Assay Detail
Binding
CHEMBL2173634
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 HEK293 cell membranes after 120 mins by scintillation counter
72
Total Activities
72
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
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 72 | 7.61 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.68 |
| CHEMBL2170226 | — | — | 1 | 8.28 |
| CHEMBL2170227 | — | — | 1 | 8.26 |
| CHEMBL73824 | — | — | 1 | 8.20 |
| CHEMBL2170222 | — | — | 1 | 8.16 |
| CHEMBL2170223 | — | — | 1 | 8.15 |
| CHEMBL2170213 | — | — | 1 | 8.14 |
| CHEMBL2170237 | — | — | 1 | 8.09 |
| CHEMBL2170206 | — | — | 1 | 8.09 |
| CHEMBL2170229 | — | — | 1 | 8.08 |
| CHEMBL2170212 | — | — | 1 | 8.07 |
| CHEMBL2170235 | — | — | 1 | 8.07 |
| CHEMBL2170211 | — | — | 1 | 8.05 |
| CHEMBL2170228 | — | — | 1 | 8.03 |
| CHEMBL2170055 | — | — | 1 | 8.03 |
| CHEMBL2170054 | — | — | 1 | 8.02 |
| CHEMBL2170219 | — | — | 1 | 8.02 |
| CHEMBL2170071 | — | — | 1 | 8.00 |
| CHEMBL2170067 | — | — | 1 | 8.00 |
| CHEMBL2170234 | — | — | 1 | 8.00 |
| CHEMBL2170068 | — | — | 1 | 8.00 |
| CHEMBL2170076 | — | — | 1 | 7.99 |
| CHEMBL2170217 | — | — | 1 | 7.98 |
| CHEMBL2170225 | — | — | 1 | 7.97 |
| CHEMBL2170231 | — | — | 1 | 7.96 |
| CHEMBL2170072 | — | — | 1 | 7.93 |
| CHEMBL2170218 | — | — | 1 | 7.88 |
| CHEMBL2170221 | — | — | 1 | 7.88 |
| CHEMBL2170051 | — | — | 1 | 7.85 |
| CHEMBL2170233 | — | — | 1 | 7.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2170226 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2170227 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL73824 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2170222 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL2170223 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL2170213 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL2170237 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2170206 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2170229 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL2170212 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL2170235 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL2170211 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL2170055 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2170228 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2170054 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL2170219 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL2170071 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL2170067 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2170234 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL2170068 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL2170076 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL2170217 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL2170225 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL2170231 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL2170072 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL2170221 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL2170218 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL2170051 | — | Ki | = | 14.2 | nM | 7.85 |
| CHEMBL2170233 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL2170203 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL2170238 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL2170230 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2169891 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL2170239 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL2170220 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2170204 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL2170060 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL2170075 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL2170216 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL2170066 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL2170205 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2170224 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2170063 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL2170070 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL2170207 | — | Ki | = | 36.8 | nM | 7.43 |
| CHEMBL2170053 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL2170061 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2170232 | — | Ki | = | 44.0 | nM | 7.36 |