Assay Detail
Binding
CHEMBL3238586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma 2 receptor in Dunkin Hartley guinea pig membrane after 120 mins by liquid scintillation counting analysis in the presence of sigma 1 receptor blocker (-)-SKF-10047
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 6.40 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.44 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.31 |
| CHEMBL3235453 | — | — | 1 | 7.01 |
| CHEMBL3235444 | — | — | 1 | 7.01 |
| CHEMBL3235437 | — | — | 1 | 7.00 |
| CHEMBL3235449 | — | — | 1 | 6.79 |
| CHEMBL3235452 | — | — | 1 | 6.69 |
| CHEMBL3235441 | — | — | 1 | 6.58 |
| CHEMBL3235456 | — | — | 1 | 6.54 |
| CHEMBL3235461 | — | — | 1 | 6.51 |
| CHEMBL3235447 | — | — | 1 | 6.50 |
| CHEMBL3235457 | — | — | 1 | 6.45 |
| CHEMBL3235460 | — | — | 1 | 6.39 |
| CHEMBL3235442 | — | — | 1 | 6.37 |
| CHEMBL3235433 | — | — | 1 | 6.33 |
| CHEMBL3235434 | — | — | 1 | 6.28 |
| CHEMBL3235451 | — | — | 1 | 6.26 |
| CHEMBL3235446 | — | — | 1 | 6.18 |
| CHEMBL3235458 | — | — | 1 | 6.12 |
| CHEMBL3235454 | — | — | 1 | 6.08 |
| CHEMBL3235459 | — | — | 1 | 6.02 |
| CHEMBL3235440 | — | — | 1 | 5.95 |
| CHEMBL3235438 | — | — | 1 | 5.92 |
| CHEMBL3235455 | — | — | 1 | 5.89 |
| CHEMBL3235448 | — | — | 1 | 5.75 |
| CHEMBL3235435 | — | — | 1 | 5.74 |
| CHEMBL3235436 | — | — | 1 | 5.70 |
| CHEMBL3235450 | — | — | 1 | - |
| CHEMBL3235432 | — | — | 1 | - |
| CHEMBL2170062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 36.4 | nM | 7.44 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 49.2 | nM | 7.31 |
| CHEMBL3235453 | — | Ki | = | 97.2 | nM | 7.01 |
| CHEMBL3235444 | — | Ki | = | 98.1 | nM | 7.01 |
| CHEMBL3235437 | — | Ki | = | 100.4 | nM | 7.00 |
| CHEMBL3235449 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL3235452 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL3235441 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3235456 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL3235461 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL3235447 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL3235457 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL3235460 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL3235442 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL3235433 | — | Ki | = | 471.0 | nM | 6.33 |
| CHEMBL3235434 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL3235451 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL3235446 | — | Ki | = | 662.0 | nM | 6.18 |
| CHEMBL3235458 | — | Ki | = | 755.0 | nM | 6.12 |
| CHEMBL3235454 | — | Ki | = | 825.0 | nM | 6.08 |
| CHEMBL3235459 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL3235440 | — | Ki | = | 1122.0 | nM | 5.95 |
| CHEMBL3235438 | — | Ki | = | 1205.0 | nM | 5.92 |
| CHEMBL3235455 | — | Ki | = | 1301.0 | nM | 5.89 |
| CHEMBL3235448 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL3235435 | — | Ki | = | 1811.0 | nM | 5.74 |
| CHEMBL3235436 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL3235450 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3235432 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2170062 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3235439 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3235445 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3235443 | — | Ki | > | 2000.0 | nM | - |