Assay Detail
Binding
CHEMBL2173633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in guinea pig brain membranes after 120 mins by scintillation counter
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 72 | 6.90 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170235 | — | — | 1 | 8.06 |
| CHEMBL2170211 | — | — | 1 | 8.05 |
| CHEMBL2170222 | — | — | 1 | 7.90 |
| CHEMBL2170207 | — | — | 1 | 7.85 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.66 |
| CHEMBL2170238 | — | — | 1 | 7.62 |
| CHEMBL2170224 | — | — | 1 | 7.57 |
| CHEMBL2170212 | — | — | 1 | 7.48 |
| CHEMBL2170219 | — | — | 1 | 7.43 |
| CHEMBL2170072 | — | — | 1 | 7.34 |
| CHEMBL2170205 | — | — | 1 | 7.33 |
| CHEMBL2170223 | — | — | 1 | 7.32 |
| CHEMBL2170217 | — | — | 1 | 7.21 |
| CHEMBL2170228 | — | — | 1 | 7.20 |
| CHEMBL2170239 | — | — | 1 | 7.19 |
| CHEMBL2170206 | — | — | 1 | 7.18 |
| CHEMBL2170067 | — | — | 1 | 7.07 |
| CHEMBL2170054 | — | — | 1 | 7.04 |
| CHEMBL2170071 | — | — | 1 | 6.99 |
| CHEMBL2170204 | — | — | 1 | 6.98 |
| CHEMBL2170203 | — | — | 1 | 6.82 |
| CHEMBL2170229 | — | — | 1 | 6.79 |
| CHEMBL2170218 | — | — | 1 | 6.77 |
| CHEMBL2170227 | — | — | 1 | 6.68 |
| CHEMBL2170049 | — | — | 1 | 6.65 |
| CHEMBL2170221 | — | — | 1 | 6.61 |
| CHEMBL2170234 | — | — | 1 | 6.60 |
| CHEMBL2170237 | — | — | 1 | 6.55 |
| CHEMBL2170220 | — | — | 1 | 6.51 |
| CHEMBL73824 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170235 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL2170211 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL2170222 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL2170207 | — | Ki | = | 14.2 | nM | 7.85 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2170238 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL2170224 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL2170212 | — | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL2170219 | — | Ki | = | 37.2 | nM | 7.43 |
| CHEMBL2170072 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL2170205 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL2170223 | — | Ki | = | 47.5 | nM | 7.32 |
| CHEMBL2170217 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL2170228 | — | Ki | = | 63.5 | nM | 7.20 |
| CHEMBL2170239 | — | Ki | = | 64.7 | nM | 7.19 |
| CHEMBL2170206 | — | Ki | = | 66.3 | nM | 7.18 |
| CHEMBL2170067 | — | Ki | = | 84.7 | nM | 7.07 |
| CHEMBL2170054 | — | Ki | = | 90.5 | nM | 7.04 |
| CHEMBL2170071 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL2170204 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL2170203 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL2170229 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL2170218 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2170227 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL2170049 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL2170221 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL2170234 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2170237 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2170220 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL73824 | — | Ki | = | 318.4 | nM | 6.50 |
| CHEMBL2170050 | — | Ki | = | 324.0 | nM | 6.49 |
| CHEMBL2170055 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL2170076 | — | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL2170060 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL2169891 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL2170068 | — | Ki | = | 395.0 | nM | 6.40 |
| CHEMBL2170048 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL2170230 | — | Ki | = | 435.0 | nM | 6.36 |
| CHEMBL2170226 | — | Ki | = | 483.0 | nM | 6.32 |
| CHEMBL2170233 | — | Ki | = | 563.0 | nM | 6.25 |
| CHEMBL2170053 | — | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL2170069 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL2170216 | — | Ki | = | 638.0 | nM | 6.20 |
| CHEMBL2170075 | — | Ki | = | 829.0 | nM | 6.08 |
| CHEMBL2170051 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170231 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170232 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170225 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170045 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170052 | — | Ki | > | 1000.0 | nM | - |