Assay Detail
Binding
CHEMBL755492
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Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | cos-7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 9.85 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 10.05 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.92 |
| CHEMBL330751 | — | — | 1 | 9.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL330751 | — | Ki | = | 0.27 | nM | 9.57 |