Assay Detail
Binding
CHEMBL809525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards sigma receptor binding site 2 using [3H]DTG of whole rat brain homogenates except cerebellum
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.64 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64683 | — | — | 1 | 10.30 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 9.92 |
| CHEMBL59273 | — | — | 1 | 9.77 |
| CHEMBL59306 | — | — | 1 | 9.72 |
| CHEMBL59249 | — | — | 1 | 9.68 |
| CHEMBL61812 | — | — | 1 | 9.62 |
| CHEMBL62137 | — | — | 1 | 9.60 |
| CHEMBL61539 | — | — | 1 | 9.57 |
| CHEMBL304232 | — | — | 1 | 9.52 |
| CHEMBL59464 | — | — | 1 | 9.39 |
| CHEMBL64302 | — | — | 1 | 9.39 |
| CHEMBL303804 | — | — | 1 | 9.36 |
| CHEMBL64113 | — | — | 1 | 9.32 |
| CHEMBL59335 | — | — | 1 | 9.32 |
| CHEMBL433831 | — | — | 1 | 9.16 |
| CHEMBL279586 | — | — | 1 | 8.89 |
| CHEMBL64344 | — | — | 1 | 8.64 |
| CHEMBL62994 | — | — | 1 | 8.60 |
| CHEMBL60845 | — | — | 1 | 8.55 |
| CHEMBL62188 | — | — | 1 | 8.52 |
| CHEMBL61747 | — | — | 1 | 8.48 |
| CHEMBL60267 | — | — | 1 | 8.40 |
| CHEMBL61343 | — | — | 1 | 8.33 |
| CHEMBL416506 | — | — | 1 | 8.12 |
| CHEMBL303336 | — | — | 1 | 7.92 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.77 |
| CHEMBL59940 | — | — | 1 | 7.68 |
| CHEMBL42228 | — | — | 1 | 7.64 |
| CHEMBL397705 | REL-PENTAZOCINE | — | 1 | 7.54 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64683 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL61479 | SIRAMESINE | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL59273 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL59306 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL59249 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL61812 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL62137 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL61539 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL304232 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL59464 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL64302 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL303804 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL64113 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL59335 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL433831 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL279586 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL64344 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL62994 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL60845 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL62188 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL61747 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL60267 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL61343 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL416506 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL303336 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL59940 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL42228 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL397705 | REL-PENTAZOCINE | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL60542 | (+)-PENTAZOCINE | IC50 | = | 2100.0 | nM | 5.68 |