Assay Detail
Binding
CHEMBL4044920
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 membranes after 120 mins by liquid scintillation counting
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| 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
Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ1 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 7.92 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062642 | — | — | 1 | 9.66 |
| CHEMBL4063826 | — | — | 1 | 9.43 |
| CHEMBL4084334 | — | — | 1 | 9.42 |
| CHEMBL4065105 | — | — | 1 | 9.29 |
| CHEMBL310240 | — | — | 1 | 9.26 |
| CHEMBL4090896 | — | — | 1 | 9.21 |
| CHEMBL4094304 | — | — | 1 | 9.11 |
| CHEMBL4073697 | — | — | 1 | 9.08 |
| CHEMBL4086541 | — | — | 1 | 9.07 |
| CHEMBL4100774 | — | — | 1 | 8.96 |
| CHEMBL4090350 | — | — | 1 | 8.43 |
| CHEMBL4080042 | — | — | 1 | 8.41 |
| CHEMBL4074010 | — | — | 1 | 8.31 |
| CHEMBL4098070 | — | — | 1 | 8.30 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.24 |
| CHEMBL4099831 | — | — | 1 | 8.22 |
| CHEMBL4077463 | — | — | 1 | 8.21 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4075547 | — | — | 1 | 7.89 |
| CHEMBL4078697 | — | — | 1 | 7.75 |
| CHEMBL4081826 | — | — | 1 | 7.70 |
| CHEMBL4102976 | — | — | 1 | 7.68 |
| CHEMBL4066655 | — | — | 1 | 7.60 |
| CHEMBL4087471 | — | — | 1 | 7.57 |
| CHEMBL4093254 | — | — | 1 | 7.55 |
| CHEMBL4083666 | — | — | 1 | 7.54 |
| CHEMBL477036 | — | — | 1 | 7.42 |
| CHEMBL4094187 | — | — | 1 | 7.42 |
| CHEMBL4078572 | — | — | 1 | 7.40 |
| CHEMBL4097642 | — | — | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062642 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL4063826 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL4084334 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL4065105 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL310240 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL4090896 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL4094304 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL4073697 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL4086541 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL4100774 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4090350 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4080042 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4074010 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4098070 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL4099831 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4077463 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4075547 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4078697 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4081826 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4102976 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4066655 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4087471 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4093254 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4083666 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL477036 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4094187 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4078572 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4097642 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4087925 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4075270 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4071325 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4101921 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL4093286 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4084922 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL4062428 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4059616 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL4077164 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL4069312 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL4065245 | — | Ki | = | 448.0 | nM | 6.35 |
| CHEMBL4061903 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4068411 | — | Ki | > | 1000.0 | nM | - |