Assay Detail
Binding
CHEMBL3590860
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membranes incubated for 2 hrs in presence of dextrallorphan by liquid scintillation counting based competitive radioligand binding assay
54
Total Activities
54
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 6.50 | 7.73 |
| Ki(app) | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589874 | — | — | 1 | 7.73 |
| CHEMBL3589720 | — | — | 1 | 7.34 |
| CHEMBL3589877 | — | — | 1 | 7.34 |
| CHEMBL3589871 | — | — | 1 | 7.33 |
| CHEMBL3589869 | — | — | 1 | 7.28 |
| CHEMBL3589714 | — | — | 1 | 7.26 |
| CHEMBL3589729 | — | — | 1 | 7.22 |
| CHEMBL3589876 | — | — | 1 | 7.21 |
| CHEMBL3589712 | — | — | 1 | 7.17 |
| CHEMBL264437 | — | — | 1 | 7.11 |
| CHEMBL3589711 | — | — | 1 | 7.07 |
| CHEMBL3589724 | — | — | 1 | 7.05 |
| CHEMBL87379 | BENZOVESAMICOL | — | 1 | 7.02 |
| CHEMBL3589717 | — | — | 1 | 6.99 |
| CHEMBL3589865 | — | — | 1 | 6.97 |
| CHEMBL3589872 | — | — | 1 | 6.96 |
| CHEMBL20730 | VESAMICOL | — | 1 | 6.95 |
| CHEMBL3589873 | — | — | 1 | 6.87 |
| CHEMBL3590030 | — | — | 1 | 6.80 |
| CHEMBL3589723 | — | — | 1 | 6.79 |
| CHEMBL3589730 | — | — | 1 | 6.79 |
| CHEMBL3589863 | — | — | 1 | 6.79 |
| CHEMBL3589870 | — | — | 1 | 6.78 |
| CHEMBL3589727 | — | — | 1 | 6.78 |
| CHEMBL3589719 | — | — | 1 | 6.68 |
| CHEMBL3589731 | — | — | 1 | 6.59 |
| CHEMBL3589716 | — | — | 1 | 6.59 |
| CHEMBL3589715 | — | — | 1 | 6.55 |
| CHEMBL473129 | — | — | 1 | 6.55 |
| CHEMBL3589721 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589874 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL3589720 | — | Ki | = | 45.6 | nM | 7.34 |
| CHEMBL3589877 | — | Ki | = | 45.9 | nM | 7.34 |
| CHEMBL3589871 | — | Ki | = | 46.9 | nM | 7.33 |
| CHEMBL3589869 | — | Ki | = | 53.1 | nM | 7.28 |
| CHEMBL3589714 | — | Ki | = | 55.5 | nM | 7.26 |
| CHEMBL3589729 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3589876 | — | Ki | = | 61.8 | nM | 7.21 |
| CHEMBL3589712 | — | Ki | = | 67.1 | nM | 7.17 |
| CHEMBL264437 | — | Ki | = | 77.1 | nM | 7.11 |
| CHEMBL3589711 | — | Ki | = | 85.8 | nM | 7.07 |
| CHEMBL3589724 | — | Ki | = | 88.2 | nM | 7.05 |
| CHEMBL87379 | BENZOVESAMICOL | Ki | = | 96.4 | nM | 7.02 |
| CHEMBL3589717 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL3589865 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3589872 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL20730 | VESAMICOL | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL3589873 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL3590030 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL3589723 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL3589730 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL3589863 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL3589870 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL3589727 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL3589719 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL3589731 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL3589716 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL3589715 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL473129 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL3589721 | — | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL87381 | — | Ki | = | 474.0 | nM | 6.32 |
| CHEMBL3589728 | — | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL3589878 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL3589879 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL3590031 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL3590029 | — | Ki | = | 695.0 | nM | 6.16 |
| CHEMBL3589732 | — | Ki | = | 726.0 | nM | 6.14 |
| CHEMBL3589725 | — | Ki | = | 717.0 | nM | 6.14 |
| CHEMBL1089853 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL3589866 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL3589713 | — | Ki | = | 1041.0 | nM | 5.98 |
| CHEMBL3589726 | — | Ki | = | 1275.0 | nM | 5.89 |
| CHEMBL3589735 | — | Ki | = | 1381.0 | nM | 5.86 |
| CHEMBL3589864 | — | Ki | = | 1829.0 | nM | 5.74 |
| CHEMBL3589722 | — | Ki | = | 1996.0 | nM | 5.70 |
| CHEMBL3589862 | — | Ki | = | 1994.0 | nM | 5.70 |
| CHEMBL3589734 | — | Ki | = | 2079.0 | nM | 5.68 |
| CHEMBL3589736 | — | Ki | = | 2112.0 | nM | 5.67 |
| CHEMBL3589875 | — | Ki | = | 2363.0 | nM | 5.63 |
| CHEMBL3589868 | — | Ki | = | 3317.0 | nM | 5.48 |