Assay Detail
Binding
CHEMBL872703
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Binding affinity was measured on Sigma receptor type 1 using [3H]- pentazocine as radioligand
13
Total Activities
11
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 sigma binding properties of 1'- and 3'-halo- and 1',3'-dihalo-N-normetazocine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.65 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318877 | — | — | 1 | 9.17 |
| CHEMBL100463 | — | — | 1 | 8.76 |
| CHEMBL103455 | — | — | 1 | 8.76 |
| CHEMBL103458 | — | — | 1 | 8.60 |
| CHEMBL318954 | — | — | 1 | 8.58 |
| CHEMBL419161 | — | — | 2 | 7.45 |
| CHEMBL102860 | — | — | 2 | 7.43 |
| CHEMBL103715 | — | — | 1 | 7.16 |
| CHEMBL103662 | — | — | 1 | 7.15 |
| CHEMBL102847 | — | — | 1 | 6.92 |
| CHEMBL103707 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318877 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL100463 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL103455 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL103458 | — | Ki | = | 2.49 | nM | 8.60 |
| CHEMBL318954 | — | Ki | = | 2.62 | nM | 8.58 |
| CHEMBL419161 | — | Ki | = | 35.2 | nM | 7.45 |
| CHEMBL102860 | — | Ki | = | 37.4 | nM | 7.43 |
| CHEMBL103715 | — | Ki | = | 68.6 | nM | 7.16 |
| CHEMBL103662 | — | Ki | = | 71.5 | nM | 7.15 |
| CHEMBL102847 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL102860 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL103707 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL419161 | — | Ki | = | 944.0 | nM | 6.03 |