMBL315166 | — | — | 1 | 5.86 |
| CHEMBL86519 | — | — | 1 | 5.36 |
| CHEMBL315846 | — | — | 1 | 5.24 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313179 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL87841 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL61946 | CARAMIPHEN | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL73234 | CARBETAPENTANE | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL84971 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL86830 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL305881 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL330021 | — | Ki | = | 66.2 | nM | 7.18 |
| CHEMBL316244 | — | Ki | = | 97.2 | nM | 7.01 |
| CHEMBL86477 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL433340 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL314433 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL7549 | PRECLAMOL | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL281594 | VANOXERINE | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL314424 | — | Ki | = | 372.0 | nM | 6.43 |
| CHEMBL316444 | — | Ki | = | 552.0 | nM | 6.26 |
| CHEMBL89832 | — | Ki | = | 596.0 | nM | 6.22 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 908.0 | nM | 6.04 |
| CHEMBL315166 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL86519 | — | Ki | = | 4420.0 | nM | 5.36 |
| CHEMBL315846 | — | Ki | = | 5720.0 | nM | 5.24 |
| CHEMBL370805 | COCAINE | Ki | = | 8830.0 | nM | 5.05 |