Assay Detail
Binding
CHEMBL808204
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Binding affinity for Sigma receptor type 1,using [3H](+)-pentazocine as radioligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.89 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304079 | — | — | 1 | 10.15 |
| CHEMBL302087 | — | — | 1 | 10.05 |
| CHEMBL67808 | — | — | 1 | 9.89 |
| CHEMBL19355 | — | — | 1 | 9.77 |
| CHEMBL19544 | — | — | 1 | 9.60 |
| CHEMBL69256 | — | — | 1 | 9.32 |
| CHEMBL303263 | — | — | 1 | 9.18 |
| CHEMBL305218 | — | — | 1 | 9.10 |
| CHEMBL71155 | — | — | 1 | 9.05 |
| CHEMBL71883 | — | — | 1 | 8.96 |
| CHEMBL304283 | — | — | 1 | 8.89 |
| CHEMBL305461 | — | — | 1 | 8.85 |
| CHEMBL72045 | — | — | 1 | 8.72 |
| CHEMBL71773 | — | — | 1 | 7.92 |
| CHEMBL282567 | PROADIFEN | 2.0 | 1 | 7.77 |
| CHEMBL71616 | — | — | 1 | 7.70 |
| CHEMBL68905 | — | — | 1 | 7.54 |
| CHEMBL72061 | — | — | 1 | 7.54 |
| CHEMBL70352 | BENACTYZINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304079 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL302087 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL67808 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL19355 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL19544 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL69256 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL303263 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL305218 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL71155 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL71883 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL304283 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL305461 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL72045 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL71773 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL282567 | PROADIFEN | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL71616 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL68905 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL72061 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL70352 | BENACTYZINE | Ki | > | 1000.0 | nM | - |