Assay Detail
Binding
CHEMBL809523
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Binding affinity towards Sigma receptor site 2 in rat brain using [3H]DTG as radioligand
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 8.32 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62002 | — | — | 1 | 10.15 |
| CHEMBL59809 | — | — | 1 | 10.15 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 9.92 |
| CHEMBL178042 | — | — | 1 | 9.85 |
| CHEMBL291624 | — | — | 1 | 9.70 |
| CHEMBL64305 | — | — | 1 | 9.70 |
| CHEMBL304671 | — | — | 1 | 9.60 |
| CHEMBL294734 | — | — | 1 | 9.59 |
| CHEMBL59852 | — | — | 1 | 9.51 |
| CHEMBL63999 | — | — | 1 | 9.47 |
| CHEMBL263271 | — | — | 1 | 9.24 |
| CHEMBL64844 | — | — | 1 | 9.05 |
| CHEMBL60389 | — | — | 1 | 8.96 |
| CHEMBL62300 | — | — | 1 | 8.96 |
| CHEMBL60099 | — | — | 1 | 8.74 |
| CHEMBL60608 | — | — | 1 | 8.59 |
| CHEMBL64549 | — | — | 1 | 8.54 |
| CHEMBL58734 | — | — | 1 | 8.52 |
| CHEMBL299284 | — | — | 1 | 8.15 |
| CHEMBL64468 | — | — | 1 | 8.14 |
| CHEMBL305335 | — | — | 1 | 7.92 |
| CHEMBL303780 | — | — | 1 | 7.64 |
| CHEMBL42228 | — | — | 1 | 7.64 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.28 |
| CHEMBL64023 | — | — | 1 | 7.16 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.64 |
| CHEMBL416854 | — | — | 1 | 6.60 |
| CHEMBL61461 | — | — | 1 | 6.57 |
| CHEMBL302670 | — | — | 1 | 6.47 |
| CHEMBL60474 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62002 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL59809 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL61479 | SIRAMESINE | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL178042 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL291624 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL64305 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL304671 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL294734 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL59852 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL63999 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL263271 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL64844 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL60389 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL62300 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL60099 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL60608 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL64549 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL58734 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL299284 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL64468 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL305335 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL303780 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL42228 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL64023 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL416854 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL61461 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL302670 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL60474 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL62615 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL60542 | (+)-PENTAZOCINE | IC50 | = | 2100.0 | nM | 5.68 |