Assay Detail
Binding
CHEMBL5164050
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from human sigma 1 receptor transfected in human HEK293T cells assessed as inhibition constant by radioligand competition binding assay
30
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.64 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5208940 | — | — | 2 | 8.42 |
| CHEMBL5191108 | — | — | 2 | 8.35 |
| CHEMBL5183680 | — | — | 2 | 8.32 |
| CHEMBL5197224 | — | — | 2 | 8.27 |
| CHEMBL5206383 | — | — | 2 | 8.17 |
| CHEMBL5177703 | — | — | 2 | 8.10 |
| CHEMBL5185602 | — | — | 2 | 7.97 |
| CHEMBL5189334 | — | — | 2 | 7.82 |
| CHEMBL5207336 | — | — | 2 | 7.75 |
| CHEMBL5175530 | — | — | 2 | 7.54 |
| CHEMBL5170591 | — | — | 2 | 7.30 |
| CHEMBL5184025 | — | — | 2 | 6.98 |
| CHEMBL5189037 | — | — | 2 | 6.80 |
| CHEMBL5182001 | — | — | 2 | 6.61 |
| CHEMBL5181506 | — | — | 2 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5208940 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL5208940 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL5191108 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5191108 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL5183680 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL5183680 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL5197224 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL5197224 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL5206383 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL5206383 | — | Ki | = | 6.918 | nM | 8.16 |
| CHEMBL5177703 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5177703 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL5185602 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL5185602 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5189334 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5189334 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL5207336 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5207336 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL5175530 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL5175530 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL5170591 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL5170591 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5184025 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL5184025 | — | Ki | = | 104.71 | nM | 6.98 |
| CHEMBL5189037 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL5189037 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL5182001 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL5182001 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL5181506 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL5181506 | — | Ki | = | 609.0 | nM | 6.21 |