Assay Detail
Binding
CHEMBL754082
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Compound was tested for binding affinity on intact HEK cells using [3H]diprenorphine as radioligand co-expressed with delta and kappa opioid receptors
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.54 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415006 | — | — | 1 | 9.52 |
| CHEMBL386810 | — | — | 1 | 9.30 |
| CHEMBL409172 | — | — | 1 | 8.85 |
| CHEMBL611140 | — | — | 1 | 6.50 |
| CHEMBL440626 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415006 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL386810 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL409172 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL611140 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL440626 | — | Ki | > | 1000.0 | nM | - |