Assay Detail
Binding
CHEMBL3293115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human cloned mu opioid receptor expressed in CHO 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 | CHO |
| 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 | 9.89 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 10.15 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 10.05 |
| CHEMBL3291216 | — | — | 1 | 10.00 |
| CHEMBL3291215 | — | — | 1 | 9.62 |
| CHEMBL3291214 | — | — | 1 | 9.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL3291216 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3291215 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL3291214 | — | Ki | = | 0.24 | nM | 9.62 |