Assay Detail
Binding
CHEMBL2350909
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis
32
Total Activities
32
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
Improvement of σ1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.45 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138809 | — | — | 1 | 8.96 |
| CHEMBL141209 | — | — | 1 | 8.89 |
| CHEMBL2349454 | — | — | 1 | 8.60 |
| CHEMBL2349459 | — | — | 1 | 8.28 |
| CHEMBL2349446 | — | — | 1 | 8.28 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL2349443 | — | — | 1 | 8.20 |
| CHEMBL2349441 | — | — | 1 | 8.05 |
| CHEMBL2349455 | — | — | 1 | 7.96 |
| CHEMBL2349456 | — | — | 1 | 7.96 |
| CHEMBL2349461 | — | — | 1 | 7.96 |
| CHEMBL2349453 | — | — | 1 | 7.80 |
| CHEMBL343793 | — | — | 1 | 7.68 |
| CHEMBL2349458 | — | — | 1 | 7.64 |
| CHEMBL138286 | — | — | 1 | 7.54 |
| CHEMBL2346692 | — | — | 1 | 7.40 |
| CHEMBL2349460 | — | — | 1 | 7.37 |
| CHEMBL2349555 | — | — | 1 | 7.06 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL2349457 | — | — | 1 | 6.97 |
| CHEMBL2349442 | — | — | 1 | 6.80 |
| CHEMBL2349444 | — | — | 1 | 6.72 |
| CHEMBL2349452 | — | — | 1 | 6.59 |
| CHEMBL2349450 | — | — | 1 | 6.40 |
| CHEMBL2349554 | — | — | 1 | 6.32 |
| CHEMBL2349447 | — | — | 1 | 6.19 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | 6.18 |
| CHEMBL2349448 | — | — | 1 | 6.11 |
| CHEMBL2349449 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138809 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL141209 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2349454 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2349459 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2349446 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2349443 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2349441 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2349455 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2349456 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2349461 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2349453 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL343793 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2349458 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL138286 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2346692 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2349460 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2349555 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL2349457 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL2349442 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL2349444 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2349452 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL2349450 | — | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL2349554 | — | Ki | = | 483.0 | nM | 6.32 |
| CHEMBL2349447 | — | Ki | = | 639.0 | nM | 6.19 |
| CHEMBL103 | PROGESTERONE | Ki | = | 661.0 | nM | 6.18 |
| CHEMBL2349448 | — | Ki | = | 784.0 | nM | 6.11 |
| CHEMBL2349449 | — | Ki | = | 777.0 | nM | 6.11 |
| CHEMBL2349451 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2349445 | — | Ki | > | 1000.0 | nM | - |