Assay Detail
Functional
CHEMBL5365899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mu opioid receptor stably transfected in CHO cells assessed as decrease in DAMGO induced receptor activation by cAMP assay
8
Total Activities
8
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
Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.29 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5421526 | — | — | 1 | 7.77 |
| CHEMBL5414957 | — | — | 1 | 7.54 |
| CHEMBL5407379 | — | — | 1 | 7.42 |
| CHEMBL5403243 | — | — | 1 | 7.40 |
| CHEMBL5435711 | — | — | 1 | 7.25 |
| CHEMBL5397104 | — | — | 1 | 6.96 |
| CHEMBL5429557 | — | — | 1 | 6.68 |
| CHEMBL5424587 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5421526 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5414957 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5407379 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5403243 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5435711 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5397104 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5429557 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5424587 | — | IC50 | > | 3000.0 | nM | - |