Assay Detail
Binding
CHEMBL4158748
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method
42
Total Activities
42
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
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.00 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53325 | — | — | 1 | 9.42 |
| CHEMBL4171436 | — | — | 1 | 8.36 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.27 |
| CHEMBL4175947 | — | — | 1 | 8.20 |
| CHEMBL4159233 | — | — | 1 | 7.92 |
| CHEMBL4170683 | — | — | 1 | 7.92 |
| CHEMBL4168393 | — | — | 1 | 7.92 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.77 |
| CHEMBL4170858 | — | — | 1 | 7.72 |
| CHEMBL4160847 | — | — | 1 | 7.55 |
| CHEMBL4169479 | — | — | 1 | 7.33 |
| CHEMBL4172125 | — | — | 1 | 7.21 |
| CHEMBL4170826 | — | — | 1 | 7.11 |
| CHEMBL4159761 | — | — | 1 | 6.80 |
| CHEMBL4165978 | — | — | 1 | 6.70 |
| CHEMBL4167468 | — | — | 1 | 6.58 |
| CHEMBL4169156 | — | — | 1 | 6.46 |
| CHEMBL4164220 | — | — | 1 | 6.27 |
| CHEMBL4164248 | — | — | 1 | 6.26 |
| CHEMBL4176252 | — | — | 1 | 6.26 |
| CHEMBL4161557 | — | — | 1 | 6.23 |
| CHEMBL4164032 | — | — | 1 | 6.20 |
| CHEMBL4160820 | — | — | 1 | 6.19 |
| CHEMBL4159559 | — | — | 1 | 6.18 |
| CHEMBL4167670 | — | — | 1 | 6.13 |
| CHEMBL4162917 | — | — | 1 | 6.09 |
| CHEMBL4162745 | — | — | 1 | 6.01 |
| CHEMBL291439 | — | — | 1 | 4.89 |
| CHEMBL4171757 | — | — | 1 | - |
| CHEMBL4168095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53325 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL4171436 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL4175947 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4159233 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4170683 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4168393 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL61479 | SIRAMESINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4170858 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4160847 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4169479 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4172125 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4170826 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4159761 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL4165978 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL4167468 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL4169156 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL4164220 | — | Ki | = | 538.0 | nM | 6.27 |
| CHEMBL4164248 | — | Ki | = | 548.0 | nM | 6.26 |
| CHEMBL4176252 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL4161557 | — | Ki | = | 583.0 | nM | 6.23 |
| CHEMBL4164032 | — | Ki | = | 635.0 | nM | 6.20 |
| CHEMBL4160820 | — | Ki | = | 639.0 | nM | 6.19 |
| CHEMBL4159559 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL4167670 | — | Ki | = | 736.0 | nM | 6.13 |
| CHEMBL4162917 | — | Ki | = | 807.0 | nM | 6.09 |
| CHEMBL4162745 | — | Ki | = | 966.0 | nM | 6.01 |
| CHEMBL291439 | — | Ki | = | 12900.0 | nM | 4.89 |
| CHEMBL4167697 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4169879 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4168777 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4175973 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4165358 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4175566 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4174291 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4166375 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4161150 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4174683 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4172875 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4161237 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4168095 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4171757 | — | Ki | > | 1000.0 | nM | - |