Assay Detail
Binding
CHEMBL4356653
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ1 Receptor Antagonists for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 55 | 7.48 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.70 |
| CHEMBL4470425 | — | — | 1 | 8.52 |
| CHEMBL4541206 | — | — | 1 | 8.22 |
| CHEMBL4515812 | — | — | 1 | 8.22 |
| CHEMBL4538620 | — | — | 1 | 8.10 |
| CHEMBL4536259 | — | — | 1 | 8.10 |
| CHEMBL4452042 | — | — | 1 | 8.10 |
| CHEMBL4534193 | — | — | 1 | 8.10 |
| CHEMBL4560624 | — | — | 1 | 8.05 |
| CHEMBL4438550 | — | — | 1 | 8.05 |
| CHEMBL4436170 | — | — | 1 | 8.00 |
| CHEMBL4584335 | — | — | 1 | 7.96 |
| CHEMBL4544352 | — | — | 1 | 7.96 |
| CHEMBL4516327 | — | — | 1 | 7.89 |
| CHEMBL4439718 | — | — | 1 | 7.89 |
| CHEMBL4578955 | — | — | 1 | 7.89 |
| CHEMBL4593220 | — | — | 1 | 7.85 |
| CHEMBL4457602 | — | — | 1 | 7.85 |
| CHEMBL4467749 | — | — | 1 | 7.85 |
| CHEMBL4550656 | — | — | 1 | 7.82 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL4450665 | — | — | 1 | 7.68 |
| CHEMBL4446292 | — | — | 1 | 7.58 |
| CHEMBL4463621 | — | — | 1 | 7.55 |
| CHEMBL4439285 | — | — | 1 | 7.50 |
| CHEMBL4526087 | — | — | 1 | 7.42 |
| CHEMBL4483643 | — | — | 1 | 7.41 |
| CHEMBL4528962 | — | — | 1 | 7.40 |
| CHEMBL4535897 | — | — | 1 | 7.32 |
| CHEMBL4592081 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4470425 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4515812 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4541206 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4538620 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4536259 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4452042 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4534193 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4560624 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4438550 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4436170 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4584335 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4544352 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4439718 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4516327 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4578955 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4593220 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4457602 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4467749 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4550656 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4450665 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4446292 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4463621 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4439285 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4526087 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4483643 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4528962 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4535897 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4592081 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4473746 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4540995 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4448670 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4446209 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4471711 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4461864 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4461774 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4439908 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4576031 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4460762 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4440055 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4448710 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL4571738 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL4522004 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL4445578 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL4513933 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL4573960 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4525653 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4459117 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4463901 | — | Ki | = | 237.0 | nM | 6.62 |