Assay Detail
Binding
CHEMBL744597
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Inhibition of radioligand [3H]DAMGO binding to rat brain mu receptor
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 7.66 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2008608 | — | — | 1 | 8.35 |
| CHEMBL38791 | — | — | 2 | 8.26 |
| CHEMBL322468 | — | — | 1 | 8.21 |
| CHEMBL110319 | — | — | 1 | 7.47 |
| CHEMBL2111686 | — | — | 1 | 7.45 |
| CHEMBL3350264 | — | — | 1 | 7.42 |
| CHEMBL2111685 | — | — | 1 | 7.35 |
| CHEMBL2111684 | — | — | 1 | 6.41 |
| CHEMBL109160 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2008608 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL38791 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL322468 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL38791 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL110319 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL2111686 | — | Ki | = | 35.5 | nM | 7.45 |
| CHEMBL3350264 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL2111685 | — | Ki | = | 45.1 | nM | 7.35 |
| CHEMBL2111684 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL109160 | — | Ki | > | 700.0 | nM | - |