Assay Detail
Functional
CHEMBL2161464
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Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 8.76 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140278 | — | — | 1 | 8.92 |
| CHEMBL551074 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140278 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL551074 | — | EC50 | = | 2.6 | nM | 8.59 |