Assay Detail
Binding
CHEMBL808205
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Binding affinity measured on Sigma receptor type 1 from guinea pig brain membranes using [3H]pentazocine as radioligand.
26
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| 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 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.79 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318877 | — | — | 2 | 9.17 |
| CHEMBL103157 | — | — | 2 | 8.83 |
| CHEMBL102406 | — | — | 1 | 8.83 |
| CHEMBL330601 | — | — | 2 | 8.80 |
| CHEMBL103816 | — | — | 1 | 8.76 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL101300 | — | — | 2 | 8.42 |
| CHEMBL103156 | — | — | 1 | 8.33 |
| CHEMBL419343 | — | — | 1 | 8.25 |
| CHEMBL276078 | — | — | 2 | 8.14 |
| CHEMBL317354 | — | — | 1 | 7.98 |
| CHEMBL103319 | — | — | 1 | 7.95 |
| CHEMBL101607 | — | — | 2 | 7.74 |
| CHEMBL99854 | — | — | 1 | 7.73 |
| CHEMBL274099 | — | — | 1 | 7.22 |
| CHEMBL560 | — | — | 1 | 7.08 |
| CHEMBL318823 | — | — | 1 | 7.08 |
| CHEMBL100789 | — | — | 1 | 6.88 |
| CHEMBL101732 | — | — | 1 | 6.32 |
| CHEMBL257661 | METAZOCINE | 2.0 | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318877 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL102406 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL103157 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL330601 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL103816 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL101300 | — | Ki | = | 3.81 | nM | 8.42 |
| CHEMBL103156 | — | Ki | = | 4.68 | nM | 8.33 |
| CHEMBL419343 | — | Ki | = | 5.68 | nM | 8.25 |
| CHEMBL276078 | — | Ki | = | 7.16 | nM | 8.14 |
| CHEMBL317354 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL103319 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL101607 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL99854 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL101300 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL330601 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL103157 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL318877 | — | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL276078 | — | Ki | = | 40.1 | nM | 7.40 |
| CHEMBL101607 | — | Ki | = | 58.6 | nM | 7.23 |
| CHEMBL274099 | — | Ki | = | 59.7 | nM | 7.22 |
| CHEMBL560 | — | Ki | = | 83.1 | nM | 7.08 |
| CHEMBL318823 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL100789 | — | Ki | = | 130.6 | nM | 6.88 |
| CHEMBL101732 | — | Ki | = | 482.0 | nM | 6.32 |
| CHEMBL257661 | METAZOCINE | Ki | = | 2100.0 | nM | 5.68 |