Assay Detail
Binding
CHEMBL4711023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 7.06 | 8.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744824 | — | — | 1 | 8.69 |
| CHEMBL3916231 | — | — | 1 | 8.65 |
| CHEMBL4795981 | — | — | 1 | 8.45 |
| CHEMBL4788794 | — | — | 1 | 8.42 |
| CHEMBL4636778 | — | — | 1 | 8.25 |
| CHEMBL4784393 | — | — | 1 | 8.23 |
| CHEMBL4758124 | — | — | 1 | 8.15 |
| CHEMBL4794406 | — | — | 1 | 7.88 |
| CHEMBL4791063 | — | — | 1 | 7.69 |
| CHEMBL4750660 | — | — | 1 | 7.58 |
| CHEMBL4741279 | — | — | 1 | 7.49 |
| CHEMBL3918282 | — | — | 1 | 7.38 |
| CHEMBL4788854 | — | — | 1 | 7.38 |
| CHEMBL4785770 | — | — | 1 | 7.34 |
| CHEMBL4742866 | — | — | 1 | 7.33 |
| CHEMBL4748901 | — | — | 1 | 7.24 |
| CHEMBL4747413 | — | — | 1 | 7.21 |
| CHEMBL4750997 | — | — | 1 | 7.21 |
| CHEMBL4798638 | — | — | 1 | 7.06 |
| CHEMBL4789139 | — | — | 1 | 6.90 |
| CHEMBL4784884 | — | — | 1 | 6.79 |
| CHEMBL4765081 | — | — | 1 | 6.79 |
| CHEMBL4782055 | — | — | 1 | 6.77 |
| CHEMBL4744739 | — | — | 1 | 6.73 |
| CHEMBL4746636 | — | — | 1 | 6.69 |
| CHEMBL4762414 | — | — | 1 | 6.69 |
| CHEMBL4781767 | — | — | 1 | 6.57 |
| CHEMBL4795634 | — | — | 1 | 6.52 |
| CHEMBL4750607 | — | — | 1 | 6.51 |
| CHEMBL4783618 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744824 | — | Ki | = | 2.03 | nM | 8.69 |
| CHEMBL3916231 | — | Ki | = | 2.24 | nM | 8.65 |
| CHEMBL4795981 | — | Ki | = | 3.57 | nM | 8.45 |
| CHEMBL4788794 | — | Ki | = | 3.81 | nM | 8.42 |
| CHEMBL4636778 | — | Ki | = | 5.62 | nM | 8.25 |
| CHEMBL4784393 | — | Ki | = | 5.87 | nM | 8.23 |
| CHEMBL4758124 | — | Ki | = | 7.11 | nM | 8.15 |
| CHEMBL4794406 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL4791063 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL4750660 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL4741279 | — | Ki | = | 32.1 | nM | 7.49 |
| CHEMBL3918282 | — | Ki | = | 41.6 | nM | 7.38 |
| CHEMBL4788854 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL4785770 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL4742866 | — | Ki | = | 46.4 | nM | 7.33 |
| CHEMBL4748901 | — | Ki | = | 57.7 | nM | 7.24 |
| CHEMBL4747413 | — | Ki | = | 60.9 | nM | 7.21 |
| CHEMBL4750997 | — | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL4798638 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL4789139 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL4765081 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL4784884 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL4782055 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL4744739 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL4746636 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4762414 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4781767 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL4795634 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL4750607 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL4783618 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL4758774 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL3931765 | — | Ki | = | 454.0 | nM | 6.34 |
| CHEMBL4762706 | — | Ki | = | 516.0 | nM | 6.29 |
| CHEMBL4764168 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL4757505 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL4742033 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL4747068 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL4777080 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL4756427 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL1672359 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4744200 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4785024 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1373 | MODAFINIL | Ki | - | — | - |