Assay Detail
Binding
CHEMBL4614015
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by microbeta scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| 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)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.47 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4641869 | — | — | 1 | 8.97 |
| CHEMBL4640152 | — | — | 1 | 8.66 |
| CHEMBL4638977 | — | — | 1 | 8.59 |
| CHEMBL4647283 | — | — | 1 | 8.52 |
| CHEMBL4636778 | — | — | 1 | 8.25 |
| CHEMBL4647200 | — | — | 1 | 8.22 |
| CHEMBL4647914 | — | — | 1 | 8.11 |
| CHEMBL4635589 | — | — | 1 | 8.02 |
| CHEMBL4640772 | — | — | 1 | 7.82 |
| CHEMBL4643955 | — | — | 1 | 7.63 |
| CHEMBL4649604 | — | — | 1 | 7.56 |
| CHEMBL4643859 | — | — | 1 | 7.54 |
| CHEMBL4635958 | — | — | 1 | 7.53 |
| CHEMBL4648300 | — | — | 1 | 7.50 |
| CHEMBL4638203 | — | — | 1 | 7.48 |
| CHEMBL4645855 | — | — | 1 | 7.41 |
| CHEMBL4640372 | — | — | 1 | 7.34 |
| CHEMBL4634263 | — | — | 1 | 7.19 |
| CHEMBL4642082 | — | — | 1 | 7.13 |
| CHEMBL4639814 | — | — | 1 | 7.12 |
| CHEMBL4634934 | — | — | 1 | 6.96 |
| CHEMBL4645184 | — | — | 1 | 6.83 |
| CHEMBL4636336 | — | — | 1 | 6.73 |
| CHEMBL4648586 | — | — | 1 | 6.55 |
| CHEMBL4643380 | — | — | 1 | 6.53 |
| CHEMBL4634776 | — | — | 1 | 6.50 |
| CHEMBL4633748 | — | — | 1 | 6.48 |
| CHEMBL4647526 | — | — | 1 | 6.04 |
| CHEMBL1373 | MODAFINIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4641869 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL4640152 | — | Ki | = | 2.19 | nM | 8.66 |
| CHEMBL4638977 | — | Ki | = | 2.58 | nM | 8.59 |
| CHEMBL4647283 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL4636778 | — | Ki | = | 5.62 | nM | 8.25 |
| CHEMBL4647200 | — | Ki | = | 5.95 | nM | 8.22 |
| CHEMBL4647914 | — | Ki | = | 7.72 | nM | 8.11 |
| CHEMBL4635589 | — | Ki | = | 9.65 | nM | 8.02 |
| CHEMBL4640772 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL4643955 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL4649604 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL4643859 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL4635958 | — | Ki | = | 29.4 | nM | 7.53 |
| CHEMBL4648300 | — | Ki | = | 31.8 | nM | 7.50 |
| CHEMBL4638203 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL4645855 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL4640372 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL4634263 | — | Ki | = | 65.1 | nM | 7.19 |
| CHEMBL4642082 | — | Ki | = | 73.7 | nM | 7.13 |
| CHEMBL4639814 | — | Ki | = | 75.4 | nM | 7.12 |
| CHEMBL4634934 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL4645184 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4636336 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL4648586 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL4643380 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL4634776 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL4633748 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL4647526 | — | Ki | = | 902.0 | nM | 6.04 |
| CHEMBL1373 | MODAFINIL | Ki | - | — | - |