Assay Detail
Binding
CHEMBL804883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against [3H]DTG binding to Sigma opioid receptor in guinea pig brain membrane homogenates
71
Total Activities
71
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 | 71 | 6.96 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310003 | — | — | 1 | 8.40 |
| CHEMBL553347 | — | — | 1 | 8.28 |
| CHEMBL553896 | — | — | 1 | 8.22 |
| CHEMBL81461 | — | — | 1 | 8.22 |
| CHEMBL81773 | — | — | 1 | 8.22 |
| CHEMBL81835 | — | — | 1 | 8.10 |
| CHEMBL78777 | — | — | 1 | 8.08 |
| CHEMBL79164 | — | — | 1 | 7.92 |
| CHEMBL543597 | — | — | 1 | 7.89 |
| CHEMBL310170 | — | — | 1 | 7.86 |
| CHEMBL312600 | — | — | 1 | 7.85 |
| CHEMBL540291 | — | — | 1 | 7.82 |
| CHEMBL545011 | — | — | 1 | 7.80 |
| CHEMBL553535 | — | — | 1 | 7.80 |
| CHEMBL553074 | — | — | 1 | 7.80 |
| CHEMBL553817 | — | — | 1 | 7.75 |
| CHEMBL79186 | — | — | 1 | 7.68 |
| CHEMBL556021 | — | — | 1 | 7.68 |
| CHEMBL554972 | — | — | 1 | 7.66 |
| CHEMBL79665 | — | — | 1 | 7.60 |
| CHEMBL78488 | — | — | 1 | 7.52 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.50 |
| CHEMBL79437 | — | — | 1 | 7.44 |
| CHEMBL81824 | — | — | 1 | 7.43 |
| CHEMBL79436 | — | — | 1 | 7.43 |
| CHEMBL309603 | — | — | 1 | 7.23 |
| CHEMBL78306 | — | — | 1 | 7.23 |
| CHEMBL280243 | — | — | 1 | 7.19 |
| CHEMBL81867 | — | — | 1 | 7.15 |
| CHEMBL82078 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310003 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL553347 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL81461 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL81773 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL553896 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL81835 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL78777 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL79164 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL543597 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL310170 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL312600 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL540291 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL553074 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL553535 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL545011 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL553817 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL79186 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL556021 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL554972 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL79665 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL78488 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL79437 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL81824 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL79436 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL309603 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL78306 | — | IC50 | = | 58.8 | nM | 7.23 |
| CHEMBL280243 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL81867 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL82078 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL539782 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL81735 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL543355 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL312588 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL545007 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL79509 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL81678 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL543839 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL536782 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL81539 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL543120 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL78083 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL556617 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL553536 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL81626 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL79145 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL543596 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL415077 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL82144 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL539360 | — | IC50 | = | 345.0 | nM | 6.46 |