Assay Detail
Binding
CHEMBL752737
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Inhibitory activity against Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]U-69593 radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 9.11 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.47 |
| CHEMBL147511 | — | — | 1 | 10.31 |
| CHEMBL357334 | — | — | 1 | 10.15 |
| CHEMBL433697 | — | — | 1 | 10.12 |
| CHEMBL146756 | — | — | 1 | 10.11 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 10.10 |
| CHEMBL413512 | — | — | 1 | 10.00 |
| CHEMBL150061 | — | — | 1 | 9.77 |
| CHEMBL318859 | ENADOLINE | 2.0 | 1 | 9.57 |
| CHEMBL358104 | — | — | 1 | 9.39 |
| CHEMBL346436 | — | — | 1 | 9.23 |
| CHEMBL405131 | — | — | 1 | 9.19 |
| CHEMBL424328 | — | — | 1 | 8.96 |
| CHEMBL346885 | — | — | 1 | 8.92 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 8.64 |
| CHEMBL435084 | — | — | 1 | 8.47 |
| CHEMBL149074 | — | — | 1 | 8.38 |
| CHEMBL348023 | — | — | 1 | 7.75 |
| CHEMBL424327 | — | — | 1 | 7.62 |
| CHEMBL356889 | — | — | 1 | 7.30 |
| CHEMBL151872 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL147511 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL357334 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL433697 | — | Ki | = | 0.076 | nM | 10.12 |
| CHEMBL146756 | — | Ki | = | 0.078 | nM | 10.11 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.079 | nM | 10.10 |
| CHEMBL413512 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL150061 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL318859 | ENADOLINE | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL358104 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL346436 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL405131 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL424328 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL346885 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL435084 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL149074 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL348023 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL424327 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL356889 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL151872 | — | Ki | = | 120.0 | nM | 6.92 |