Assay Detail
Binding
CHEMBL4675309
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69,593 from kappa opioid receptor in guinea-pig brain membranes incubated for 30 mins by liquid scintillation counting method
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 6.99 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4788003 | — | — | 1 | 8.06 |
| CHEMBL607405 | — | — | 1 | 7.99 |
| CHEMBL4793888 | — | — | 1 | 7.90 |
| CHEMBL4755067 | — | — | 1 | 7.60 |
| CHEMBL4754944 | — | — | 1 | 7.54 |
| CHEMBL4741873 | — | — | 1 | 7.47 |
| CHEMBL4753934 | — | — | 1 | 7.40 |
| CHEMBL1672084 | — | — | 1 | 7.37 |
| CHEMBL4755734 | — | — | 1 | 7.35 |
| CHEMBL4743953 | — | — | 1 | 7.34 |
| CHEMBL4740360 | — | — | 1 | 7.30 |
| CHEMBL4763643 | — | — | 1 | 7.20 |
| CHEMBL4789014 | — | — | 1 | 7.16 |
| CHEMBL4757463 | — | — | 1 | 7.15 |
| CHEMBL4777389 | — | — | 1 | 7.15 |
| CHEMBL4761784 | — | — | 1 | 7.13 |
| CHEMBL4757240 | — | — | 1 | 7.12 |
| CHEMBL4761211 | — | — | 1 | 7.06 |
| CHEMBL4760163 | — | — | 1 | 6.99 |
| CHEMBL4750229 | — | — | 1 | 6.93 |
| CHEMBL4783612 | — | — | 1 | 6.86 |
| CHEMBL4780909 | — | — | 1 | 6.85 |
| CHEMBL4782642 | — | — | 1 | 6.85 |
| CHEMBL4797321 | — | — | 1 | 6.84 |
| CHEMBL4740464 | — | — | 1 | 6.83 |
| CHEMBL4795312 | — | — | 1 | 6.82 |
| CHEMBL4788604 | — | — | 1 | 6.82 |
| CHEMBL4795517 | — | — | 1 | 6.80 |
| CHEMBL4748047 | — | — | 1 | 6.75 |
| CHEMBL4776879 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4788003 | — | Ki | = | 8.66 | nM | 8.06 |
| CHEMBL607405 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL4793888 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL4755067 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4754944 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL4741873 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL4753934 | — | Ki | = | 39.5 | nM | 7.40 |
| CHEMBL1672084 | — | Ki | = | 43.2 | nM | 7.37 |
| CHEMBL4755734 | — | Ki | = | 44.8 | nM | 7.35 |
| CHEMBL4743953 | — | Ki | = | 45.6 | nM | 7.34 |
| CHEMBL4740360 | — | Ki | = | 50.2 | nM | 7.30 |
| CHEMBL4763643 | — | Ki | = | 63.7 | nM | 7.20 |
| CHEMBL4789014 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4757463 | — | Ki | = | 71.4 | nM | 7.15 |
| CHEMBL4777389 | — | Ki | = | 71.5 | nM | 7.15 |
| CHEMBL4761784 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL4757240 | — | Ki | = | 76.4 | nM | 7.12 |
| CHEMBL4761211 | — | Ki | = | 87.2 | nM | 7.06 |
| CHEMBL4760163 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL4750229 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL4783612 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL4780909 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL4782642 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL4797321 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4740464 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4795312 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL4788604 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL4795517 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL4748047 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL4776879 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL4745745 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL4741308 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL4781006 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL4741203 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL4754111 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL4763225 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL4782629 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL4793953 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL4755501 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL4747179 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL4792012 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL4740918 | — | Ki | = | 1252.0 | nM | 5.90 |