Assay Detail
Binding
CHEMBL915240
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Displacement of [3H](+)-pentazocine from guinea pig brain sigma 1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Novel sigma receptor ligands: synthesis and biological profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.45 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375499 | — | — | 1 | 9.17 |
| CHEMBL225516 | — | — | 1 | 9.09 |
| CHEMBL374686 | — | — | 1 | 9.01 |
| CHEMBL426724 | — | — | 1 | 9.00 |
| CHEMBL222301 | — | — | 1 | 8.82 |
| CHEMBL222445 | — | — | 1 | 8.77 |
| CHEMBL222235 | — | — | 1 | 8.72 |
| CHEMBL222236 | — | — | 1 | 8.66 |
| CHEMBL385795 | — | — | 1 | 8.51 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL221348 | — | — | 1 | 8.51 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.39 |
| CHEMBL222287 | IBOGAINE | 2.0 | 1 | 6.60 |
| CHEMBL221347 | — | — | 1 | 6.46 |
| CHEMBL222394 | — | — | 1 | 6.45 |
| CHEMBL386002 | — | — | 1 | 6.30 |
| CHEMBL225653 | — | — | 1 | 6.21 |
| CHEMBL222307 | — | — | 1 | 6.15 |
| CHEMBL222444 | — | — | 1 | 6.11 |
| CHEMBL386931 | — | — | 1 | 5.90 |
| CHEMBL222736 | — | — | 1 | 5.88 |
| CHEMBL434385 | — | — | 1 | 5.69 |
| CHEMBL373686 | — | — | 1 | 5.51 |
| CHEMBL221370 | — | — | 1 | - |
| CHEMBL374814 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375499 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL225516 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL374686 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL426724 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL222301 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL222445 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL222235 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL222236 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL385795 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL221348 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL222287 | IBOGAINE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL221347 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL222394 | — | Ki | = | 353.0 | nM | 6.45 |
| CHEMBL386002 | — | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL225653 | — | Ki | = | 619.0 | nM | 6.21 |
| CHEMBL222307 | — | Ki | = | 707.0 | nM | 6.15 |
| CHEMBL222444 | — | Ki | = | 769.0 | nM | 6.11 |
| CHEMBL386931 | — | Ki | = | 1255.0 | nM | 5.90 |
| CHEMBL222736 | — | Ki | = | 1328.0 | nM | 5.88 |
| CHEMBL434385 | — | Ki | = | 2028.0 | nM | 5.69 |
| CHEMBL373686 | — | Ki | = | 3088.0 | nM | 5.51 |
| CHEMBL221370 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL374814 | — | Ki | > | 10000.0 | nM | - |