Assay Detail
Binding
CHEMBL3293117
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Binding affinity to human cloned kappa opioid receptor expressed in HEK293 cells by radioligand displacement assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of three structurally related ¹⁸F-labeled orvinols of different intrinsic activities: 6-O-[¹⁸F]fluoroethyl-diprenorphine ([¹⁸F]FDPN), 6-O-[¹⁸F]fluoroethyl-buprenorphine ([¹⁸F]FBPN), and 6-O-[¹⁸F]fluoroethyl-phenethyl-orvinol ([¹⁸F]FPEO).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 10.11 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 10.70 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 10.15 |
| CHEMBL3291216 | — | — | 1 | 10.10 |
| CHEMBL3291215 | — | — | 1 | 9.92 |
| CHEMBL3291214 | — | — | 1 | 9.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL3291216 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3291215 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3291214 | — | Ki | = | 0.2 | nM | 9.70 |