Assay Detail
Binding
CHEMBL753407
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Inhibitory activity against Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cells membranes was determined using [3H]-DAMGO radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.87 | 10.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.21 |
| CHEMBL147511 | — | — | 1 | 10.05 |
| CHEMBL413512 | — | — | 1 | 9.85 |
| CHEMBL433697 | — | — | 1 | 9.80 |
| CHEMBL146756 | — | — | 1 | 9.70 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 9.68 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 9.64 |
| CHEMBL357334 | — | — | 1 | 9.64 |
| CHEMBL150061 | — | — | 1 | 9.55 |
| CHEMBL405131 | — | — | 1 | 9.05 |
| CHEMBL358104 | — | — | 1 | 9.03 |
| CHEMBL346436 | — | — | 1 | 9.01 |
| CHEMBL424328 | — | — | 1 | 8.74 |
| CHEMBL346885 | — | — | 1 | 8.48 |
| CHEMBL435084 | — | — | 1 | 8.48 |
| CHEMBL149074 | — | — | 1 | 8.33 |
| CHEMBL318859 | ENADOLINE | 2.0 | 1 | 7.66 |
| CHEMBL348023 | — | — | 1 | 7.54 |
| CHEMBL424327 | — | — | 1 | 7.32 |
| CHEMBL356889 | — | — | 1 | 7.28 |
| CHEMBL151872 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL147511 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL413512 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL433697 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL146756 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL357334 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL150061 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL405131 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL358104 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL346436 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL424328 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL346885 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL435084 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL149074 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL318859 | ENADOLINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL348023 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL424327 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL356889 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL151872 | — | Ki | = | 66.0 | nM | 7.18 |