Assay Detail
Binding
CHEMBL4017718
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.04 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.68 |
| CHEMBL299499 | — | — | 1 | 8.57 |
| CHEMBL4092687 | — | — | 1 | 7.87 |
| CHEMBL4084182 | — | — | 1 | 7.42 |
| CHEMBL4098778 | — | — | 1 | 7.34 |
| CHEMBL4065001 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL299499 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4092687 | — | Ki | = | 13.36 | nM | 7.87 |
| CHEMBL4084182 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4098778 | — | Ki | = | 46.08 | nM | 7.34 |
| CHEMBL4065001 | — | Ki | = | 45.32 | nM | 7.34 |