Assay Detail
Binding
CHEMBL809515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay.
41
Total Activities
41
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 (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 | 41 | 7.88 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303336 | — | — | 1 | 9.59 |
| CHEMBL304671 | — | — | 1 | 9.57 |
| CHEMBL59809 | — | — | 1 | 9.40 |
| CHEMBL291624 | — | — | 1 | 9.28 |
| CHEMBL60389 | — | — | 1 | 9.25 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.19 |
| CHEMBL64305 | — | — | 1 | 9.09 |
| CHEMBL294734 | — | — | 1 | 9.02 |
| CHEMBL62002 | — | — | 1 | 8.82 |
| CHEMBL64549 | — | — | 1 | 8.66 |
| CHEMBL64468 | — | — | 1 | 8.60 |
| CHEMBL42228 | — | — | 1 | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.52 |
| CHEMBL63999 | — | — | 1 | 8.47 |
| CHEMBL305335 | — | — | 1 | 8.42 |
| CHEMBL64047 | — | — | 1 | 8.33 |
| CHEMBL59852 | — | — | 1 | 8.26 |
| CHEMBL60474 | — | — | 1 | 8.20 |
| CHEMBL58734 | — | — | 1 | 8.15 |
| CHEMBL560 | — | — | 1 | 8.05 |
| CHEMBL64115 | — | — | 1 | 8.02 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.77 |
| CHEMBL62300 | — | — | 1 | 7.64 |
| CHEMBL299284 | — | — | 1 | 7.52 |
| CHEMBL61739 | — | — | 1 | 7.51 |
| CHEMBL178042 | — | — | 1 | 7.46 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.44 |
| CHEMBL64844 | — | — | 1 | 7.28 |
| CHEMBL60859 | BMY-14802 | — | 1 | 7.22 |
| CHEMBL64023 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303336 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL304671 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL59809 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL291624 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL60389 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL64305 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL294734 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL62002 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL64549 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL64468 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL42228 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL63999 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL305335 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL64047 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL59852 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL60474 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL58734 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL560 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL64115 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL61479 | SIRAMESINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL62300 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL299284 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL61739 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL178042 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL64844 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL64023 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL303780 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL292512 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL263271 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL62615 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL60608 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL416854 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL60099 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL302670 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL61461 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL64369 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 690.0 | nM | 6.16 |