Assay Detail
Binding
CHEMBL873129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against [3H]- (+)-3-PPP binding to Sigma opioid receptor in guinea pig brain membrane homogenates
30
Total Activities
30
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 structure-activity relationships of N,N'-di-o-tolylguanidine analogues, high-affinity ligands for the haloperidol-sensitive sigma receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.06 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553896 | — | — | 1 | 8.30 |
| CHEMBL81835 | — | — | 1 | 8.10 |
| CHEMBL543597 | — | — | 1 | 8.10 |
| CHEMBL553535 | — | — | 1 | 7.96 |
| CHEMBL79164 | — | — | 1 | 7.82 |
| CHEMBL312600 | — | — | 1 | 7.80 |
| CHEMBL78488 | — | — | 1 | 7.70 |
| CHEMBL79186 | — | — | 1 | 7.64 |
| CHEMBL78777 | — | — | 1 | 7.52 |
| CHEMBL79436 | — | — | 1 | 7.50 |
| CHEMBL539782 | — | — | 1 | 7.48 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.42 |
| CHEMBL81824 | — | — | 1 | 7.41 |
| CHEMBL310170 | — | — | 1 | 7.36 |
| CHEMBL81867 | — | — | 1 | 7.32 |
| CHEMBL309603 | — | — | 1 | 7.08 |
| CHEMBL312588 | — | — | 1 | 7.03 |
| CHEMBL79145 | — | — | 1 | 6.85 |
| CHEMBL536782 | — | — | 1 | 6.81 |
| CHEMBL543596 | — | — | 1 | 6.66 |
| CHEMBL543120 | — | — | 1 | 6.62 |
| CHEMBL81070 | — | — | 1 | 6.46 |
| CHEMBL77675 | — | — | 1 | 6.40 |
| CHEMBL78585 | — | — | 1 | 6.36 |
| CHEMBL81539 | — | — | 1 | 6.12 |
| CHEMBL80081 | — | — | 1 | 6.10 |
| CHEMBL541828 | — | — | 1 | 6.07 |
| CHEMBL310729 | — | — | 1 | 5.42 |
| CHEMBL79165 | — | — | 1 | 5.29 |
| CHEMBL545471 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553896 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL81835 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL543597 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL553535 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL79164 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL312600 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL78488 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL79186 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL78777 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL79436 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL539782 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL81824 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL310170 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL81867 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL309603 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL312588 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL79145 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL536782 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL543596 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL543120 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL81070 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL77675 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL78585 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL81539 | — | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL80081 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL541828 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL310729 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL79165 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL545471 | — | IC50 | > | 10000.0 | nM | - |