Assay Detail
Binding
CHEMBL804718
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against radioligand [3H]3-PPP binding to Sigma opioid receptor type 1 in rat brain membrane
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 7.57 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL545597 | — | — | 1 | 9.00 |
| CHEMBL11736 | — | — | 1 | 9.00 |
| CHEMBL537238 | — | — | 1 | 9.00 |
| CHEMBL521582 | — | — | 1 | 8.89 |
| CHEMBL12107 | — | — | 1 | 8.82 |
| CHEMBL11290 | — | — | 1 | 8.77 |
| CHEMBL542298 | — | — | 1 | 8.74 |
| CHEMBL542047 | — | — | 1 | 8.57 |
| CHEMBL542295 | — | — | 1 | 8.54 |
| CHEMBL542785 | — | — | 1 | 8.51 |
| CHEMBL11182 | — | — | 1 | 8.33 |
| CHEMBL11774 | — | — | 1 | 8.18 |
| CHEMBL11474 | — | — | 1 | 8.17 |
| CHEMBL537251 | — | — | 1 | 8.15 |
| CHEMBL11803 | — | — | 1 | 8.14 |
| CHEMBL542049 | — | — | 1 | 8.03 |
| CHEMBL269638 | — | — | 1 | 7.96 |
| CHEMBL11279 | — | — | 1 | 7.96 |
| CHEMBL11894 | — | — | 1 | 7.92 |
| CHEMBL543015 | — | — | 1 | 7.89 |
| CHEMBL275948 | — | — | 1 | 7.89 |
| CHEMBL276007 | — | — | 1 | 7.82 |
| CHEMBL542048 | — | — | 1 | 7.75 |
| CHEMBL542783 | — | — | 1 | 7.72 |
| CHEMBL11535 | — | — | 1 | 7.66 |
| CHEMBL545598 | — | — | 1 | 7.60 |
| CHEMBL542046 | — | — | 1 | 7.60 |
| CHEMBL11657 | — | — | 1 | 7.58 |
| CHEMBL262955 | — | — | 1 | 7.58 |
| CHEMBL11598 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL545597 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL537238 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL11736 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL521582 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL12107 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL11290 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL542298 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL542047 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL542295 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL542785 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL11182 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL11774 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL11474 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL537251 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL11803 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL542049 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL269638 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL11279 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL11894 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL543015 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL275948 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL276007 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL542048 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL542783 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL11535 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL545598 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL542046 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL11657 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL262955 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL11598 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL11479 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL11304 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL542786 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL11255 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL11231 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL11740 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL273626 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL11311 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL11640 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL11581 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL11675 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL11437 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL11534 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL11637 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL11289 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL11380 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL416335 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL11669 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL11161 | — | IC50 | = | 415.0 | nM | 6.38 |