Assay Detail
Binding
CHEMBL5365002
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 membrane assessed as inhibition constant measured after 120 mins by scintillation counting method
25
Total Activities
25
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
Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.57 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5421604 | — | — | 1 | 8.57 |
| CHEMBL5432456 | — | — | 1 | 8.38 |
| CHEMBL5435194 | — | — | 1 | 8.18 |
| CHEMBL5410173 | — | — | 1 | 8.12 |
| CHEMBL5398972 | — | — | 1 | 8.06 |
| CHEMBL5423529 | — | — | 1 | 8.00 |
| CHEMBL5410339 | — | — | 1 | 7.92 |
| CHEMBL5435626 | — | — | 1 | 7.92 |
| CHEMBL5406518 | — | — | 1 | 7.77 |
| CHEMBL5425955 | — | — | 1 | 7.70 |
| CHEMBL5431988 | — | — | 1 | 7.68 |
| CHEMBL5403196 | — | — | 1 | 7.64 |
| CHEMBL5429038 | — | — | 1 | 7.58 |
| CHEMBL114644 | — | — | 1 | 7.58 |
| CHEMBL5394862 | — | — | 1 | 7.50 |
| CHEMBL5441115 | — | — | 1 | 7.44 |
| CHEMBL5396018 | — | — | 1 | 7.40 |
| CHEMBL5432037 | — | — | 1 | 7.26 |
| CHEMBL5409908 | — | — | 1 | 7.24 |
| CHEMBL5435354 | — | — | 1 | 7.24 |
| CHEMBL5408501 | — | — | 1 | 7.11 |
| CHEMBL5417143 | — | — | 1 | 7.07 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL5416753 | — | — | 1 | 6.65 |
| CHEMBL5440346 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5421604 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5432456 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL5435194 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL5410173 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL5398972 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL5423529 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5410339 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5435626 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5406518 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5425955 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5431988 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5403196 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5429038 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL114644 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5394862 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5441115 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5396018 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5432037 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL5409908 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL5435354 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL5408501 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5417143 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL5416753 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL5440346 | — | Ki | = | 562.0 | nM | 6.25 |