Assay Detail
Binding
CHEMBL4841080
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Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of an <i>M</i>-Substituted <i>N</i>-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.62 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4859512 | — | — | 1 | 10.80 |
| CHEMBL4449252 | — | — | 1 | 9.33 |
| CHEMBL4864911 | — | — | 1 | 8.22 |
| CHEMBL58033 | (-)-U-50488 | — | 1 | 8.21 |
| CHEMBL4876542 | — | — | 1 | 8.18 |
| CHEMBL4848808 | — | — | 1 | 8.15 |
| CHEMBL4860416 | — | — | 1 | 8.14 |
| CHEMBL4873458 | — | — | 1 | 8.10 |
| CHEMBL4875933 | — | — | 1 | 8.01 |
| CHEMBL4860580 | — | — | 1 | 7.93 |
| CHEMBL4870433 | — | — | 1 | 7.86 |
| CHEMBL4862968 | — | — | 1 | 7.86 |
| CHEMBL4874064 | — | — | 1 | 7.79 |
| CHEMBL4857172 | — | — | 1 | 7.43 |
| CHEMBL4851681 | — | — | 1 | 7.34 |
| CHEMBL4858515 | — | — | 1 | 7.33 |
| CHEMBL4858270 | — | — | 1 | 7.31 |
| CHEMBL4850589 | — | — | 1 | 7.29 |
| CHEMBL4863358 | — | — | 1 | 7.25 |
| CHEMBL4857175 | — | — | 1 | 7.21 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.11 |
| CHEMBL4870917 | — | — | 1 | 7.03 |
| CHEMBL4856092 | — | — | 1 | 6.70 |
| CHEMBL4861737 | — | — | 1 | 6.68 |
| CHEMBL4876239 | — | — | 1 | 6.65 |
| CHEMBL4851082 | — | — | 1 | 6.62 |
| CHEMBL4870270 | — | — | 1 | 6.57 |
| CHEMBL4879175 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4859512 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL4449252 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL4864911 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL58033 | (-)-U-50488 | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL4876542 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4848808 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL4860416 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL4873458 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4875933 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL4860580 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4870433 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL4862968 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL4874064 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL4857172 | — | Ki | = | 37.4 | nM | 7.43 |
| CHEMBL4851681 | — | Ki | = | 45.6 | nM | 7.34 |
| CHEMBL4858515 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL4858270 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL4850589 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4863358 | — | Ki | = | 56.2 | nM | 7.25 |
| CHEMBL4857175 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL70 | MORPHINE | Ki | = | 76.9 | nM | 7.11 |
| CHEMBL4870917 | — | Ki | = | 93.8 | nM | 7.03 |
| CHEMBL4856092 | — | Ki | = | 200.2 | nM | 6.70 |
| CHEMBL4861737 | — | Ki | = | 206.5 | nM | 6.68 |
| CHEMBL4876239 | — | Ki | = | 224.5 | nM | 6.65 |
| CHEMBL4851082 | — | Ki | = | 242.7 | nM | 6.62 |
| CHEMBL4870270 | — | Ki | = | 268.1 | nM | 6.57 |
| CHEMBL4879175 | — | Ki | = | 423.3 | nM | 6.37 |