Assay Detail
Binding
CHEMBL753174
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Inhibition of radioligand [3H]U-69593 binding to kappa 1 receptor of guinea pig brain
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.03 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38791 | — | — | 2 | 6.31 |
| CHEMBL110319 | — | — | 1 | 6.24 |
| CHEMBL2111684 | — | — | 1 | 6.05 |
| CHEMBL3350264 | — | — | 1 | 5.96 |
| CHEMBL2111686 | — | — | 1 | 5.60 |
| CHEMBL109160 | — | — | 1 | - |
| CHEMBL2008608 | — | — | 1 | - |
| CHEMBL2111685 | — | — | 1 | - |
| CHEMBL322468 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38791 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL110319 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL2111684 | — | Ki | = | 889.0 | nM | 6.05 |
| CHEMBL38791 | — | Ki | = | 1013.0 | nM | 5.99 |
| CHEMBL3350264 | — | Ki | = | 1091.0 | nM | 5.96 |
| CHEMBL2111686 | — | Ki | = | 2536.0 | nM | 5.60 |
| CHEMBL109160 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2008608 | — | Ki | > | 500.0 | nM | - |
| CHEMBL2111685 | — | Ki | > | 500.0 | nM | - |
| CHEMBL322468 | — | Ki | > | 500.0 | nM | - |