Assay Detail
Binding
CHEMBL3238585
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Dunkin Hartley guinea pig membrane after 180 mins by liquid scintillation counting analysis
33
Total Activities
33
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 and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.61 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3235459 | — | — | 1 | 9.11 |
| CHEMBL3235447 | — | — | 1 | 8.96 |
| CHEMBL3235455 | — | — | 1 | 8.91 |
| CHEMBL3235458 | — | — | 1 | 8.83 |
| CHEMBL3235454 | — | — | 1 | 8.77 |
| CHEMBL3235446 | — | — | 1 | 8.73 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.47 |
| CHEMBL3235449 | — | — | 1 | 8.37 |
| CHEMBL2170062 | — | — | 1 | 7.98 |
| CHEMBL3235433 | — | — | 1 | 7.83 |
| CHEMBL3235437 | — | — | 1 | 7.67 |
| CHEMBL3235441 | — | — | 1 | 7.65 |
| CHEMBL3235451 | — | — | 1 | 7.62 |
| CHEMBL3235457 | — | — | 1 | 7.46 |
| CHEMBL3235453 | — | — | 1 | 7.41 |
| CHEMBL3235461 | — | — | 1 | 7.40 |
| CHEMBL3235444 | — | — | 1 | 7.40 |
| CHEMBL3235438 | — | — | 1 | 7.35 |
| CHEMBL3235434 | — | — | 1 | 7.22 |
| CHEMBL3235460 | — | — | 1 | 7.18 |
| CHEMBL3235442 | — | — | 1 | 7.15 |
| CHEMBL3235452 | — | — | 1 | 7.08 |
| CHEMBL3235435 | — | — | 1 | 7.05 |
| CHEMBL3235456 | — | — | 1 | 7.05 |
| CHEMBL3235448 | — | — | 1 | 7.01 |
| CHEMBL3235445 | — | — | 1 | 6.71 |
| CHEMBL3235450 | — | — | 1 | 6.47 |
| CHEMBL3235436 | — | — | 1 | 6.17 |
| CHEMBL3235440 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3235459 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL3235447 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3235455 | — | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL3235458 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL3235454 | — | Ki | = | 1.69 | nM | 8.77 |
| CHEMBL3235446 | — | Ki | = | 1.84 | nM | 8.73 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3235449 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2170062 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL3235433 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL3235437 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL3235441 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL3235451 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL3235457 | — | Ki | = | 34.3 | nM | 7.46 |
| CHEMBL3235453 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL3235461 | — | Ki | = | 40.2 | nM | 7.40 |
| CHEMBL3235444 | — | Ki | = | 40.2 | nM | 7.40 |
| CHEMBL3235438 | — | Ki | = | 44.8 | nM | 7.35 |
| CHEMBL3235434 | — | Ki | = | 60.2 | nM | 7.22 |
| CHEMBL3235460 | — | Ki | = | 66.7 | nM | 7.18 |
| CHEMBL3235442 | — | Ki | = | 70.7 | nM | 7.15 |
| CHEMBL3235452 | — | Ki | = | 83.2 | nM | 7.08 |
| CHEMBL3235435 | — | Ki | = | 88.4 | nM | 7.05 |
| CHEMBL3235456 | — | Ki | = | 89.1 | nM | 7.05 |
| CHEMBL3235448 | — | Ki | = | 98.2 | nM | 7.01 |
| CHEMBL3235445 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL3235450 | — | Ki | = | 340.9 | nM | 6.47 |
| CHEMBL3235436 | — | Ki | = | 682.0 | nM | 6.17 |
| CHEMBL3235440 | — | Ki | = | 792.0 | nM | 6.10 |
| CHEMBL3235443 | — | Ki | = | 852.0 | nM | 6.07 |
| CHEMBL3235439 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3235432 | — | Ki | > | 2000.0 | nM | - |