Assay Detail
Functional
CHEMBL2422696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affinity and function.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 8.55 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.80 |
| CHEMBL2417568 | — | — | 1 | 8.97 |
| CHEMBL2419119 | — | — | 1 | 8.94 |
| CHEMBL2419122 | — | — | 1 | 8.91 |
| CHEMBL2419121 | — | — | 1 | 8.76 |
| CHEMBL2419124 | — | — | 1 | 8.58 |
| CHEMBL2419116 | — | — | 1 | 8.48 |
| CHEMBL522201 | — | — | 1 | 8.48 |
| CHEMBL2419118 | — | — | 1 | 8.34 |
| CHEMBL2419123 | — | — | 1 | 8.22 |
| CHEMBL2419125 | — | — | 1 | 8.14 |
| CHEMBL2419120 | — | — | 1 | 7.85 |
| CHEMBL2419117 | — | — | 1 | 7.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL2417568 | — | EC50 | = | 1.06 | nM | 8.97 |
| CHEMBL2419119 | — | EC50 | = | 1.14 | nM | 8.94 |
| CHEMBL2419122 | — | EC50 | = | 1.23 | nM | 8.91 |
| CHEMBL2419121 | — | EC50 | = | 1.74 | nM | 8.76 |
| CHEMBL2419124 | — | EC50 | = | 2.62 | nM | 8.58 |
| CHEMBL2419116 | — | EC50 | = | 3.32 | nM | 8.48 |
| CHEMBL522201 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2419118 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2419123 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2419125 | — | EC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2419120 | — | EC50 | = | 14.1 | nM | 7.85 |
| CHEMBL2419117 | — | EC50 | = | 19.4 | nM | 7.71 |