Assay Detail
Binding
CHEMBL813142
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Binding affinity was measured on Sigma receptor type 2 using [3H]- DTG as radioligand
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 16 | 6.31 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL560 | — | — | 1 | 7.44 |
| CHEMBL102860 | — | — | 2 | 7.14 |
| CHEMBL419161 | — | — | 2 | 7.03 |
| CHEMBL102847 | — | — | 1 | 6.68 |
| CHEMBL103458 | — | — | 1 | 6.55 |
| CHEMBL103455 | — | — | 1 | 6.46 |
| CHEMBL103707 | — | — | 1 | 6.22 |
| CHEMBL100463 | — | — | 1 | 6.12 |
| CHEMBL103715 | — | — | 1 | 5.91 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 5.81 |
| CHEMBL318877 | — | — | 1 | 5.77 |
| CHEMBL328608 | — | — | 1 | 5.70 |
| CHEMBL103662 | — | — | 1 | 5.66 |
| CHEMBL318954 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL560 | — | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL102860 | — | Ki | = | 72.8 | nM | 7.14 |
| CHEMBL419161 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL102847 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL419161 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL103458 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL103455 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL102860 | — | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL103707 | — | Ki | = | 597.0 | nM | 6.22 |
| CHEMBL100463 | — | Ki | = | 764.0 | nM | 6.12 |
| CHEMBL103715 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 1540.0 | nM | 5.81 |
| CHEMBL318877 | — | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL328608 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL103662 | — | Ki | = | 2170.0 | nM | 5.66 |
| CHEMBL318954 | — | Ki | = | 4960.0 | nM | 5.30 |