Assay Detail
Binding
CHEMBL753526
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Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.26 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.74 |
| CHEMBL96525 | — | — | 1 | 9.67 |
| CHEMBL92917 | — | — | 1 | 9.65 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.61 |
| CHEMBL92665 | — | — | 1 | 9.45 |
| CHEMBL2112373 | — | — | 1 | 9.29 |
| CHEMBL96609 | — | — | 1 | 9.28 |
| CHEMBL2112374 | — | — | 1 | 9.13 |
| CHEMBL93543 | — | — | 1 | 9.09 |
| CHEMBL96273 | — | — | 1 | 8.55 |
| CHEMBL330751 | — | — | 1 | 8.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL96525 | — | Ki | = | 0.214 | nM | 9.67 |
| CHEMBL92917 | — | Ki | = | 0.226 | nM | 9.65 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.244 | nM | 9.61 |
| CHEMBL92665 | — | Ki | = | 0.354 | nM | 9.45 |
| CHEMBL2112373 | — | Ki | = | 0.507 | nM | 9.29 |
| CHEMBL96609 | — | Ki | = | 0.529 | nM | 9.28 |
| CHEMBL2112374 | — | Ki | = | 0.745 | nM | 9.13 |
| CHEMBL93543 | — | Ki | = | 0.823 | nM | 9.09 |
| CHEMBL96273 | — | Ki | = | 2.83 | nM | 8.55 |
| CHEMBL330751 | — | Ki | = | 4.46 | nM | 8.35 |