Assay Detail
Binding
CHEMBL804959
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Binding affinity towards sigma opioid receptor in guinea pig cerebral homogenate using [3H]DTG as radioligand
20
Total Activities
20
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
Identification and exploitation of the sigma-opiate pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.01 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1907650 | — | — | 1 | 8.59 |
| CHEMBL20700 | — | — | 1 | 8.20 |
| CHEMBL20976 | — | — | 1 | 8.18 |
| CHEMBL20302 | — | — | 1 | 8.18 |
| CHEMBL12047 | — | — | 1 | 8.03 |
| CHEMBL20337 | — | — | 1 | 7.66 |
| CHEMBL20626 | — | — | 1 | 7.55 |
| CHEMBL20804 | — | — | 1 | 7.51 |
| CHEMBL1907648 | — | — | 1 | 7.35 |
| CHEMBL1907647 | — | — | 1 | 7.25 |
| CHEMBL278585 | — | — | 1 | 7.22 |
| CHEMBL1907649 | — | — | 1 | 7.01 |
| CHEMBL1907644 | N-BENZYLAMPHETAMINE | — | 1 | 6.93 |
| CHEMBL273866 | — | — | 1 | 6.56 |
| CHEMBL274099 | — | — | 1 | 6.37 |
| CHEMBL1907645 | — | — | 1 | 6.18 |
| CHEMBL1907646 | — | — | 1 | 6.18 |
| CHEMBL1907643 | — | — | 1 | 5.79 |
| CHEMBL1201201 | METHAMPHETAMINE | 4.0 | 1 | 5.08 |
| CHEMBL19393 | LEVAMFETAMINE | 4.0 | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1907650 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL20700 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL20976 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL20302 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL12047 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL20337 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL20626 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL20804 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1907648 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL1907647 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL278585 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL1907649 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL1907644 | N-BENZYLAMPHETAMINE | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL273866 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL274099 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL1907645 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL1907646 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL1907643 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL1201201 | METHAMPHETAMINE | Ki | = | 8320.0 | nM | 5.08 |
| CHEMBL19393 | LEVAMFETAMINE | Ki | = | 46400.0 | nM | 4.33 |