Assay Detail
Binding
CHEMBL3239228
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RPMI-8226 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.23 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233532 | — | — | 1 | 8.17 |
| CHEMBL3233531 | — | — | 1 | 8.12 |
| CHEMBL3233528 | — | — | 1 | 7.68 |
| CHEMBL3233529 | — | — | 1 | 7.64 |
| CHEMBL3233533 | — | — | 1 | 7.57 |
| CHEMBL3104857 | — | — | 1 | 7.54 |
| CHEMBL3233530 | — | — | 1 | 7.54 |
| CHEMBL3104856 | — | — | 1 | 7.47 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 7.44 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.40 |
| CHEMBL3233527 | — | — | 1 | 7.39 |
| CHEMBL3233526 | — | — | 1 | 6.97 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.68 |
| CHEMBL3233525 | — | — | 1 | 6.55 |
| CHEMBL3233536 | — | — | 1 | 6.33 |
| CHEMBL3233537 | — | — | 1 | 6.31 |
| CHEMBL3233535 | — | — | 1 | 6.15 |
| CHEMBL3233524 | — | — | 1 | - |
| CHEMBL3233534 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233532 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL3233531 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3233528 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3233529 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3233533 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3104857 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3233530 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3104856 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3233527 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL3233526 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL3233525 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL3233536 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL3233537 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL3233535 | — | Ki | = | 711.0 | nM | 6.15 |
| CHEMBL3233524 | — | Ki | - | — | - | |
| CHEMBL3233534 | — | Ki | - | — | - |