Assay Detail
Binding
CHEMBL754735
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Binding affinity for the Opioid receptor kappa 1
33
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.29 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL538309 | — | — | 1 | 8.51 |
| CHEMBL544960 | — | — | 3 | 8.43 |
| CHEMBL556957 | — | — | 1 | 8.40 |
| CHEMBL537616 | — | — | 1 | 8.38 |
| CHEMBL535581 | — | — | 1 | 8.25 |
| CHEMBL535801 | — | — | 1 | 8.19 |
| CHEMBL440765 | U-69593 | — | 1 | 8.14 |
| CHEMBL290543 | — | — | 1 | 8.00 |
| CHEMBL557426 | — | — | 1 | 7.92 |
| CHEMBL558608 | — | — | 2 | 7.92 |
| CHEMBL118865 | SPIRADOLINE | 2.0 | 1 | 7.77 |
| CHEMBL559217 | — | — | 1 | 7.54 |
| CHEMBL558979 | — | — | 1 | 7.52 |
| CHEMBL541619 | — | — | 1 | 7.46 |
| CHEMBL537169 | — | — | 1 | 7.40 |
| CHEMBL539582 | — | — | 1 | 7.28 |
| CHEMBL537615 | — | — | 1 | 7.14 |
| CHEMBL354548 | — | — | 1 | 7.13 |
| CHEMBL536937 | — | — | 1 | 7.09 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.07 |
| CHEMBL535130 | — | — | 1 | 6.82 |
| CHEMBL537165 | — | — | 1 | 6.70 |
| CHEMBL538308 | — | — | 1 | 6.60 |
| CHEMBL534684 | — | — | 1 | 6.52 |
| CHEMBL556802 | — | — | 1 | 6.44 |
| CHEMBL535133 | — | — | 1 | 6.14 |
| CHEMBL536939 | — | — | 1 | 5.75 |
| CHEMBL556547 | — | — | 1 | 5.68 |
| CHEMBL559214 | — | — | 1 | - |
| CHEMBL535803 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL538309 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL544960 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL556957 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL537616 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL535581 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL535801 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL440765 | U-69593 | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL544960 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL290543 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL557426 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL558608 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL118865 | SPIRADOLINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL559217 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL558979 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL541619 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL537169 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL539582 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL537615 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL354548 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL536937 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL70 | MORPHINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL535130 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL537165 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL538308 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL534684 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL556802 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL535133 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL544960 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL558608 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL536939 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL556547 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL559214 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL535803 | — | Ki | > | 10000.0 | nM | - |