Assay Detail
Binding
CHEMBL848647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine
16
Total Activities
16
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
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.42 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL154397 | — | — | 1 | 8.70 |
| CHEMBL20377 | — | — | 1 | 8.68 |
| CHEMBL142596 | — | — | 1 | 8.66 |
| CHEMBL358109 | — | — | 1 | 8.62 |
| CHEMBL152426 | — | — | 1 | 8.60 |
| CHEMBL152057 | — | — | 1 | 8.60 |
| CHEMBL346153 | — | — | 1 | 8.54 |
| CHEMBL81602 | — | — | 1 | 8.51 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL356909 | — | — | 1 | 8.44 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.43 |
| CHEMBL151136 | — | — | 1 | 8.37 |
| CHEMBL152478 | — | — | 1 | 8.27 |
| CHEMBL153758 | — | — | 1 | 8.22 |
| CHEMBL152618 | — | — | 1 | 8.05 |
| CHEMBL349793 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL154397 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL20377 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL142596 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL358109 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL152426 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL152057 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL346153 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL81602 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL356909 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL151136 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL152478 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL153758 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL152618 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL349793 | — | Ki | = | 26.6 | nM | 7.58 |