Assay Detail
Binding
CHEMBL3300408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis
26
Total Activities
26
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
Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.46 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2435438 | — | — | 1 | 9.02 |
| CHEMBL2435435 | — | — | 1 | 8.62 |
| CHEMBL3298974 | — | — | 1 | 8.55 |
| CHEMBL3298973 | — | — | 1 | 8.35 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.25 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL2435426 | — | — | 1 | 7.96 |
| CHEMBL2435437 | — | — | 1 | 7.72 |
| CHEMBL2435441 | — | — | 1 | 7.72 |
| CHEMBL2435433 | — | — | 1 | 7.66 |
| CHEMBL2435425 | — | — | 1 | 7.54 |
| CHEMBL2435427 | — | — | 1 | 7.43 |
| CHEMBL2435443 | — | — | 1 | 7.37 |
| CHEMBL2435440 | — | — | 1 | 7.26 |
| CHEMBL2435424 | — | — | 1 | 7.12 |
| CHEMBL2435432 | — | — | 1 | 7.08 |
| CHEMBL2435431 | — | — | 1 | 7.08 |
| CHEMBL3298885 | — | — | 1 | 7.07 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL3298884 | — | — | 1 | 6.95 |
| CHEMBL2435442 | — | — | 1 | 6.94 |
| CHEMBL2435439 | — | — | 1 | 6.92 |
| CHEMBL2435428 | — | — | 1 | 6.78 |
| CHEMBL2435434 | — | — | 1 | 6.72 |
| CHEMBL2435429 | — | — | 1 | 6.63 |
| CHEMBL2435430 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2435438 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL2435435 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3298974 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3298973 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL2435426 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2435437 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2435441 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2435433 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2435425 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2435427 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL2435443 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2435440 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2435424 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2435432 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL2435431 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL3298885 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3298884 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL2435442 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL2435439 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL2435428 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL2435434 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL2435429 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL2435430 | — | Ki | = | 805.0 | nM | 6.09 |