Assay Detail
Binding
CHEMBL846480
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against sigma receptor in bovine cerebellum using 2.0 nM [3H]haloperidol in the presence of 25 nM unlabeled spiperone
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(1-arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective sigma receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.07 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129452 | — | — | 1 | 9.30 |
| CHEMBL338181 | — | — | 1 | 8.40 |
| CHEMBL340401 | — | — | 1 | 8.15 |
| CHEMBL130357 | — | — | 1 | 8.10 |
| CHEMBL126437 | — | — | 1 | 7.64 |
| CHEMBL125913 | — | — | 1 | 7.60 |
| CHEMBL101664 | — | — | 1 | 7.30 |
| CHEMBL126684 | — | — | 1 | 7.18 |
| CHEMBL127067 | — | — | 1 | 7.00 |
| CHEMBL129521 | — | — | 1 | 6.80 |
| CHEMBL340541 | — | — | 1 | 6.80 |
| CHEMBL446358 | — | — | 1 | 6.63 |
| CHEMBL340532 | — | — | 1 | 6.55 |
| CHEMBL435211 | — | — | 1 | 6.40 |
| CHEMBL420344 | — | — | 1 | 6.30 |
| CHEMBL126086 | — | — | 1 | 6.30 |
| CHEMBL6224 | — | — | 1 | 6.00 |
| CHEMBL130526 | — | — | 1 | 5.90 |
| CHEMBL126738 | — | — | 1 | 5.90 |
| CHEMBL50115 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129452 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL338181 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL340401 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL130357 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL126437 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL125913 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL101664 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL126684 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL127067 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL129521 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL340541 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL446358 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL340532 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL435211 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL420344 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL126086 | — | IC50 | = | 495.0 | nM | 6.30 |
| CHEMBL6224 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL130526 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL126738 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL50115 | — | IC50 | > | 5000.0 | nM | - |