Assay Detail
Functional
CHEMBL4040566
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Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay
16
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Opioid Receptor Modulators with a Cinnamyl Group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.59 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270190 | ALVIMOPAN | 4.0 | 2 | 8.52 |
| CHEMBL4100902 | — | — | 2 | 7.75 |
| CHEMBL80 | NALOXONE | 4.0 | 2 | 7.35 |
| CHEMBL4075084 | — | — | 2 | 6.19 |
| CHEMBL4104814 | — | — | 2 | 6.11 |
| CHEMBL4096255 | — | — | 2 | 5.90 |
| CHEMBL4081855 | — | — | 2 | 5.80 |
| CHEMBL4081523 | — | — | 2 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270190 | ALVIMOPAN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL270190 | ALVIMOPAN | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4100902 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL80 | NALOXONE | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4100902 | — | IC50 | = | 76.56 | nM | 7.12 |
| CHEMBL80 | NALOXONE | IC50 | = | 94.84 | nM | 7.02 |
| CHEMBL4075084 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4075084 | — | IC50 | = | 660.69 | nM | 6.18 |
| CHEMBL4104814 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4104814 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4096255 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4096255 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL4081855 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4081855 | — | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL4081523 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4081523 | — | IC50 | = | 2344.23 | nM | 5.63 |